前苏联专利SU786855A3 Method of preparing polysaccharides possessing antitumor activity

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专利摘要:
1521168 Extracting therapeutically active polysaccharides ex basidiomycetes fungus KUREHA KAGAKU KOGYO KK 15 Dec 1976 [18 Dec 1975] 52440/76 Heading C3U Therapeutically active nitrogen-containing polysaccharides are extracted from Basidiomycetes fungus of the coriolus genus using an aqueous solvent under superatmospheric pressure, preferably 1À8-20 kg/cm<2> at 120-200‹ C. The preferred fungi are Coriolus biformis Coriolus conchifer, Coriolus consors, Coriolus hirsutus, Coriolus pargamenus, Coriolus pubescens and Coriolus versicolor. The solvent may be an alkaline solution, less than IN used in an amount of 10-50 times the weight of fungus used and the aqueous extract may then be treated, e.g. by dialysis, to remove material of MW less than 5,000.
公开号:SU786855A3
申请号:SU762428806
申请日:1976-12-16
公开日:1980-12-07
发明作者:Асано Киро；Сайто Цуеси；Танака Хиромицу；Эномото Сатору
申请人:Куреха Кагаку Когио Кабусики Кайся (Фирма)；
IPC主号:

专利说明:

neither a bad one, but a extraction period exceeding 360 minutes can cause decomposition of the active constituent.
The extraction operation can be repeated under the conditions mentioned above, or the basic material of basidiomycers can be immersed in an aqueous solvent at a heating temperature lower before the extraction operation, or the resulting extract can be washed with an aqueous solvent of nprf temperature lower after extraction, the solvent used is pure water, an aqueous acidic or alkaline solution, an aqueous solution of 15 ochevin and an aqueous solution of amino acids. The most preferred aqueous solvent is water or diluted with less than 1 and alkaline solution.
The extract thus obtained is then purified by ultrafiltration, salting out, dialysis, reverse osmosis or other methods that can be used individually or in combination to remove substances with a low molecular weight (substances with a molecular weight less than 5000). extract.
Such purification allows to obtain a nitrogen-containing polysaccharide with a high antitumor activity, a high inhibitory effect against the solid (Solid) cancer Sarcoma-180, not only with intraperitoneal administration, but also with the oral administration of mice.
The resulting polysaccharides are not only effective in preventing side effects during chemical therapy of patients affected by the tumor and detecting increased sensitivity to radiotherapy, but also increase their resistance against infection by viruses or bacteria, when the patient’s immunity or physical condition is weak, the dental administration of polysaccharides improves Hepatic capacity, improves appetite, cures gastric disorders, improves urination, and is effective in treating leprosy. The method is illustrated by the following examples.
Example 1. The artificially diluted Mycelium of Coriolus versicolor (Fr.) QueJ is dried to a water content of 10% and divided into five parts. Each portion is then mixed with a 12.5-fold amount (by weight) of water and loaded into an autoclave, in which the extraction is performed under the extraction conditions shown in Table 2. 1. The extract obtained from each part is then filtered to separate the extract solution, and the resulting extract solution is dialyzed with a 72-hour stream of water using dialysis
tube in accordance with the usual method. This analytical treatment removes from the extract substances with a low molecular weight (substances with a molecular weight less than 5000). The dialyzed solution is then concentrated to obtain a red-brown powder with a water content of about 7%. This powdered material has an average molecular weight of more than 10,000. The results of an elementary analysis and various color reaction tests are given in table. 2, proves that this substance is a nitrogen-containing polysaccharide.
From the results of the above tests, it can be seen that the obtained α-products are polysaccharides containing primary peptide-bound nitrogen.
In order to determine the antitumor effect of nitrogen containing -. The following polysaccharides prepared in accordance with the present invention are tested.
Sarcoma-180 tumor cells are transplanted into the abdominal cavities of mice and seven days later (after sufficient cell proliferation) 10 cell fragments are then transplanted to another group of mice in the subcutaneous region of the armpit to develop solid tumors. Intraperitoneal administration of polysaccharides begins 24 hours after transplantation. The substance is administered once a day every other day in the amount of 10 mg / kg per administration in a total amount of 0.2 ml / 20 g (live weight of the mouse). On the 25th day after transplantation, the tumor of each mouse is removed and its weight is determined. The inhibitory effect of polysaccharides on tumor growth is calculated from the average weight of tumors in the group of mice administered with polysaccharides, and the average weight of tumors in the control group.
The measurement results are presented in Table. 3. Details of the preparation of the relevant samples used in this experiment, i.e. the amount of aqueous solvent used (water), the temperature and time of extraction, the degree of extraction, selectivity and yield are also shown in Table. 3
From the results given in table. 3 shows that in experiments conducted on mice that were subcutaneously transplanted with Sarcoma-180 tumor cells, each of the nitrogen-containing polysaccharides obtained in accordance with this invention shows equal or higher antitumor activity compared with similar preparations obtained under normal conditions. x extraction. Output with respect
the amount of fungus used is noticeably improved.
Example 2. The mycelium of the same basidiomycete used in example 1 is divided into eight parts and each part is loaded into an autoclave together with a 12.5-fold (relative to the weight of the mycelium) amount of alkaline or essentially neutral aqueous solution. described in table. 3. Next, the extraction is carried out under the conditions of pressure and temperature shown in Table. 3. After extraction, the material in the autoclave is neutralized and filtered in order to fraction the extract solution by separating it from the insoluble residue from the extraction. This extract solution was subjected to dialysis treatment in accordance with the procedure described in Example 1, obtaining substances with a combined molecular weight of more than 10,000. When these substances are tested for various color reactions, presented in Table. 2, it is confirmed that they are nitrogen-containing polysaccharides. In order to determine the antitumor activity of the nitrogen-containing polysaccharides thus obtained, samples 1 through 8 of these substances are administered to mice, which are subcutaneously transplanted with Sarcoma-180. results
show (see Table 4) that these substances produce an equal or higher antitumor effect as compared to nitrogen-containing polysaccharides obtained in accordance with the usual method of extraction with hot water under normal pressure.
The proposed method allows to obtain polysaccharides with high antitumor activity.
Table
1 2 3 4 5 П
0.71 0.72 0.72 0.73 0.73 Comparative specimen is a specimen prepared using the same basidiomycete as for samples 1 to 5 in accordance with the invention, but by extraction at normal carbon pressure according to the usual method. The degree of extraction is the degree of the dissolved fungus used as starting material, which is expressed in% by weight. Selectivity is the percentage yield of nitrogen-containing polysaccharides with a molecular weight above 10,000, obtained from the extract. Yield relative to the fungus is the percentage yield of nitrogen-containing polysaccharides with a molecular weight above 10,000 relative to the total load of the fungus. Note.
Table 2 The comparison sample is a sample prepared using the same baeid-dissolve as for samples 1 to 8, in accordance with the usual method of extraction with hot water under normal pressure.
Table4
Comparative data on antitumor activity (%)

权利要求:
Claims (3)
[1]
1. The method of obtaining polysaccharides with antitumor activity, by extraction from fungi with
subsequent purification of the target product from ballast impurities, characterized in that, in order to increase the antitumor activity of polysaccharides, the fungi are subjected to the extraction of fungi Coriolus biformis, Cofiolus conchifer, Coriolus consors, Coriolus hirsutus, Coriolus pargamenus, Coriolus pubecens or Coriolus Iriusiriusirusirusirus, coriolus hirsutus alkalis
0 by autoclaving under pressure for 5-360 min at 150-200 C,
POP.1 method, I distinguish
[2]
2
U and i, -. . with the fact that the extraction
lead under pressure of 5-20 kg / cm.
five
[3]
3. Method POP.1; characterized in that the extraction is carried out with a dilute alkali solution at a concentration below 1 n.
Information sources,
0 taken into account in the examination
1. Japanese Patent 50-32304, Cl, 30 A 32, published. 20.10.75,

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同族专利:

公开号 | 公开日

AU496814B2|1978-11-02|

CH622948A5|1981-05-15|

RO69485A2|1980-01-25|

NL171224B|1982-10-01|

AU2035476A|1978-06-15|

DK147766C|1985-05-20|

IN142077B|1977-05-28|

AT347031B|1978-12-11|

HU176827B|1981-05-28|

SE435678B|1984-10-15|

US4202885A|1980-05-13|

BE849476A|1977-06-16|

DE2655844A1|1977-07-07|

MX4646E|1982-07-15|

IT1123693B|1986-04-30|

YU303776A|1984-02-29|

PL101771B1|1979-01-31|

DK147766B|1984-12-03|

CS200503B2|1980-09-15|

DE2655844C3|1980-01-31|

GB1521168A|1978-08-16|

FR2335235B1|1980-08-29|

DD129330A5|1978-01-11|

DE2655844B2|1979-06-07|

NL171224C|1983-03-01|

NL7614016A|1977-06-21|

DK570176A|1977-06-19|

PH12234A|1978-11-29|

YU40467B|1986-02-28|

CA1055487A|1979-05-29|

ES454304A1|1978-08-16|

JPS5628152B2|1981-06-30|

SE7614202L|1977-06-19|

ATA934876A|1978-04-15|

FR2335235A1|1977-07-15|

JPS5290614A|1977-07-30|

BR7608526A|1977-12-20|

引用文献:

公开号 | 申请日 | 公开日 | 申请人 | 专利标题

RU2475529C2|2011-03-14|2013-02-20|Федеральное бюджетное учреждение науки "Государственный научный центр вирусологии и биотехнологии "Вектор" |INHIBITOR OF INFLUENZA A VIRUS REPRODUCTION BASE ON EXTRACT OF BASIDIAL FUNGUS Phallus impudicus|BE757248A|1969-10-15|1971-04-08|Kureha Chemical Ind Co Ltd|SUBSTANCE WITH ANTI-CANCER PROPERTY AND METHODS FOR ITS PREPARATION|JPS5614274B2|1976-07-07|1981-04-03|

JPS5614275B2|1976-07-07|1981-04-03|

US4851395A|1976-07-07|1989-07-25|Kureha Kagaku Kogyo Kabushiki Kausha|Nitrogen-containing polysaccharide|

JPS5614276B2|1976-07-22|1981-04-03|

JPS5726645B2|1977-09-16|1982-06-05|

EP0022426B1|1979-07-04|1986-09-10|Kureha Chemical Industry Co., Ltd.|Nasal preparations, process for making same and their use|

JPS5646793B2|1979-08-08|1981-11-05|

US4512972A|1980-06-30|1985-04-23|Kureha Chemical Industry Co., Ltd.|Nasal preparation and processes for their production|

JPS5932480B2|1981-02-10|1984-08-09|Kureha Chemical Ind Co Ltd|

US4614733A|1981-12-31|1986-09-30|Kureha Kagaku Kogyo Kabushiki Kaisha|Polysaccharides pharmaceutical compositions and the use thereof|

DE3448155C2|1983-08-11|1989-11-02|Kureha Kagaku Kogyo K.K., Nihonbashi, Tokio/Tokyo, Jp|

JP2746532B2|1994-02-23|1998-05-06|宮和男|Immunity-enhanced foods based on Isaria-type insects|

US7048932B2|2002-05-22|2006-05-23|The Chinese University Of Hong Kong|Preparation and standardization of immunomodulatory peptide-linked glucans with verifiable oral absorbability from coriolus versicolor|

法律状态:

优先权:

申请号 | 申请日 | 专利标题

JP15011475A|JPS5628152B2|1975-12-18|1975-12-18|

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