• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    A cancer drug is formed by synthesizing a cancer cell toxicant, such as furfural, and a metabolizable substance, such as gluconic acid, by the cancer cell fermentation metabolism.
    公开号:AT514533A2
    申请号:T50431/2014
    申请日:2014-06-20
    公开日:2015-01-15
    发明作者:Christoph Dr Pallua
    申请人:Christoph Dr Pallua；
    IPC主号:
    专利说明:

    cancer drug
    The cancer cell, in contrast to the healthy cell, which has a metabolic metabolism with oxygen, a fermentation metabolism on.
    The fermentation metabolism consumes a multiple of energy compared to the metabolic metabolism, which explains, inter alia, the rapid emaciation of cancer patients.
    The fermentation metabolism generates hydrogen ions, which would lead to acidification and thus destruction of the cancer cell. However, the cancer cell protects itself against this hyperacidity by reductive amination, by which the hydrogen ions are bound to nitrogen.
    It has already been proposed to block the reductive amination of the cancer cell by administration of furfural to cause hyperacidity and thus cell death of the cancer cell (see Dr. Dr. Rudolf Dobril, "Vaccination Against Cancer", Verlag Wilhelm Maudrich, Vienna-Munich-Berne , 2nd ed., 1985, especially pages 39 to 61).
    However, as has been noted, furfural blood levels persist only for a short time, so the efficacy of furfural as a cancer drug leaves much to be desired, especially in large metastatic tumors.
    The object of the invention is therefore to provide a high-potency anticancer drug by prolonged blocking of reductive termination.
    This is achieved according to the invention by the anticancer drug indicated in claim 1, which is formed by synthesis of a cancer cell toxic substance and a metabolizable substance by the cancer cell fermentation metabolism. That is, the cancer medicine of the present invention has a compound which has a cancer cell toxic compound component and a cancer cell fermentation metabolizable compound component, the toxic compound component being synthesized by the cancer cell toxic substance synthesis and the metabolizable compound component from the cancer cell fermentation metabolizable substance is formed.
    The cancer cell toxicant is preferably a substance blocking the reductive amination of the cancer cell.
    The substance blocking the reductive amination of the cancer cell is preferably a heterocyclic aldehyde, especially furfural or a furfural derivative.
    The substance metabolizable by the fermentation metabolism of the cancer cell is preferably formed by gluconic acid, glucose or another glucose derivative.
    Galvanotherapy has been shown to reduce zinc levels to an absolute minimum after a short time, despite the administration of high-dose zinc gluconates. Thus, it is not known that the cancer cell ferrites gluconate at high speed than metabolizes it. The same applies to glucose and other glucose derivatives.
    On the other hand, when furfural is administered, the rapid drop in the blood level of the furfural low-furfural furfural can be explained.
    The coupling of furfural or other substance of the invention for the cancer cell into gluconic acid, gluconic acid derivatives, glucose or another glucose derivative or another metabolizing substance in the cancer cell by the fermentation metabolism in a compound now causes the drug to be induced by the cancer cell High levels of metabolizable substance are taken up by the cancerous cell, releasing the toxicant, furfural, for example, in high concentrations in the cancer cell, thereby blocking the reductive amination in the cancer cell and thus destroying the cancerous cell by hyperacidity.
    Furthermore, the coupling of gluconic acid or another substance metabolizable metabolically in the cancer cell with the toxicant, such as furfural, achieves a significantly higher molecular weight and thus prevents the toxic substance, eg furfural, from rapidly being eliminated by the kidney because of its low molecular weight without being accepted by the cancer cell as the actual desired site of action.
    That is, by coupling the furfural to the metabolite metabolizable by fermentation metabolism, due to the high molecular weight, a sustainable plasma level can be achieved on the medicament of the invention and thus indirectly on furfural.
    The cancer drug according to the invention thus causes a long-lasting high blood level because of its higher molecular weight compared to the unbound toxic substance.
    In addition, the toxic substance in the cancer cell is released by the rapidly metabolized in the cancer cell compound component with far higher efficacy. The anti-cancer drug according to the invention can therefore also be administered in low doses, since the toxic compound is released only in the cancer cell.
    Thus, by coupling the cancer cell toxicant, such as furfural, to the metabolizable metabolite in the cancerous cell, such as gluconic acid, the cancer medicament of the invention can easily be absorbed by the patient's body and rapidly enter the fermentation metabolism of the cancer cell.
    It should be mentioned that the patient should preferably take the medicament according to the invention fasting or hungry, since at a low level of glucose, such as sobriety, the cancer cell absorbs particularly intensively substances such as gluconic acid in order to metabolize them by fermentation metabolism.
    The medicament according to the invention can be administered orally, but also, for example, intravenously.
    As the furfural derivative, for example, 5-hydroxymethylfurfural can be used for synthesizing the medicament of the present invention to obtain, by esterifying the 5-hydroxymethyl group with gluconic acid or a gluconic acid derivative, a cancer medicine of the present invention formed from 5-hydroxymethyl furfural and gluconic acid or gluconic acid derivative receive.
    For this purpose, common methods for ester formation can be used, e.g. the reaction of the silver salt of gluconic acid with iodomethylfurfural with elimination of silver iodide.
    Although carcinogenicity of furfural has been claimed. However, no evidence has been provided so far. Rather, the above-mentioned reference by Dr. med. Dr. Dobril, especially pages 44 to 49, for deriving the non-toxicity of furfural also in relation to cancers.
    权利要求:
    Claims (5)
    [1]
    Claims 1. A cancer drug comprising a compound formed by the synthesis of a cancer cell toxicant and a metabolizable metabolite by the fermentation metabolism of the cancerous cell.
    [2]
    The anticancer drug according to claim 1, characterized in that the cancer cell toxic substance is a substance blocking the reductive amination of the cancer cell.
    [3]
    Cancer medicament according to claim 1 or 2, characterized in that the toxic substance is a heterocyclic aldehyde.
    [4]
    A medicament according to claim 3, characterized in that the heterocyclic aldehyde is furfural or a furfural derivative.
    [5]
    Medicament according to one of the preceding claims, characterized in that the substance metabolizable by the fermentation metabolism of the cancerous cell is formed by gluconic acid, a gluconic acid derivative or glucose.
    类似技术:
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    同族专利:
    公开号 | 公开日
    AT514533B1|2017-04-15|
    DE102013106530A1|2014-12-24|
    CH708261A2|2014-12-31|
    AT514533A3|2016-06-15|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    EP1834951A1|2006-03-10|2007-09-19|Avantium International B.V.|Method for the synthesis of organic acid esters of 5-hydroxymethylfurfural and their use|
    EP1958944A1|2007-02-16|2008-08-20|Evonik Degussa GmbH|Method for producing enantiomer 5-hydroxymethylfurfural with 5-acyloxymethylfurfural as intermediate|
    WO2009030512A2|2007-09-07|2009-03-12|Furanix Technologies B.V.|Hydroxymethylfurfural ethers and esters prepared in ionic liquids|
    US20090156841A1|2007-12-12|2009-06-18|Sanborn Alexandra J|Conversion of carbohydrates to hydroxymethylfurfural and derivatives|
    AT393221B|1988-02-03|1991-09-10|Leopold Pharma Gmbh|AGENT WITH DESTROYING EFFECT ON MALIGNE TUMORS, METHOD FOR THE PRODUCTION THEREOF AND PREPARATION FOR USE IN THE THERAPY OF CANCER DISEASES|
    AT412447B|2002-11-27|2005-03-25|C Y L Handelsges M B H|MEANS DAMAGING EFFECT ON MALIGNANT TUMORS AND PROCESS FOR THEIR MANUFACTURE|
    US20050124684A1|2003-08-29|2005-06-09|Ying Du|5- furfural and derivatives as inhibitors of TNFalpha and IL-1beta production|
    JP4693093B2|2005-01-27|2011-06-01|国立大学法人鹿児島大学|Anticancer drug|
    KR101377037B1|2010-11-11|2014-03-21|주식회사 노암|Anticancer compositions|DE102016113143A1|2016-07-15|2018-01-18|Christoph Pallua|cancer drug|
    法律状态:
    2021-02-15| MM01| Lapse because of not paying annual fees|Effective date: 20200620 |
    优先权:
    申请号 | 申请日 | 专利标题
    DE201310106530|DE102013106530A1|2013-06-21|2013-06-21|cancer drug|
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