COMPOSITIONS TO REDUCE THE APPETITE AND THE ANSIA, TO POTENTIATE THE SACITY, TO IMPROVE THE STATE OF

专利摘要:
Compositions to reduce appetite and craving, enhance satiety, improve mood and reduce stress. A composition comprising: a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof; b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or c) a synergistic combination of (a) and (b); for use in the enhancement of at least one of reduction of craving, improvement of mood, avoidance of depression, prevention of weight gain after weight loss from diet, reduction of negative side effects produced by drugs that reduce Appetite and stop smoking and help healthy aging in a person who needs it. The composition for use can comprise a third active principle in combination with the extract of Cyperus esculentus and mangiferin or noratiriol. (Machine-translation by Google Translate, not legally binding)
公开号:ES2681996A2
申请号:ES201830028
申请日:2018-01-10
公开日:2018-09-17
发明作者:Miguel JIMÉNEZ DEL RÍO；Julia C. WIEBE；Laura LOPÉZ RÍOS；Tanausú VEGA MORALES；Rubén PÉREZ MACHÍN；Álvaro SÁNCHEZ RODRÍGUEZ；Carlos J. MATEOS；Nigel Peter Gericke
申请人:Nektium Pharma S L；Nektium Pharma Sl；
IPC主号:

专利说明:

Compositions to reduce appetite and craving, boost satiety, improve mood and reduce stress
Background 1. Technical field
This disclosure generally refers to compositions that reduce the craving for unhealthy foods, sugary and sweet drinks, products containing nicotine, or alcohol without producing unwanted physical or physiological side effects, while improving mood and mood. Stress is reduced simultaneously. 2. Description of the related technique
This disclosure refers to a composition that reduces craving and serves as a substitute for drugs to reduce appetite and to stop smoking. This new combination contains a plant extract of tiger nut, also known as chufa (Cyperus esculentus), and an extract that contains the compound xantonoid mangiferin that could be of different origin. For example, the extract containing mangiferin could be an extract of fruit, skin or mango leaf, honey bush tea, or an extract of coffee leaves.
Stop smoking, weight gain and relapse
Tobacco, which contains the addictive nicotine alkaloid, is highly addictive and one of the most widely used drugs in the world. According to WHO, around one billion men and 250 million women smoke worldwide. Half of them, 5.4 million a year worldwide, eventually die as a direct result of their tobacco addiction. The positive reinforcement effects of smoking include mild euphoria, relaxation and improved attention and functional memory, while quitting smoking leads not only to nicotine withdrawal, but also to a depressed mood, increased stress, irritability, anxiety and impaired memory and attention, increasing the risk of relapse to smoking. The drug rimonabant, an inverse agonist of CB1 cannabinoid receptor, decreases nicotine intake and the search for nicotine in rodents. Rimonabant has been shown to improve the ability of smokers to quit smoking in randomized clinical trials, but has been withdrawn from the market due to its serious psychiatric side effects and increased risk of suicide. The side effects of rimonabant are due to the reduction in mood improvement and the de-stressing activities of the endogenous endocannabinoid and opioid systems, and to the decrease in the elevation of dopamine, induced by nicotine and food in the reward zone of the brain, thereby leading to depression. One possible pharmaceutical treatment for improving mood to quit smoking is selegiline, a selective and irreversible inhibitor of monoamine oxidase B with antidepressant activity used primarily as a neuroprotective in Parkinson's disease. Selegiline primarily affects dopamine levels in the brain, but cholinergic entry affects nicotine-induced dopanimeric activity. Scientific evidence since 2013 suggests that targeting anxiety during early abstinence and adding attention to mood to behavioral support can improve smoking cessation outcomes.
Quitting smoking is often accompanied by metabolic changes including increased secretion of  cells in response to glucose and fasting insulin resistance. These alterations may be associated with or contribute to increased body weight after quitting smoking, which is supposedly a main reason why many smokers relapse after starting to quit smoking, followed by accompanying discouragement and depression related to the loss of reward response. The present combination decreases the craving, increases the electroencephalographic signaling of the neurotransmitters dopamine and serotonin, thereby attenuating the reduced reward response, and simultaneously improves mood and decreases emotional stress.
Overweight and obesity worldwide
In 2003, more than one billion adults in the world were overweight or obese. This number doubled in 2013, reaching 2 billion individuals in all age groups and making obesity the leading preventable cause of death in the world and the most serious burden on public health systems in the 21st century. In 2010, overweight and obesity produced approximately 3.4 million deaths worldwide, 3.9% of years of loss of life and 3.8% of years of life adjusted for disability. In 2013, the American Medical Association finally classified obesity as a disease. Both physical and psychological well-being are at risk in overweight and obese individuals due to the increased risk of cardiometabolic disease and the stigma of social discrimination, particularly in the western world. The pandemic increase in overweight and obesity in children and adults has led to widespread requests for regular monitoring of changes in the prevalence of overweight and obesity in all populations 1. Eating too much is the result of the imbalance between the circuits of the motivation related to conditioning and reward, and the circuits that control and inhibit the reward system and the cognitive and affective processes involved in the deregulation of eating behavior.
Caloric restriction
In contrast to the negative side effects of excess nutrition, calorie restriction is the only physiological intervention known to have a systematic and predictable effect on maintaining health and reducing disease risk, improving the quality of life and duration of health, and retarding aging, as demonstrated in multiple studies in various animal models. Many hormonal signals of peripheral tissues contribute to the regulation of energy homeostasis and food intake. These regulators, including leptin, insulin and ghrelin, modulate orexigenic and anorexigenic expression of neuropeptides in the hypothalamic nuclei. A negative energy balance seems to promote the activity of specific populations of neurons in these hypothalamic nuclei that lead to hunger. The anti-aging effects of caloric restriction have been explained from an evolutionary point of view as the adaptive response of neuroendocrine and metabolic response systems to maximize survival during periods of food shortage. In organisms, excess energy is stored in adipose tissues as triglycerides for such survival situations. Adipose tissue is increasingly recognized as an endocrine organ, and leptin, since it is secreted by adipocytes, appears to be an especially important factor for the adaptive response to fasting and neuroendocrine abnormalities under caloric restriction. Instead, deregulation of satiety signaling can have the opposite effect because it promotes metabolic overload in tissues, ultimately leading to chronic diseases. These observations have implications for the development of anti-obesity drugs, because compounds that target satiety pathways will ultimately promote homeostatic mechanisms that can prevent metabolic overload and, therefore, chronic disorders.
Drugs for obesity
The promising rimonabant anti-obesity anti-obesity drug was withdrawn from the market as it was associated with serious psychiatric side effects and increased risk of suicide. A stimulant drug that is also used as an appetite suppressant in weight control is methylphenidate, the most frequently used medication for the treatment of attention deficit / hyperactivity disorder (ADHD). In addition to suppressing appetite, a single dose of methylphenidate decreases energy intake in the form of fat and carbohydrates in obese adolescents. Methylphenidate selectively binds to and inhibits the dopamine transporter, thereby increasing dopamine levels in the brain, which mediate the reward value of food, shortly after oral administration. This effect highlights the importance of dopamine signaling of central origin on eating behavior.
Regulation of food intake
Regions and networks of the human brain involved in eating behavior and appetite control have been identified with neuronal imaging techniques such as functional MRI, PET, electroencephalography and magnetoencephalography. The hormones that regulate our tendency to eat (for example, leptin, insulin and glucagon-like peptide 1) can affect brain function.
The central nervous system (CNS) controls appetite and body weight regulation in a rather complicated way. The human brain integrates internal and external inputs to modulate energy homeostasis. It is currently considered that the homeostatic control performed by the hypothalamus is mainly responsible for controlling appetite, food intake, body weight and the development of obesity. The hypothalamic region is controlled by multiple signals that come from the digestive tract, adipose tissue and pancreas in the form of leptin, cholecystokinin (CCK), ghrelin, incretins, orexin, insulin, YY peptide, glucose, amino acids and fatty acids, reflecting the physiological situation of the body. The so-called reward effect, a physiological process associated with food intake, is related to the hypothalamus and other diverse brain regions, including the limbic region and the frontal cortex. The limbic region includes the nucleus accumbens, the tonsillar complex and the hippocampus. The neurotransmitter system of the frontal cortex responds to dopamine, serotonin, opioids and cannabinoids, and is closely related to the reward system and homeostasis of food intake regulation.
Neurotransmitters
The action of multiple neurotransmitters in relation to hunger is complex. Most of them are involved in homeostatic and reward mechanisms, depending on the physiological situation and the affected brain areas. The brain regions with dopaminergic connections are the ventral tegmental area (ATV), the accumbens nucleus, the dorsal stratum, the frontal cortex, the limbic regions, for example, the hippocampus, the tonsillar complex and the lateral hypothalamus. Although the release of dopamine is related to the feeling of reward as a reaction to food intake, exposure to photographs that represent food can also increase dopamine levels and lead to an increased desire for food.
Field potentials and EEG results
Neurotransmitter receptors and transporters represent the main targets of drugs in the central nervous system. The interaction of drugs with these molecules induces a signaling cascade, which eventually ends the control of the conductance of the ion channels. Since the electrical activity of the individual neurons depends on the set of active channels at a time, the communication between the neurons is governed by the activity of the channel. From here, it is obvious that the electric field potentials reflect the information of larger local networks of electrically active neurons, representing the interaction of drugs with their targets within the neurotransmission concert including the complex modulation of feedback loops. The frequency analysis of field potentials in the presence of drugs leads to the so-called electropharmacogram, which has been widely used to characterize the actions of drugs in rat and human brains. The comparison of the electropharmacogram of research compositions can be performed with the electropharmacograms of pharmaceutical and vegetable reference compounds, since the electropharmacogram similarity between the research composition and the reference compound indicates similarity in the activity of the CNS, and allows the understanding Health applications in humans. Dimpfel, W. 2015. Drug Discovery and Translational Medicine. Freienbrink Herstellung und Verlag. ISBN: 978-37386-7039-4, p. 47-54.
Increased alpha waves (8–12.99 Hz) in humans, such as during meditation for example, indicate a reduction in stress and anxiety, and that the brain is relaxed. Beta waves (13–29.99 Hz) range between 13–20 Hz during daily activity (beta-1 waves), while the presence of high-frequency  waves (beta-2 and beta-3 waves) indicates stress , excessive concentration and anger. Therefore, a composition that stimulates alpha waves and short-wavelength beta-1 waves, while stimulating beta-2 waves to a lesser extent, is expected to relieve stress and anxiety.
It has been found that CNS stimulants influence brain wave activity. It is well known in the art that the pattern of attenuation or stimulation and the type of brain wave activity reflects underlying brain activities including attention and depression. The anatomical location of the activity may also be related to specific brain functions, for example the activation of memory through the activation of the hippocampus. It has been shown that drowsiness and / or fatigue, for example, are correlated with a significant increase in alpha wave activity and a decrease in gamma wave activity. Papadelis et al., Proceedings of the 28th IEEE EMBS Annual International Conference, New York City, USA, August 30-September 3, 2006, p. 6201-6204. Increased gamma band EEG activity is associated with high activation, alert or attention states. The attenuation of the alpha and beta activity in the in vivo EEG of implanted brain electrodes is generally correlated with an increase in neurotransmission, resulting in increased effects of alertness, stimulation and antidrepressants. The midbrain dopamine center comprises a key network for reward, relevance, motivation and mood and the decreased functioning and metabolism of serotonin in the central nervous system is associated with depression. The release of specific neurotransmitters may be related to the antidepressant and anti-anxiety effect, as shown for drugs that modulate the activity of serotonin-dopamine such as brexpiprazole or the serotonin and norepinephrine reuptake inhibitor (SNRI) ZBH2012001.
Differences in brain wave activities could be related to diseases such as compulsive eating disorder in obesity (BE). The subjects show greater electrical activity of beta brain waves in EEG results than that of subjects without BE during the presentation of food, while no significant differences were found between the groups in the amplitudes of alpha, delta or theta.
This suggests that elevated frontal beta activity may be a marker of dysfunctional inhibition-inhibition mechanism, which could make obese women with BE more vulnerable or sensitive to food and environmental signals (Tammela et al., Clin. Physiol. Funct. Imaging., 2010, vol. 30, pp. 135-40). Therefore, a composition that suppresses the frontal electrical activity of beta brain waves can act to suppress the desire for excessive food.
Quitting smoking and nicotine withdrawal seem to affect brain wave activity, and nicotine deprivation among smokers may be associated with lower resting cortical activity (i.e., higher power density in theta EEG bands and alpha-1, which can be interpreted as a reduction in noradrenaline and serotonergic activity, and lower potency in the beta bands, in relation to an increase in glutamatergic / GABAergic neurotransmission). The comparison of low-frequency theta and alpha-1 waves during the satiety and nicotine deprivation states showed that they were higher in the very low nicotine state (deprivation) in relation to the superior nicotine state (satiety), while not Differences were shown in the alpha-2, beta-1 and beta-2 bands. Similarly, increased activity of theta waves was found in smokers who had abstained from smoking; administration of nicotine gum led to a reduction in the activity of teta waves. Similarly, the ratio of alpha-1 / alpha-2 was high in smokers who had abstained from smoking; administration of nicotine gum led to a reduction in the ratio of alpha-1 / alpha-2. The high activity of teta waves and a high ratio of alpha-1 / alpha-2 in cortical activity may be indicative of cognitive deficits related to withdrawal. A composition that suppresses the activity of slow-wave brain waves, for example, the activity of brain waves of theta and / or alpha-1 wave, or that elevates the activity of alpha-2 in relation to the activity of alpha- 1, can act to suppress the effects of nicotine withdrawal, and help a user reduce or stop smoking.
The present disclosure provides useful compositions for: reducing craving and appetite (mainly craving and appetite for high-calorie fatty or sweet foods, sugary and sweet drinks, and craving for smoking); prolong the duration of satiety after eating; reduce appetite; reduce weight gain after quitting smoking, and reduce the rate of relapse after smoking. Simultaneously, these compositions improve mood and act as antidepressants, and thereby counteract serious side effects in the mood of products that reduce craving and appetite such as rimonabant. The compositions disclosed herein reduce the craving and appetite for high-calorie foods, snacks and drinks, reduce the craving for smoking and do not cause nervousness, anxiety or depression, offer a CNS activation effect and serve to maintain health and prolong the duration of health and life expectancy by promoting calorie restriction from reduced cravings for high-calorie foods, snacks, sugary and sweet drinks, and reduced cravings for cigarettes in smokers, and reduced craving for alcohol
The compositions disclosed herein provide reduced appetite and cravings, enhanced satiety, decreased stress and improved mood over a relatively long period of time, but are substantially free of side effects and have no addictive potential, so which can be consumed over a prolonged period of time by a person or mammal.
The compositions disclosed herein may be included in food and beverage products including snack bars, chewing gum, sweets, meal replacement shakes, fruit smoothies, beverages, chocolate and energy drinks used for anti-craving purposes. and satiety enhanced to:
a) support a responsible and healthy weight control program for reduced calorie intake and exercise without the known negative side effects of complementary supplements and existing drugs that reduce appetite or boost satiety; Y
b) support smoking cessation programs by reducing nicotine cravings, at the same time
that related side effects such as depression, discouragement and
weight gain.
Metabolic health
Tiger nuts in animal models have been shown to improve serum lipid profiles and reduce elevated serum glucose, while it has been shown that mangiferin prevents hyperglycemia, and has antihyperlipidemic and antiatetrogenic activities. These activities of the compositions contribute additionally to health, well-being, healthy aging and longevity.
The foregoing objects and advantages of the invention are illustrative of those that can be achieved by the various exemplary embodiments and are not intended to be exhaustive or limiting of the possible advantages that can be realized. Therefore, these and other objects and advantages of the various exemplary embodiments will be apparent from the description herein or may be learned from the implementation of the various exemplary embodiments, both as they are made herein or as modified in view of any variation that may be apparent to those skilled in the art. Accordingly, the present invention resides in the novel methods, arrangements, combinations and improvements shown and described herein in various exemplary embodiments. Summary
In the light of the present need for effective anti-craving and satiety enhancement products with mood improvement and antidepressant effects, a brief summary of various known embodiments is presented. Such anti-anxiety and satiety enhancement products are necessary to help people involved in responsible weight control programs, maintain their weight after losing weight in a weight control program, or prevent weight gain after stopping smoke. Such anti-craving and appetite reduction products are required to help and support people to achieve their goals, without the side effects of depression, weight gain or relapse after the end of the program. Some simplifications and omissions can be made in the following summary, which are aimed at highlighting and introducing some aspects of the disclosed content, but not limiting the scope of the invention. Subsequent sections will follow the detailed descriptions of preferred embodiments, suitable to allow those of ordinary skill in the art to make and use the inventive concepts.
Various embodiments disclosed herein refer to a combination of two natural products to reduce craving, reduce appetite, boost satiety and reduce stress and improve mood, which contains a Cyperus extract. esculentus and mangiferina. The combination has an effect comparable to the appetite reduction effect provided by either rimonabant or methylphenidate, but does not have the negative disadvantages of these drugs. In addition, it has the ability to improve mood and reduce stress, as opposed to increased stress and discouragement or depression frequently associated with weight loss and smoking cessation programs, and with relapses observed with frequency after finishing such programs. This combination is based on functional foods and is not addictive. It can be combined with numerous natural compounds or plant extracts to obtain additional benefits or aromas or it can be added to existing formats, formulations and food products in various ways, for example being a liquid or a powder, granules, a gum or an envelope.
The components of the described invention are an aqueous or ethanolic extract of whole tiger nut or tiger nut skin, and pure mangiferin or a standardized vegetable extract for mangiferin, derived from the extraction of, for example, mango leaves, bark Mango, mango fruit or honey bush tea. These products can be part of different products and can be combined in different reasons and added to other components.
Various embodiments disclosed herein refer to methods to reduce craving, reduce appetite and boost satiety to avoid weight gain and relapse after quitting smoking, improve mood and reduce stress and stress. depression in a person who needs it, by administering an herbal composition to that person. The herbal composition may comprise an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof. In some embodiments, the herbal composition may comprise an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol. In other embodiments, the herbal composition may comprise a mixture of an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof; and an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol.
In various embodiments, the Cyperus esculentus skin extract and / or Cyperus esculentus rhizomes, or a combination thereof is an aqueous extract, an alcoholic extract.
or a hydroalcoholic extract. The extract of Cyperus esculentus can be a hydroalcoholic extract of the skin of rhizomes of Cyperus esculentus. Cyperus esculentus skin extract and / or Cyperus esculentus rhizomes can be used in an amount of between 20 mg and 20 g per dose.
In various embodiments, the herbal composition contains mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol, used in an amount of between 20 mg and 5 g per dose. In some embodiments, the herbal composition contains an extract comprising mangiferin or noratiriol in an amount sufficient to provide between 20 mg and 5 g of mangiferin or noratiriol per dose. The extract comprising mangiferin or noratiriol may be an extract containing mangiferin of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus , Coffea, and mixtures thereof.
Various embodiments disclosed herein refer to methods to reduce craving, reduce appetite, boost satiety, reduce stress and improve mood in a person or animal in need, by administering a composition. herbal to said person, by administering a mixture of an effective amount of:
a) an extract of the skin of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof; Y
b) an effective amount of mangiferin or an extract comprising mangiferin, where the ratio of (a) with respect to (b) is between about 1: 1 and about 50: 1, between about 1: 1 and 30: 1, between approximately
2: 1 and 25: 1, between approximately 1: 1 and 20: 1, between approximately 4: 1 and 15: 1, between approximately 10: 1 and 15: 1 or between approximately 12: 1. In various embodiments, the effective amount of (a) is between 20 mg and 20 g per dose; and the effective amount of said mangiferin or said extract containing mangiferin is between 5 mg and 5 g per dose. In some embodiments, the mixture of (a) and (b) is provided as a unit dose containing between about 10 mg and about 20 g per dose.
In various embodiments, the herbal compositions disclosed herein contain:
a) an herbal composition comprising:
i. a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
ii. an effective amount of mangiferin or an extract comprising mangiferin; or
iii. a mixture of (i) and (ii); in combination with:
b) an active substance to support weight control activity or to quit smoking selected from the group consisting of 5-hydroxytryptophan, vitamins of group B, caffeine, celastrol, citicoline, citrulline, choline, chromium picolinate, coenzyme Q10, curcumin , docosahexanoic acid, eicosapentanoic acid, ginsenosides, glycomapeptide, huperzine, hydroxycitrate, L-carnitine, L-carnosine, L-tryptophan, luteolin, ibogaine, magnesium, N-methylthiramine, oleamide, omega 3 fatty acids, octopamine, octopamine Phosphatidylserine, quercetin, raspberry ketones, rutin, resveratrol, synephrine, taurine, taxifoline, theanine, theobromine, witaferin A, xanthohumol, yangonin, yohimbine, ecdysteroids (20HE), extracts of Aphanizomenon flos-aqueae, and other cyanobacteria, Astrophyllumum, other cyanobacteria, Astrophyllum nodes and other microalgae, extracts of plant species of the genera Abelmoschus, Acacia, Acnistus, Adansonia, Aframomum, Aloysia, Alpinia, Amaranthus, Amorphophallus , Anacardium, Arachis, Astragalus, Bacopa, Cajanus, Capsicum, Carraluma, Celastrus, Chicorium, Cinnamomum, Ciser, Cissus, Crocus, Centella, Citrus, Coca, Cola, Curcuma, Coffea, Celastrus, Camellia, Eleutherococcus, Ephedraia, Garus , Ginkgo, Ganoderma, Glycyrrhiza, Griffonia, Gymnema, Hibiscus, Hoodia, Hordeum, Icarine, Ilex, Ipomoea, Irvingia, Kaempferia, Moringa, Murraya, Ocimum, Olea, Oreganum, Oryza, Paullinia, Panax, Persea, Phaseolus, Pinus , Pfaffia, Piper Pueraria, Punica, Rhodiola, Rhaponticum, Shisandra, Sida, Sideritis, Simondia, Solanum, Tabernanthe, Tamarindus, Theobroma, Tragaopogon, Trichocaulon, Trigonella, Tripterygium, Vicia, Vigna, Vitis, Withania, Zingiber, Zusiber, resistant Zusiber , non-starch polysaccharides, including galactamannan, guar gum, garrofin gum, tara gum, ispaghula, -glucans, konjac glucomaman, methylcellulose, gum tragacanth, detario, plant and animal based proteins, hydrolyzed proteins, and mixtures thereof.
Various embodiments disclosed herein refer to compositions and methods for reducing craving, reducing appetite, boosting satiety as well as raising mood, treating depression and reducing stress. Discouragement and depression are common side effects of pharmaceutical products to reduce appetite and boost satiety. The method comprises the replacement of drugs for the reduction of satiety and appetite for a product of the composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof, where the effective amount may be between about 20 mg and about 20,000 mg, between about 100 mg and about 5000 mg , between about 500 mg and about 4000 mg, or between about 1000 mg and about 3000 mg of the extract;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol, where the effective amount can be between about 10 mg and about 500 mg, between about 10 mg and about 350 mg, between about 10 and about 200 mg, between about 5 and about 150 mg, or between about 8 and about 100 mg of the extract; or
c) a synergistic mixture of (a) and (b).
Various embodiments disclosed herein refer to methods to reduce craving, reduce appetite, boost satiety while improving mood and reduce stress, prevent weight gain during and after leaving smoking, during calorie restriction diets responsible for maintaining health, facilitating healthy aging and longevity of a composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof, where the effective amount may be between about 20 mg and about 20,000 mg, between about 100 mg and about 5000 mg , between about 500 mg and about 4000 mg, or between about 1000 mg and about 3000 mg of the extract;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol, where the effective amount can be between about 10 mg and about 500 mg, between about 10 mg and about 350 mg, between about 10 and about 200 mg, between about 5 and about 150 mg, or between about 8 and
approximately 120 mg of the extract; or
c) a synergistic mixture of (a) and (b).
Either or both of Cyperus esculentus and mangiferin can be used to reduce craving, reduce appetite and boost satiety, alone or in combination with a product or weight loss program or a smoking cessation program. It is expected that both extracts, through their mood activation effects, have mood improvement and antidepressant activities comparable to selegiline and other antidepressants. These extracts are expected to reduce craving as effectively as rimonabant or methylphenidate. However, it has been shown that these natural functional food extracts lack the undesirable side effects associated with rimonabant and methylphenidate.
The combination of Cyperus esculentus and mangiferin leads to a reduction in craving, reduced appetite and enhanced satiety for food and reduced craving for tobacco and nicotine, a reduction in depression and stress, and improved mood. This is unexpected, since products for appetite reduction usually lead to depression, as observed with rimonabant.
The combination of Cyperus esculentus and mangiferin has an EEG signature that is comparable to that of pharmaceutical selegiline, which has an antidepressant effect. The signature of EEG in rats shows synergy for the attenuation of alpha-1 brain waves in vivo from electrodes implanted in rats, indicating the synergy of the composition to improve mood / treat depression, and reduce stress .
Various embodiments disclosed herein refer to a method for reducing the cravings for products containing nicotine, and alcohol in a person trying to quit smoking or reduce caloric intake, which comprises administering a composition to the person, where The composition includes:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b).
When the composition is administered to a person trying to quit smoking, the composition is administered in an amount effective to reduce at least one of theta brain wave activity and a ratio of alpha-1 / alpha-2 in the person.
When the composition is administered to a person trying to reduce caloric intake, the composition is administered in an amount effective to reduce food cravings by reducing the activity of beta brain waves in the person.
When the composition is administered to a person trying to quit smoking, the composition can be administered in an amount effective to:
reduce at least one activity of theta brain waves and a ratio of alpha-1 / alpha-2 in the person;
Y
reduce food cravings and avoid weight gain by said person by also reducing the activity of beta brain waves in said person.
Various embodiments disclosed herein refer to a method for reducing stress and improving mood in a human subject or person, which comprises administering a composition to the person where the composition comprises:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b);
wherein said composition is administered in an amount effective to modulate the activity of alpha brain waves in said person. In various embodiments, the person is under stress from attempts to lose weight, control food intake or quit smoking. The composition of Cyperus esculentus / mangiferin extract helps relieve this stress by modulating the activity of alpha brain waves. Reduced stress can prevent relapses in eating or smoking. Brief description of the drawings
In order to better understand various embodiments by way of example, reference is made to the accompanying drawings, in which:
Figure 1 shows encephalographic studies (EEG) in extracts of tuberous rhizome of Cyperus esculentus, mango leaf extract, extracts of tuberous rhizome of Cyperus esculentus plus mango leaf extract, rimonabant, methylphenidate and selegiline, where the statistical significance is designated as follows: * = p <0.10, ** = p <0.05, *** = p <0.01; Y
Figures 2A to 2D show the impact on neuronal activity in the frontal cortex, the hippocampus and the striatum of the control with saline solution (Figure 2A), tuberous rhizome of Cyperus esculentus, extract in 30% ethanol (Figure 2B), mango leaf extract containing 60% mangiferin (figure 2C) and a mixture of tuberous rhizome of Cyperus esculentus, 30% ethanol extract and mango leaf extract containing 60% mangiferin (figure 2D), where the statistical significance is designated as follows: * = p <0.10, ** = p <0.05, *** = p <0.01. Detailed description
The current application refers to herbal compositions to reduce craving and improve mood and depression / stress in a person in need, comprising administering a composition to said person, where the composition comprises:
a) an effective amount of an extract of Cyperus esculentus;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b).
In the current application, the term "approximately" encompasses the normal variability in the quoted quantities. In the context of an effective amount of a biologically active principle, the term "approximately" means that the actual amount of a dosage form is between 80% and 125%, between 90% and 110%, or between 95% and 105% of an established value. In the context of a ratio between biologically active principles, the term "approximately" means ± 20%, ± 10% or ± 5% of the established value.
In the current application, the term "a person who needs it" refers to any person
or human subject who needs a reduction in craving to support a weight control or anti-smoking program or who needs a mood improvement and antidepressant agent. Such human persons or subjects may be children, adolescents, adults.
or elders Such people or human subjects may be overweight, obese or smokers who need to reduce craving while avoiding depression or improving their mood during and after a weight loss program or to quit smoking, increasing from that compliance mode and reducing the risk of relapse.
Various embodiments disclosed herein refer to herbal compositions to reduce craving and improve mood, which comprise an effective amount of an extract of Cyperus esculentus. Cyperus esculentus extract can be an extract of the whole plant, or any part of the plant. The part of the Cyperus esculentus plant to be extracted may be the leaf, the skin, the root, the rhizome, the stem, the tuber, or a combination thereof. The extract of Cyperus esculentus can be a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, a skin derived from rhizomes of Cyperus esculentus, or a combination thereof. The part of the Cyperus esculentus plant can be extracted with water, an organic solvent, or a mixture thereof. The organic extraction solvent may be a polar aprotic solvent, such as DMSO, acetone, or a mixture thereof; or a polar protic solvent, such as a lower alcohol having from 1 to 4 carbon atoms. In various embodiments, the Cyperus esculentus extract is a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, a skin derived from rhizomes of Cyperus esculentus, or a combination thereof, derived by extraction with water, a lower alcohol having from 1 to 4 carbon atoms, or a mixture thereof. In some embodiments, the Cyperus esculentus extract is a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, a skin derived from rhizomes of Cyperus esculentus, derived by extraction with a hydroalcoholic mixture of water and ethanol. The extract can be obtained from extraction by subcritical or supercritical CO2.
Various embodiments disclosed herein refer to herbal compositions to reduce craving and improve mood, which
5 comprise mangiferin or noratiriol. Mangiferin has a structure of formula Ia, where R is a ring of 1,5-anhydro-D-glucitol. Noratiriol is a mangiferin aglycone, and has a structure of formula Ib, where R is hydroxyl. Unless otherwise indicated, the term mangiferin is defined herein as encompassing:
10 mangiferin as a pure compound, where “pure” is defined as meaning that the compound has at least 90% mangiferin, at least 95% mangiferin, at least 98% mangiferin or at least 99.5% mangiferin; or
a composition comprising at least 90% by weight of a mixture of mangiferin and noratiriol.
Ia: R = 1,5-anhydro-D-glucitol 20 1b: R = —OH
Mangiferin is a xantonoid polyphenol. Mangiferin is found in several plant components, including extracts of mango fruit, mango skin, bark of
25 mango and / or mango leaf, as well as in extracts of various species of Cyclopia, for example, honey bush tea and extracts of species of the genus Salacia. Mangiferin has acetylcholinesterase inhibition activity, a useful activity to improve cognitive function in Alzheimer's disease.
30 Mangiferin, an xantonoid, is a natural phenolic compound formed from the main xanthone structure. If reference is made to mangiferin, its aglycone, noratiriol, is always included as an alternative component. Mangiferin is an antioxidant and anti-inflammatory agent that has various pharmacological activities, including antidiabetic, anticancer and antioxidant effects, as well as anti-inflammatory, antiviral, immunomodulatory and antimicrobial activities. With mangiferin, the prevention of stress-induced effects related to neurodegenerative diseases, the reduction of neurological brain deficiencies and a positive effect on damaged neurons has been reported, indicating that mangiferin can play a role in pathologies related to neuroinflammation and damage oxidative Mangiferin can also enhance recognition memory and improve memory deficiencies, while MAOA inhibition seems to be responsible for its antidepressant effect. In the literature no effects have been described that indicate a reduction in craving.
The mangiferin of the invention can be extracted from a plant containing mangiferin. Excellent sources of the desired material are Mangifera indica (fruit, bark or leaf) or honey bush tea, which are preferably normalized to a concentration of 20-70% mangiferin, depending on the starting material. However, mangiferin can be obtained from other sources, including plant species of the genera Mangifera, Salacia, Cyclopia, Hypericum, Mangifera, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus and Coffea.
The tiger nut (Cyperus esculentus), a crop of the Ciperaceae family widely spread throughout the world, is a typical Spanish food found in markets and supermarkets. In Spain, the milky extract of tiger nut (that is, “horchata de chufa”), a non-alcoholic beverage, has an annual economic impact of 60 million euros. Tiger nut is rich in fiber, protein, sugars, oleic acid and glucose, as well as phosphorus, potassium and vitamins C and E. Tiger nut is useful for improving blood circulation, preventing heart disease and reducing risk of colon cancer. The scientific literature has not described any effect of chufa on reducing cravings, for example, craving for food or tobacco, or improving mood.
The 30% aqueous and ethanolic extracts of whole tiger nut and tiger nut skin contain high amounts of fat and carbohydrates, but no detectable alkaloids or flavonoids. The extracts have a very pleasant and sweet taste, so no restriction has to be made due to the taste. The oral ingestion of 4 g of tiger nut extract provides a reduction in craving as well as a calming effect.
It has now been found according to the present invention that the combination of tiger nut and mangiferin serves to moderate the bitter taste and the unusual aroma of mangiferin. In addition, the combination electropharmacogram is remarkably similar to rimonabant and methylphenidate (Ritalin) electropharmaceuticals, both appetite and selegiline inhibitors (an antidepressant drug and an antiparkinsonian drug used successfully to quit smoking and as an antidepressant) (Figure 1) . In addition, the invention resulted in synergistic attenuation of the alpha 1 and alpha 2 brain waves of the hippocampus in rats (Figure 2D), which represents an activation of the neurotransmitters serotonin and dopamine, which are closely related to the reward system. and homeostasis regulating food intake.
Mangiferin and its aglycone metabolite, noratiriol, can be included in the compositions disclosed as pure compounds, or as components of an extract of a plant species in a genus selected from the group consisting of
Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, Coffea and mixtures thereof. The plant species contain mangiferin and / or noratiriol, and can be extracted with water, an aqueous base, a polar protic organic solvent, a polar aprotic organic solvent, or a mixture thereof. In various embodiments, the plant species comprises mangiferin and is extracted with water, a lower alcohol having 1 to 4 carbon atoms, or a mixture thereof.
In various embodiments, the herbal composition contains mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol, used in an amount of between 20 mg and 5 g per dose. The herbal composition may contain an extract comprising mangiferin or noratiriol of between 20 mg and 5 g per dose. If the concentration of mangiferin and / or noratiriol in the extract is known, the extract can be provided in an amount sufficient to provide between 20 mg and 5 g of mangiferin or noratiriol per dose. Therefore, for example, if an extract of a plant of the genus Mangifera contains 30% of mangiferin, the extract can be provided in an amount of between 20 mg and 5 g per dose, based on the weight of the extract. Alternatively, Mangifera extract can be administered in an amount of between 66.7 mg and 16.7 grams per dose, to provide between 20 mg and 5 g of mangiferin per dose.
Various embodiments disclosed relate to herbal compositions containing tigernut or nut nut extracts and plant extracts containing mangiferin, where the compositions are effective in improving CNS activity in the frontal cortex, hippocampus and striatum. In various embodiments, the compositions are effective for the reduction of cravings, as shown by the increased activity of alpha waves in the brain. The compositions are also effective in improving mood and reducing depression, as shown by the similarity with selegiline and increased serotonin release, indicated by the reduction of alpha-1 waves in rat EEG.
Through encephalographic studies (EEG) of animals, the current application shows that tiger nut or nut extracts (prepared by the extraction of tuberous rhizome from Cyperus esculentus) and mangiferin (as a pure compound) and plant extracts containing mangiferin They are remarkably similar to each other in the CNS profile. In addition, they are surprisingly similar in activity to the known appetite reduction agent rimonabant and methylphenidate. Chufa extracts are less potent than mangiferin. In a human adult subject, approximately 4 grams of chufa extract have approximately the same activity as approximately 400 mg of mangiferin.
The key findings presented herein are that the extracts of Cyperus esculentus and mangiferin have a very similar CNS activation effect (as evidenced by EEG) with each other and rimonabant, methylphenidate and selegiline. However, unlike rimonabant, the extracts of Cyperus esculentus and mangiferin also have a calming, de-stressing activity when ingested. In addition, the extracts of Cyperus esculentus and mangiferin have a plateau effect. Beyond a certain threshold value, an increased intake of these extracts does not give a greater CNS stimulation, minimizing the potential for abuse. Even with high portions or doses, the extracts of Cyperus esculentus and mangiferin do not present any of the well-known side effects, for example, drowsiness and depression, caused by excessive doses of rimonabant or methylphenidate.
In the prior art, chufa skins have generally been considered to be a waste product of chufa processing. However, it has been discovered that an extract in 30% ethanol - water from chufa skins, for example, skins from tuberous rhizomes from chufa, have a more potent activation activity than an extract in 30% ethanol - water from the complete chufa, which in turn has a more potent activity than an extract in water from the complete chufa. However, the ethanol, aqueous and hydroalcoholic extracts of chufa tuberous rhizomes all have desirable CNS activation activity.
In various embodiments, tigernut or nut nut extracts and vegetable extracts containing mangiferin can be taken as individual active ingredients. Tiger nut or tiger nut extracts are desirably taken by an adult human in an amount of about 0.1 g / day to about 10 g / day, from about 0.5 g / day to about 8 g / day, from about 1 g / day to about 5 g / day, or from about 1 g / day to about 4 g / day. Plant extracts containing mangiferin are desirably taken by an adult human in an amount of about 25 mg / day to about 5 g / day, from about 50 mg / day to about 2 g / day, from about 100 mg / day at about 1 g / day, or from about 200 mg / day to about 400 mg / day.
Tiger nut or tiger nut extracts and vegetable extracts containing mangiferin have synergistic activity on the activity of alpha-1 and alpha-2 brain waves in the hippocampus. The increase in the activity of alpha waves in the hippocampus, comparable to that of rimonabant and methylphenidate, is proof that the composition increases the effect against craving. Tiger nut or tiger nut extracts and vegetable extracts containing mangiferin are desirably combined in a ratio of between about 0.5: 1 and about 30: 1, between about 1: 1 and about 20: 1, between about 5: 1 and approximately 10: 1 and approximately 7.5: 1.
Tiger nut or tiger nut extracts and vegetable extracts containing mangiferin, whether taken separately or together, have a rapid onset of action. Within one hour after oral ingestion, or within 15-20 minutes after absorption by the jugular mucosa, the EEG results show an impact of the extracts on neuronal activity. The extracts have a long duration of action, between 3-6 hours. When chufa or tiger nut extracts and vegetable extracts containing mangiferin are combined and ingested together, the duration of action is at least 5 hours, and the effect of the combination on brain wave activity after 5 hours It is significantly greater than the effect on brain wave activity of any individual extract 5 hours after ingestion.
People who have ingested tigernut or nut nut extracts and vegetable extracts containing mangiferin as disclosed herein, taken individually or together, report that the extracts reduce craving. People who have ingested tiger nut or tiger nut extracts and vegetable extracts containing mangiferin as disclosed herein, taken individually or together, report that the extracts improve motivation and elevate mood, while which simultaneously induce a feeling of calm, reduced anxiety and stress, reduced tension and nervousness, and reduced impulsivity. Unlike rimonabant, even at very high doses, the extracts do not produce discouragement, depression or increase the risk of suicide.
Tiger nut or tiger nut extracts and vegetable extracts containing mangiferin as disclosed herein are not bitter, have a pleasant taste and are perfectly suitable for application in beverages and functional foods. Extracts can be used to reduce craving and improve mood in food, drinks and complementary contributions without causing depression or anxiety. As previously mentioned, the herbal compositions disclosed herein contain a herbal composition comprising:
a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
an effective amount of mangiferin or an extract comprising mangiferin; or
a mixture of a skin extract or rhizomes of Cyperus esculentus and mangiferin or an extract comprising mangiferin.
The claimed compositions may comprise:
i) from about 10% to about 95% by weight, from about 25% to about 90% by weight, from about 40% to about 85% by weight or from about 50% to about 80 % by weight, of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof; and from about 5% to about 90% by weight, from about 10% to about 75% by weight, from about 15% to about 60% by weight, or from about 20% to about 50 % by weight of an additional component to improve mood or reduce stress or anxiety;
ii) from about 10% to about 95% by weight, from about 25% to about 90% by weight, from about 40% to about 85% by weight or from about 50% to about 80 % by weight, of mangiferin or an extract comprising mangiferin; and from about 5% to about 90% by weight, from about 10% to about 75% by weight, from about 15% to about 60% by weight or from about 20% to about 50% by weight of the additional component to improve mood or reduce stress or anxiety; or
iii) from about 10% to about 95% by weight, from about 25% to about 90% by weight, from about 40% to about 85% by weight or from about 50% to about 80 % by weight of a mixture of
to. an extract of skin and / or rhizomes of Cyperus esculentus and
b. mangiferin or an extract comprising mangiferin; Y
from about 5% to about 90% by weight, from about 10% to about 75% by weight, from about 15% to about 60% by weight or from about 20% to about 50% by weight Additional component weight to improve mood or decrease stress or anxiety.
c) This additional component to further improve mood or to reduce depression, stress or anxiety is selected from the group consisting of 5-hydroxytryptophan, group B vitamins, caffeine, citicoline, citrulline, choline, chromium picolinate, coenzyme Q10, curcumin, glyomacropeptide, huperzine, hydroxycitrate, L-carnitine, L-carnosine, L-tryptophan, luteolin, ibogaine, magnesium, N-methylthyramine, oleamide, omega 3 fatty acids, octopamine, phenylalanine, phenylethylamine, quercidinetin, phosphatidylserine of raspberry, rutin, resveratrol, synephrine, taurine, taxifoline, theanine, theobromine, xanthohumol, yangonin, yohimbine, ecdysteroids (20HE), extracts of Aphanizomenon flos
aqueae and other cyanobacteria, Ascophyllum nodosum, Chlorella and other microalgae, extracts of plant species of the genera Aframomum, Aloysia, Alpinia, Astragalus, Bacopa, Capsicum, Carraluma, Chicorium, Cinnamomum, Ciser, Cissus, Crocus, Centella, Citrus, Coca, Cola, Curcuma, Coffea, Celastrus, Camellia, Eleutherococcus, Ephedra, Euterpe, Garcinia, Ginkgo, Ganoderma, Glycyrrhiza, Griffonia, Gymnema, Hoodia, Hordeum, Hypericum, Icarine, Ilex, Ipomoea, Irvingia, Kaumferia, Ocumre, Ocum, Occupation Paullinia, Panax, Persea, Phaseolus, Pinus, Prunus, Pfaffia, Piper Pueraria, Punica, Rhodiola, Rhaponticum, Shisandra, Sida, Sideritis, Simondia, Solanum, Tabernanthe, Tamarindus, Theobroma, Tragaopogon, Trichocaulon, Trigonella, Vicia, Vitis, Vicia Withania, Zingiber, Zizyphus, non-starch polysaccharides, including galactamannan, guar gum, garrofin gum, tara gum, ispaghula, -glucans, glucomannan konjac, methylcellulose, gum tragacanth, detario, and mixtures thereof mos.
Mangiferin and Mangifera extracts can be incorporated in an oral dosage form, including a oral strip that can be dispersed or dissolved orally, a chewing gum, a tablet, a capsule, an emulsion, a suspension, an oral spray, powder
or granules that can dissolve, effervescent, an envelope, or a transparent drink. Chufa extracts, alone or in combination with mangiferin and Mangifera extracts, are usually opaque and milky in the form of a drink, and can be incorporated into an oral dosage form, including a oral strip that can be dispersed or dissolved orally, a chewing gum, a tablet, a capsule, powder or granules that can be dissolved, an envelope, an emulsion, a suspension, milk milk, non-milk milks, yogurt, and milk-fruit juice combinations.
The compositions disclosed herein may be provided as:
a yugal strip that can be dispersed or dissolved orally for mucosal absorption, a chewing gum, a chewable tablet, a lozenge, an effervescent tablet, a capsule or an emulsion;
a chocolate, marzipan or functional sweet,
a functional spreadable substance in measured doses in an aluminum foil envelope, which is to be spread on bread or biscuits;
a powder with a measuring spoon for addition to any beverage or food;
a lozenge;
an oral or nasal spray;
a non-dairy cream in the form of an envelope or bar to add to a drink; Y
a snack bar, caramel or cookie.
The compositions disclosed herein may be used for cravings in weight control programs or for smoking cessation and may be added to all types of formats, replacing the pharmaceutical products currently used for appetite reduction or satiety.
However, it also loses the harmful side effects of rimonabant, including depression and the risk of suicide. The elimination of all or part of the drug in a product with a skin extract and / or rhizomes of Cyperus esculentus, mangiferin or an extract comprising mangiferin, or a mixture thereof allows the side effects of this drug to be eliminated (by example, rimonabant), while restoring the stimulating activity of the desired CNS. It is estimated that approximately 2 grams of chufa extract is equivalent to 10 mg of rimonabant or 10 mg of methylphenidate. Similarly, mangiferin and extracts containing mangiferin can be used to reduce the craving for a complementary food, drink or intake. It is estimated that about 100 to about 200 mg of mangiferin is equivalent to 10 mg of rimonabant or 10 mg of methylphenidate.
A composition that combines Cyperus esculentus extract and mangiferin in a ratio between approximately 20: 1 and 1: 1 can be used instead of 10 mg of rimonabant or 10 mg of methylphenidate. From about 20 mg to about 200 mg of the combination of Cyperus esculentus / mangiferin extract can be used to replace 10 mg of rimonabant or 10 mg of methylphenidate. The combined extract of Cyperus esculentus-mangiferin or the plant extract containing mangiferin is used in an amount between 10 mg and 20 g for the replacement of rimonabant or methylphenidate.
The extract composition of Cyperus esculentus / mangiferin according to the invention can be a simple mixture of the two components after the extraction procedure. The invention may advantageously include additional components in order to further increase the craving effect and the positive effect on weight loss.
or quit smoking Therefore, it may be advantageous to add, for example, other components of appetite reduction, mood improvement, anti-obesity or anti-craving to the combined product presented, to enhance the anti-craving effect provided by the present invention. The same products can also be added to Cyperus esculentus extract or to mangiferin separately.
To improve other aspects of the invention, such as the effect on mood and well-being, natural products such as Ganoderma, Garcinia Kola and Astragalus can be combined with the composition. Components that enhance absorption and bioavailability, such as piperine, capsaicin or ginger, may be added. Natural and artificial sweeteners and aromas such as coffee, vanilla, hazelnut, chocolate, cream or fruit can be integrated. Nutrients such as omega 3 fatty acids, vitamins and minerals can be added. For athletes, adaptogens including Withania and Rhodiola, products that improve muscle health and recovery such as the amino acids citrulline and phosphatidylserine, natural nitrate sources including spinach and beets, anabolic or anti-catabolic components such as ecdisterones and ursolic acid, and antioxidants can be added. Suitable antioxidants that include polyphenols with antioxidant or xanthine oxidase inhibitors effects can be added. Representative polyphenols include green tea catechins, cocoa polyphenols, grape resveratrol, Polygonum or Gnetum gnemon seeds, Humulus lupulus xanthohumol, and luteolin, rutin or quercetin.
The extract composition of Cyperus esculentus / mangiferin can be combined with anti-craving products, to lose weight or anti-smoking such as Hoodia, Curcuma and ginger, and / or mood improvement products such as Ginkgo, citicoline or huperzine.
The amount of the additional component included in the composition of the present invention varies depending on the characteristics of each additional component. The invention can be combined, for example, with an antioxidant in a ratio of from 1:50 to 50: 1.
The composition has a wide range of applications useful for industry: it can be provided in liquid, syrup or solid (compressed) or powdered or granulated or rubber form or can be incorporated into foodstuffs of liquid, solid (compressed), syrup consistency , granulated or powdered. The liquid can be presented in concentrated form to be diluted by mixing it with teas, coffee, water or milk, juices, yogurts or fruit smoothies to provide the final consumable liquid beverage that provides the reduction of craving normally associated with rimonabant and the benefits of state improvement of spirit. The concentration of the present invention varies depending on the format, purpose and / or additional components of the product.
The compositions disclosed herein can be used to replace pharmaceutical products currently used for appetite or satiety reduction, in particular rimonabant and methylphenidate. In certain embodiments, approximately 2 to 5 grams of Cyperus esculentus extract has an activity that is equivalent to 5.5 to 14.5 mg of rimonabant or 5.5 to 14.5 mg of methylphenidate; approximately 3 to 4 grams of Cyperus esculentus extract has an activity that is equivalent to 8.5 to 11.5 mg of rimonabant or 8.5 to 11.5 mg of methylphenidate; or approximately 3.5 grams of Cyperus esculentus extract has an activity that is equivalent to 10 mg of rimonabant or 10 mg of methylphenidate. Similarly, about 100 to about 400 mg of mangiferin is equivalent to about 10 to 40 mg of rimonabant or about 2 to 8 mg of methylphenidate; from about 200 to about 300 mg of mangiferin is equivalent to about 20 to 30 mg of rimonabant or about 4 to 6 mg of methylphenidate; or about 250 mg of mangiferin is equivalent to about 25 mg of rimonabant or 5 mg of methylphenidate.
A composition that combines extract of Cyperus esculentus and mangiferin in a ratio between approximately 20: 1 and 1: 1 can be used to reduce cravings. From about 20 mg to about 200 mg of the combination of Cyperus esculentus / mangiferin extract can be used to replace 5 mg to 50 mg of rimonabant or 1 to 10 mg of methylphenidate; or approximately 100 mg of the combination of Cyperus esculentus / mangiferin extract can be used to replace 25 mg of rimonabant or 5 mg of methylphenidate. The combined extract of Cyperus esculentusmangiferina or the vegetable extract containing mangiferin can be used in an amount between 10 mg and 20 g to replace 10 mg of rimonabant or for the replacement of 10 mg of methylphenidate.
The composition of the invention may also be a pharmaceutical composition, further comprising a pharmaceutically acceptable excipient. Non-limiting examples of said pharmaceutically acceptable excipients include water, an alcohol such as ethanol or mixtures thereof.
The invention can also be described by the following embodiments:
Embodiment 1: a composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b);
for use in reducing cravings for at least one of high-calorie foods, sugary and sweet drinks, products containing nicotine, and alcohol in a person who needs it.
Embodiment 2: The composition for use according to Embodiment 1, in which said person is trying to quit smoking; and said composition reduces the cravings for products containing nicotine in said person.
Embodiment 3: The composition for use according to embodiment 1 or embodiment 2, wherein said composition is administered in an amount effective to reduce the activity of theta brain waves and the ratio of alpha-1 / alpha-2 in said person.
Embodiment 4: The composition for use according to Embodiment 1, in which said person is trying to reduce caloric intake; and said composition reduces food cravings in said person; wherein said composition is administered in an amount effective to reduce the activity of beta brain waves in said person.
Embodiment 5: The composition for use according to embodiment 3, wherein said composition further reduces the craving for food in said person; wherein said composition is administered in an amount effective to reduce the activity of theta brain waves, the activity of the beta brain waves, and the ratio of alpha-1 / alpha-2 in said person.
Embodiment 6: a composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b);
for use in reducing stress and improving mood in a person, in which said composition modulates the activity of alpha brain waves in said person.
Embodiment 7: The composition for use according to any one of embodiments 1 to 5, wherein said composition comprises said Cyperus esculentus skin extract, Cyperus esculentus rhizomes, or a combination thereof.
Embodiment 8: The composition for use according to any one of embodiments 1 to 5 or 7, wherein said skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus,
or a combination thereof is an aqueous extract, an alcoholic extract or a hydroalcoholic extract, or a subcritical or supercritical CO2 extract.
Embodiment 9: The composition for use according to any one of embodiments 1 to 5
or embodiments 7 or 8, wherein said extract composition comprises a hydroalcoholic skin extract of rhizomes of Cyperus esculentus.
Embodiment 10: The composition for use according to any one of embodiments 1 to 5, or embodiments 7 to 9, wherein said effective amount of said skin of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof is between 20 mg and 20 g per dose.
Embodiment 11: The composition for use according to any one of embodiments 1 to 5, wherein said composition comprises said effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol.
Embodiment 12: The composition for use according to embodiment 11, wherein said effective amount of said mangiferin or said noratiriol is between 20 mg and 5 g per dose.
Embodiment 13: The composition for use according to embodiment 11, wherein said effective amount of said extract comprising mangiferin or noratiriol is sufficient to provide between 20 mg and 5 g of mangiferin or noratiriol per dose.
Embodiment 14: The composition for use according to any one of embodiments 1 to 5, or embodiments 11 to 13, wherein said extract comprising mangiferin or noratiriol is an extract containing mangiferin from a plant species in a genus selected from group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and mixtures thereof.
Embodiment 15: The composition for use according to any one of embodiments 1 to 5, wherein said composition comprises said synergistic combination of (a) and (b).
Embodiment 16: The composition for use according to embodiment 15, wherein (a) is an aqueous extract, an alcoholic extract or a hydroalcoholic extract of Cyperus esculentus skin, rhizomes of Cyperus esculentus, or a combination thereof.
Embodiment 17: The composition for use according to any one of embodiments 15 or 16, wherein (a) comprises a hydroalcoholic extract of rhizome skin of Cyperus esculentus.
Embodiment 18: The composition for use according to any one of embodiments 15 to 17, wherein (b) comprises mangiferin or an extract containing mangiferin of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia , Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and mixtures thereof.
Embodiment 19: The composition for use according to any one of embodiments 15 to 18, wherein the ratio of (a) to (b) is between about 1: 1 and about 50: 1.
Embodiment 20: The composition for use according to any one of embodiments 15 to 18, wherein the ratio of (a) to (b) is between about 1: 1 and about 20: 1.
Embodiment 21: The composition for use according to any one of embodiments 15 to 18, wherein the ratio of (a) to (b) is between about 4: 1 and about 15: 1.
Embodiment 22: The composition for use according to embodiment 18, wherein said effective amount of (a) is between 20 mg and 20 g per dose; and said effective amount of said mangiferin or said extract containing mangiferin is between 5 mg and 5 g per dose.
Embodiment 23: The composition for use according to any one of embodiments 15 to 19, wherein said composition is provided as a unit dose containing between 10 mg and 20 g per dose.
Embodiment 24: The composition for use according to any one of embodiments 1 to 5 or 7 to 23 or the composition for use according to embodiment 6, wherein said composition further comprises an active ingredient selected from the group consisting of 5-hydroxytryptophan, Group B vitamins, caffeine, citicoline, citrulline, choline, chromium picolinate, coenzyme Q10, curcumin, glycomacropeptide, huperzine, hydroxycitrate, L-carnitine, L-carnosine, L-tryptophan, luteolin, ibogaine, magnesium, N-methylthiramine, oleamide, omega 3 fatty acids, octopamine, phenylalanine, phenylethylamine, phosphatidylserine, quercetin, raspberry ketones, rutin, resveratrol, synephrine, taurine, taxifoline, theanine, theobromine, xanthohumol, yangonin, yohimbine, ecdysteoson (20H Aphanos) and other cyanobacteria, Ascophyllum nodosum, Chlorella and other microalgae, extracts of plant species of the Aframomum, Aloysia, Alpinia, Astragalus, Bacopa genera, Capsicum, Carraluma, Chicorium, Cinnamomum, Ciser, Cissus, Crocus, Centella, Citrus, Coca, Cola, Curcuma, Coffea, Celastrus, Camellia, Eleutherococcus, Ephedra, Euterpe, Garcinia, Ginkgo, Ganoderma, Glycyrrhma, Griffonia, Gymnastics, Griffonia, Gymnastics Hordeum, Icarine, Ilex, Ipomoea, Irvingia, Kaempferia, Ocimum, Olea, Oreganum, Paullinia, Panax, Persea, Phaseolus, Pinus, Prunus, Pfaffia, Piper Pueraria, Punica, Rhodiola, Rhaponticum, Shisandra, Sida, Sideritis, Simondia, Soondum, Simondia, Soondum , Tabernanthe, Tamarindus, Theobroma, Tragaopogon, Trichocaulon, Trigonella, Vicia, Vigna, Vitis, Withania, Zingiber, Zizyphus, polysaccharides other than starch, including galactamannan, guar gum, garrofin gum,
Tara gum, ispaghula, -glucans, konjac glucomaman, methyl cellulose, tragacanth gum, detario, and mixtures thereof. Embodiment 25: a composition comprising: a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof; b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or c) a synergistic combination of (a) and (b);
for use in reducing appetite and enhancing satiety in a person. Embodiment 26: A pharmaceutical composition comprising a composition according to embodiment 1, or according to embodiment 6, or according to embodiment 25, further comprising a pharmaceutically acceptable excipient.
Example 1 Test subjects: Fisher 344 rats (11 months old and with day-night conversion, weight of approximately 350-400 g, provided by Charles River Laboratories, D97633, Sulzfeld) were used in a series of experiments on the effects of various products
Herbal and pharmaceutical on the activity of the central nervous system. The products areprovided test subjects orally (nasogastric tube).Test substances: The substances tested in this study included:a control vehicle (0.9% NaCl);Ethanol extract of tuberous rhizome of Cyperus esculentus, administered in an amount
from 200 mg / kg to 7 rats;mango leaf ethanol extract, administered in an amount of 50 mg / kg to 7 rats;
Ethanol extract of tuberous rhizome of Cyperus esculentus skin, 150 mg / kg, plus mango leaf extract, containing 60% mangiferin, 50 mg / kg, administered to 5 rats
selegiline, administered in an amount of 1.5 mg / kg to 8 rats
methylphenidate administered in an amount of 1.0 mg / kg to 8 rats
Rimonabant administered in an amount of 5 mg / kg to 6 rats
The EEG signals were recorded by means of telemetry of 4 electrodes implanted in the frontal cortex, the hippocampus and the striatum of rats that moved freely within a room totally protected with copper. The signals were collected in sweeps of 4 seconds duration and fast Fourier transform using a Hanning window. EEG signals were recorded over a period that began 5 minutes after administration of the test substances, and ended 65 minutes after administration of the test substances. The sampling frequency was 512 Hz. The spectra were averaged in stages of 3 minutes each and displayed online. In an offline procedure, the spectra were averaged to give longer periods for analysis and presentation of additional data. Spectral activity was recorded within the frontal cortex, hippocampus, striatum and reticular formation. Oral administration of the control vehicle (0.9% NaCl) only resulted in minor changes in spectral power within the four brain regions.
Through these encephalographic studies (EEG) with animals in vivo, it has surprisingly been discovered that Cyperus esculentus tuberous rhizome extracts, mangiferin, mangiferin-containing plant extracts and the combination of Cyperus esculentus tuberous rhizome extract and non-mangiferin They are only remarkably similar in the CNS profile to each other, but are also surprisingly similar to rimonabant, methylphenidate and selegiline reference. As shown in Figure 1, during the first hour of registration, each of these extracts or compounds provides a decrease in spectral potency in the EEG in vivo in the frontal cortex, and some decrease in brain waves in the hippocampus , the striatum and the reticular formation. Such decreases correlate with an activation of neurotransmission. As shown in Figure 1, the main significant effect of rimonabant, methylphenidate and selegiline on neuronal activity in all brain areas refers to alpha-2 (green) (p <0.01, relative to the initial level before the drug), in relation to dopaminergic neurotransmission. Cyperus esculentus tuberous rhizome extract and the combination of Cyperus esculentus tuberous rhizome extract and mango leaf extract also have a strong impact on alpha-2 waves, similar to rimonabant, methylphenidate and selegiline, a drug that increases Dopamine blood levels and greatly improves symptoms of depression.
Administration of a mixture of 30% ethanol extract of tuberous rhizome of Cyperus esculentus and mango leaf extract containing 60% of mangiferin decreased brain wave activity of delta, teta, alpha-1, alpha waves -2, beta-1, and beta-2 in the frontal cortex, the hippocampus and the striatum. The effect on brain wave activity of the mixture of Cyperus esculentus extract / mango leaf extract was approximately similar to the effect on brain wave activity of 5.0 mg / kg of rimonabant, 1.0 mg / kg of methylphenidate and 1.5 mg / kg of selegiline, as shown in figure 1.
Example 2
Test subjects:
Fisher 344 rats (11 months old and with day-night conversion, weight of approximately 350-400 g, provided by Charles River Laboratories, D-97633, Sulzfeld) were used in additional experiments on the effects of ethanol extract of tuberous rhizome of Cyperus esculentus, and mangiferin on the activity of the central nervous system. Products were provided to test subjects orally (nasogastric tube).
Test substances:
The substances tested in this study included:
a control vehicle (0.9% NaCl);
30% ethanol extract of tuberous rhizome skin of Cyperus esculentus, administered in an amount of 200 mg / kg to 7 rats;
Mango leaf extract containing 60% mangiferin, administered in an amount of 50 mg / kg to 6 rats; Y
a mixture of 30% ethanol extract of tuberous rhizome skin of Cyperus esculentus, in an amount of 150 mg / kg, and mango leaf extract containing 60% of mangiferin, in an amount of 50 mg / kg, administering the combination to 6 rats.
The EEG signals were recorded by means of telemetry of 4 electrodes implanted in the frontal cortex, the hippocampus and the striatum of rats that moved freely within a room totally protected with copper. EEG signals were recorded along:
a first period, which began 5 minutes after the administration of the test substances, and ended 65 minutes after the administration of the test substances; Y
a second period, which began 245 minutes (4.1 hours) after the administration of the test substances, and ended 305 minutes (5.1 hours) after the administration of the test substances.
Neural activity in the frontal cortex and hippocampus:
The administration of a saline tube control had little impact on neuronal activity in the frontal cortex and the hippocampus, as shown in Figure 2A. However, administration of 30% ethanol extract of tuberous rhizome of Cyperus esculentus significantly decreased the activity of brain waves in the frontal cortex. Approximately one hour after administration of Cyperus esculentus extract, the activity of brain waves in the frontal cortex of delta, teta, alpha and beta waves decreased to, on average, approximately 60% of the initial level before the drug, such as shown in figure 2B. Simultaneously, the delta and alpha-2 waves decreased significantly in the hippocampus (p <0.1). After approximately 5 hours, the effect on the delta and alpha-2 waves in the hippocampus was no longer visible, although suppressed activity was still present in the frontal cortex.
The administration of mango leaf extract containing 60% of mangiferin also decreased the activity of brain waves in the frontal cortex. Approximately one hour after the administration of the mango leaf extract, the activity of the brain waves in both the frontal cortex and the hippocampus of the delta, theta, alpha-2 and beta-1 waves decreased markedly, as shown in the figure 2C. The decrease in delta and teta wave activity was statistically significant (p <0.05). After approximately 5 hours, there was no significant change in the activity of brain waves in the hippocampus or delta and teta waves in the frontal cortex, relative to the initial level before the drug, although suppressed activity was present in the waves alpha and beta in the frontal cortex.
The administration of a mixture of 30% ethanol extract of tuberous rhizome skin of Cyperus esculentus and mango leaf extract containing 60% of mangiferin decreased brain wave activity in the frontal cortex to approximately the same degree as 30% ethanol extract of tuberous rhizome of Cyperus esculentus alone. Approximately one hour after administration of the combined extracts, the activity of brain waves in the frontal cortex and the hippocampus of the delta, theta, alpha-1, alpha-2 and beta-1 waves decreased significantly (p <0.01 ), as shown in Figure 2D. The effect on alpha-2 waves was greater than the effect on alpha-1 waves, as seen in Figure 2D; This leads to a reduction in the ratio of alpha-1 / alpha-2. Based on the change in the activity of theta waves and the ratio of alpha-1 / alpha-2, the combination of Cyperus esculentus extract / mango leaf extract has the potential to help smokers who wish to quit smoking.
Simultaneously, the activity of brain waves in the hippocampus of the theta, alpha-1 and alpha-2 waves decreased significantly (p <0.05 for alpha-1 and alpha-2 waves; p <0.1 for waves tit).
After approximately 5 hours, there was no significant change in brain wave activity of the theta, alpha-1, alpha-2, beta-1 and beta-2 waves in the frontal cortex, relative to the initial level before drug, although suppression of brain wave activity was present in the hippocampus. In the hippocampus, suppression of the activity of theta, alpha-1, alpha-2, beta-1 and beta-2 waves was observed (p <0.05 for alpha1 waves; p <0.1 for theta waves , alpha-2, beta-1 and beta-2). Additionally, in relation to the control with saline solution, the extract of Cyperus esculentus alone and the extract of mango leaf alone, the combination of the extract of Cyperus esculentus and extract of mango leaf produced a statistically significant increase (p <0.05 ) in the activity of gamma waves in the frontal cortex. Increased gamma band EEG activity is associated with alert or attention states.
Synergy was observed in the activity of brain waves in the hippocampus after administration of a mixture of extract in 30% ethanol of tuberous rhizome skin of Cyperus esculentus, and mango leaf extract containing 60% of mangiferin. First, neither Cyperus esculentus extract nor mango leaf extract have a statistically significant impact on the activity of alpha-1 brain waves in the hippocampus, either in the first hour after administration or 5 hours after administration, as shown in Figures 2B and 2C. However, the combination of Cyperus esculentus extract and mango leaf extract has a statistically significant impact on the activity of alpha-1 brain waves in the hippocampus, both in the first hour after administration and 5 hours after administration ( p <0.05, both 1 hour after administration and 5 hours after administration). In addition, neither the Cyperus esculentus extract nor the mango leaf extract have any statistically significant impact on the activity of brain waves in the hippocampus 5 hours after administration, as shown in Figures 2B and 2C. The combination of Cyperus esculentus extract and mango leaf extract has a statistically significant synergistic impact on the activity of alpha brain waves in the hippocampus 5 hours after administration, in relation to an increase in serotonergic activity.
In summary, the effect of the combination of tiger nut extract or mango leaf extract can be explained through the significant, synergistic and long-lasting decrease in the activity of alpha-1 brain waves in rats, which It represents an activation of the serotonergic and dopaminergic neurotransmission, measured in the hippocampus during the first hour and during the fifth hour after ingestion. Neither tiger nut extract nor mango leaf extract (60% mangiferin) or pure mangiferin administered alone showed a significant decrease in the activity of alpha-1 brain waves in these periods of time (see Figure 2 ). As previously mentioned, a decrease in the activity of alpha-1 brain waves of electrodes implanted in the rat is the result of increased serotonergic and dopaminergic neurotransmission. Such a change in neurotransmission, measured by external EEG electrodes in a person, would be seen as an increase in the activity of alpha-1 brain waves. In both rats and humans, increased serotonergic and dopaminergic neurotransmission correlates with increased relaxation and reduced stress.
Example 4: Studies with humans Four-week study
Four adults participated in a 4-week observational study, which took:
- 3 grams of an extract in 30% ethanol of tuberous rhizome of Cyperus esculentus, one to two times a day for a week,
- 400 mg of a mango leaf extract containing 284 mg of mangiferin, taken once a day for a week, and
- a combination of 3 grams of the tuberous rhizome extract of Cyperus esculentus and 400 mg of mango leaf extract (300 mg of mangiferin), taken one to two times a day for two weeks.
Subjects took daily notes on themselves about side effects, well-being, mood, concentration, alertness, stress. No side effects were experienced. All subjects noted clearly improved mood and well-being and a reduction in food cravings and enhanced satiety that lasted from 2 to 4 hours after ingestion of the Cyperus esculentus tuberous rhizome extract, mango leaf extract and combination of mango leaf extract and tiger nut extract. Two individuals skipped lunch time several days since the usual feeling of hunger did not appear at a precise time. Cyperus esculentus is less strong than mango leaf extract, so a larger dose was needed for the same effect.
In two adult subjects, the extract of mango leaf and Cyperus esculentus was formulated in gelatin gums and chewing gum to check the jugular absorption. In both subjects, for both formulations, there was a marked effect on the reduction of craving and the reduction of appetite.
Two week study
In a 2-week observational study where 9 adults ingested a combination of 3 grams of the tuberous rhizome extract of Cyperus esculentus and 400 mg of mango leaf extract daily for a period of two weeks, seven participants (78%) felt less hungry at lunchtime and they were able to delay lunch without problems for 30 minutes to an hour.
Addictive potential
In a study in which 6 adults ingested a combination of 3 grams of the tuberous rhizome extract of Cyperus esculentus and 400 mg of mango leaf extract daily over a period of two weeks, no signs of dependence or tolerance were observed , and there was no evidence of physical or psychological withdrawal. In a similar study in which 2 adults ingested a combination of 3 grams of the tuberous rhizome extract of Cyperus esculentus and 400 mg of mango leaf extract daily over a period of two months, no signs of tolerance were observed, dependence or abstinence In addition, daily intake over 2 months showed no negative side effects, but improved mood and wellbeing were indicated.
Two human subjects ingested higher doses of Cyperus esculentus tuberous rhizome extract / mango leaf extract in high doses (up to 20 g / day); The increase in dosage did not increase the observed effect on mood and craving.
Profile of moods
In a double-blind, randomized, placebo-controlled study of 2 branches with a parallel design with 32 adult subjects, the mood profile questionnaire (POMS) was completed one hour after a single oral dose of a composition of the invention that they contained tiger nut extract (1000 mg) and mangiferin (300 mg) of a mango leaf extract, and for placebo.
The mood profile is a psychological classification scale used to evaluate different transient moods. The evaluation provides a quick method to evaluate active, fluctuating, transient moods. It is an instrument to measure and monitor the change of treatment in clinical, medical and addiction treatment centers. It is also very suitable for clinical trials with drugs because its sensitivity to change allows accurate documentation of the effects of drugs on mood. POMS is a conventional validated psychological test that contains 65 words or statements that describe people's feelings. The test requires an indication, for each word or statement, of how the
subject in the previous week. Possible scores for each word or statement include: Score 1: Dejection; 5 Score 2: Feeling taciturn; Score 3: Fatigue; and 10 Score 4: Thirst for action. The results of the four scores are represented in the following table:
Mood Profile (POMS)
Score 1 Dejection Score 2 Feeling taciturnScore 3 FatigueScore 4 Thirst for action
Placebo n = 16 Half:0.240.380.732.84
Tiger Nutsmangiferina N = 16 Half:0.080.130.593.18
The results showed that only one hour after the ingestion of the nut combination
15 tiger-mangiferin, the 3 POMS scores for negative moods (dejection, feeling taciturn, fatigue) decreased compared to placebo, while the POMS score for positive mood, thirst for action, increased by score for composition compared to placebo.
Although the various embodiments have been described in detail by way of example with particular reference to certain aspects by way of example thereof, it should be understood that the invention may present other embodiments and its details may have modifications in various obvious aspects. As is readily apparent to those skilled in the art, variations and modifications may be made while
25 remain within the spirit and scope of the invention. Accordingly, the disclosure, the description and the preceding figures are for illustrative purposes only and do not limit in any way the invention, which is defined only by the claims.

权利要求:
Claims (24)
[1]
1. Composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b);
for use in reducing cravings for at least one of high-calorie foods, sugary and sweet drinks, products containing nicotine, and alcohol in a person who needs it.
[2]
2. Composition for use according to claim 1, wherein said person is trying to quit smoking; and said composition reduces the cravings for products containing nicotine in said person.
[3]
3. Composition for use according to claim 1 or claim 2, wherein said composition is administered in an amount effective to reduce the activity of theta brain waves and the ratio of alpha-1 / alpha-2 in said person.
[4]
Four. Composition for use according to claim 1, wherein said person is trying to reduce caloric intake; and said composition reduces food cravings in said person; wherein said composition is administered in an amount effective to reduce the activity of beta brain waves in said person.
[5]
5. Composition for use according to claim 3, wherein said composition further reduces food cravings in said person; wherein said composition is administered in an amount effective to reduce the activity of theta brain waves, the activity of the beta brain waves and the ratio of alpha1 / alpha-2 in said person.
[6]
6. Composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of Cyperus esculentus, or a combination thereof;
b) an effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b);
for use in reducing stress and improving mood in a person, in which said composition modulates the activity of alpha brain waves in said person.
[7]
7. Composition for use according to any one of claims 1 to 5, or composition for use according to claim 6, wherein said composition comprises said Cyperus esculentus skin extract, Cyperus esculentus rhizomes, or a combination thereof.
[8]
8. Composition for use according to any one of claims 1 to 5 or 7, or composition for use according to claim 6, wherein said Cyperus esculentus skin extract, Cyperus esculentus rhizomes, or a combination thereof is a aqueous extract, an alcoholic extract or a hydroalcoholic extract, or a subcritical or supercritical CO2 extract.
[9]
9. Composition for use according to any one of claims 1 to 5 or 7 or 8,
or composition for use according to claim 6, wherein said extract composition comprises a hydroalcoholic skin extract of rhizomes of Cyperus esculentus.
[10]
10. Composition for use according to any one of claims 1 to 5 or 7 to 9,
or composition for use according to claim 6, wherein said effective amount of said Cyperus esculentus skin, rhizomes of Cyperus esculentus, or a combination thereof is between 20 mg and 20 g per dose.
[11]
eleven. Composition for use according to any one of claims 1 to 5, or
composition for use according to claim 6, wherein said composition comprises said effective amount of mangiferin, noratiriol, or an extract comprising mangiferin or noratiriol.
[12]
12. Composition for use according to claim 11, wherein said effective amount of said mangiferin or said noratiriol is between 20 mg and 5 g per dose.
[13]
13. Composition for use according to claim 11, wherein said effective amount of said extract comprising mangiferin or noratiriol is sufficient to provide between 20 mg and 5 g of mangiferin or noratiriol per dose.
[14]
14. Composition for use according to any one of claims 11 to 13, wherein said extract comprising mangiferin or noratiriol is an extract containing mangiferin of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum , Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and mixtures thereof.
[15]
fifteen. Composition for use according to any one of claims 1 to 5, or composition for use according to claim 6, wherein said composition comprises said synergistic combination of (a) and (b).
[16]
16. Composition for use according to claim 15, wherein (a) it is an aqueous extract, an alcoholic extract or a hydroalcoholic extract of Cyperus esculentus skin, rhizomes of Cyperus esculentus, or a combination thereof.
[17]
17. Composition for use according to any one of claims 15 or 16, wherein (a) comprises a hydroalcoholic extract of skin of rhizomes of Cyperus esculentus.
[18]
18. Composition for use according to any one of claims 15 to 17, wherein (b) comprises mangiferin or an extract containing mangiferin of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora , Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and mixtures thereof.
[19]
19. Composition for use according to any one of claims 15 to 18, wherein the ratio of (a) to (b) is between about 1: 1 and about 50: 1.
[20]
twenty. Composition for use according to any one of claims 15 to 18, wherein the ratio of (a) to (b) is between about 1: 1 and about 20: 1.
[21]
twenty-one. Composition for use according to any one of claims 15 to 18, wherein the ratio of (a) to (b) is between about 4: 1 and about 15: 1.
[22]
22 Composition for use according to any one of claims 15 to 18, wherein said effective amount of (a) is between 20 mg and 20 g per dose; and said effective amount of said mangiferin or said extract containing mangiferin is between 5 mg and 5 g per dose.
[23]
2. 3. Composition for use according to any one of claims 15 to 18, wherein said composition is provided as a unit dose containing between 10 mg and 20 g per dose.
[24]
24. Composition for use according to any one of claims 1 to 5 or 7 to 23, or composition for use according to claim 6, wherein said composition further comprises an active ingredient selected from the group consisting of 5-hydroxytryptophan, vitamins of group B , caffeine, citicoline, citrulline, choline, chromium picolinate, coenzyme Q10, curcumin, glycomacropeptide, huperzine, hydroxycitrate, Lcarnithine, L-carnosine, L-tryptophan, luteolin, ibogaine, magnesium, N-methyl tyramine, omega 3 acids , octopamine, phenylalanine, phenylethylamine, phosphatidylserine, quercetin, raspberry ketones, rutin, resveratrol, synephrine, taurine, taxifoline, theanine, theobromine, xanthohumol, yangonine, yohimbine, ecdysteroids (20HE), extracts of Aphanizaeon, ethans Ascophyllum nodosum, Chlorella and other microalgae, extracts of plant species of the genera Aframomum, Aloysia, Alpinia, Astragalus, Bacopa, Capsicum, Carra luma, Chicorium, Cinnamomum, Ciser, Cissus, Crocus, Centella, Citrus, Coca, Cola, Curcuma, Coffea, Celastrus, Camellia, Eleutherococcus, Ephedra, Euterpe, Garcinia, Ginkgo, Ganoderma, Glycyrrhiza, Griffonia, Gymnema,
Hoodia, Hordeum, Icarine, Ilex, Ipomoea, Irvingia, Kaempferia, Ocimum, Olea,
Oreganum, Paullinia, Panax, Persea, Phaseolus, Pinus, Prunus, Pfaffia, Piper
Pueraria, Punica, Rhodiola, Rhaponticum, Shisandra, AIDS, Sideritis, Simondia,
Solanum, Tabernanthe,Tamarindus,Theobroma,Tragaopogon,Trichocaulon,
5 Trigonella, Vicia, Vigna, Vitis, Withania, Zingiber, Zizyphus, polysaccharides other than
starch, includinggalactamannan,rubberguar,rubbergarrofín,rubbertare,
ispaghula, -glucans, konjac glucomaman, methylcellulose, gum tragacanth,
detario, and mixtures thereof.
10 25.Composition comprising:
a) an effective amount of a skin extract of Cyperus esculentus, rhizomes of
Cyperus esculentus, or a combination thereof;
fifteen b)aeffective amount of mangiferin, noratiriol,or aextract that comprises
mangiferin or noratiriol; or
c) a synergistic combination of (a) and (b);
twenty for use in reducing appetite and enhancing satiety in a
person.

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优先权:

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申请号 | 申请日 | 专利标题

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US15/402,886|US10874708B2|2017-01-10|2017-01-10|Compositions for reducing appetite and craving, increasing satiety, enhancing mood, and reducing stress|

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US15/402,886|2017-01-10|

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