Use of 20(S)-protopanoxadiol in preparation of anti-bowelcancer medicine

A protopanaxadiol and drug technology, applied in the field of medicine, can solve the problems of not improving the 5-year survival rate, high toxicity and side effects of chemotherapy, and short effective time limit, etc.

Inactive Publication Date: 2007-01-17
SHANGHAI INNOVATIVE RESEARCH CENTER OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
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  • Claims
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Problems solved by technology

[0005] Colon cancer is a tumor with poor sensitivity to chemotherapy. At present, 5-fluorouracil and cyclophosphamide are the most commonly used drugs, but their effective rate is less than 20%, and the effective time is short. In effective cases, the prolongation of life is only a

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  • Use of 20(S)-protopanoxadiol in preparation of anti-bowelcancer medicine

Examples

Experimental program
Comparison scheme
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Example Embodiment

[0087] Example 1

[0088] Panax notoginseng 18kg (specifications: countless heads, purchased from Yunnan), crushed into powder (100-200 mesh), soaked in 30kg 95% ethanol for two days, filtered, and the filtrate is concentrated to obtain the ethanol extract of Panax notoginseng. The ethanol is recycled and reused to soak the filter residue. After six times, a total of 3.37kg of the ethanol extract of notoginseng was obtained, which was dissolved in water, extracted with petroleum ether three times, and the water phase was extracted with n-butanol four times, and the n-butanol layer was concentrated to obtain a total of notoginseng saponins n-butyl. The alcohol extract is 1.78kg.

[0089] Dissolve 100g of total saponin extract in 1300ml of n-butanol, heat and stir, add 132.6g (1.56mol, concentration: 1.2mol / L) of sodium ethoxide (chemically pure, purity: 80%), ventilate, and react at 90°C After 65 hours, the reaction was over. The reaction solution was cooled to room temperature, wa...

Example Embodiment

[0090] Example 2

[0091] Dissolve 100g of Panax notoginseng saponins extract (prepared in Example 1) in 1500ml n-pentanol, heat and stir, add 150g (1.56mol, concentration: 1.04) of sodium n-butoxide (chemically pure, purity: 80%) mol / L), pass compressed air, and react at 100°C for 60 hours. The reaction is complete. The reaction solution was cooled to room temperature, washed with water saturated with n-butanol, the n-butanol layer was concentrated and dissolved in water, extracted with ethyl acetate, and the ethyl acetate layer was washed with water and dried. After concentration, it was purified by silica gel column chromatography [cyclohexane: ethyl acetate = 10:1 to 1:1 (V / V) gradient elution] to obtain 8 g of protopanaxadiol (A2), and the purity determined by HPLC was 97 %;

Example Embodiment

[0092] Example 3

[0093] Notoginseng leaf glycosides (content: ginsenoside Rb3, 91.9%; purchased from Yunnan) 1000g dissolved in 14L n-butanol, heated, stirred, and sodium ethoxide (chemically pure, purity: 80%) 1190g (14.0mol, Concentration: 1.0mol / L), oxygen, react at 110°C for 55 hours, and the reaction is over. The reaction solution was cooled to room temperature, washed with water saturated with n-butanol, the n-butanol layer was concentrated and dissolved in water, extracted with ethyl acetate, and the ethyl acetate extract phase was washed with water, dried, and evaporated to dryness. Purified by silica gel column chromatography [petroleum ether: ethyl acetate = 9:1-2:1 (V / V) gradient elution], 181.6 g of protopanaxadiol (A2) was obtained, and the purity determined by HPLC was 99.3%. Its physical and chemical data are consistent with the literature value: J. Asakawa et al, Tetrahedron, 1977, 33, 1935-1939; Nagai, M. et al, Chem. Pharm. Bull, 1972, 20(6), 1212-1216.

[0094...

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Abstract

An application of 20(S)-protopanoxadiol in preparing the medicines for preventing and treating intestinal cancer is disclosed.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of 20(S)-protopanaxadiol in the preparation of anti-intestinal cancer drugs. Background technique [0002] Protopanaxadiol is the aglycone of ginsenosides in the diol group, and is divided into 20(S)-protopanaxadiol and 20-(R) protopanaxadiol, which are enantiomers of each other, and their structures are as follows: [0003] [0004] 20-(S) Protopanaxadiol 20-(R) Protopanaxadiol [0005] Colon cancer is a tumor with poor sensitivity to chemotherapy. At present, 5-fluorouracil and cyclophosphamide are the most commonly used drugs, but their effective rate is less than 20%, and the effective time is short. In effective cases, the prolongation of life is only about half a year, and it cannot improve The 5-year survival rate after surgery is low, and the side effects of chemotherapy are high, so it is only used as a placebo therapy for advanced cases. Therefore, people ha...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61K9/08A61K9/10A61K9/16A61K9/20A61K9/48A61P35/00
Inventor 惠永正杨子荣杨志奇葛强
Owner SHANGHAI INNOVATIVE RESEARCH CENTER OF TRADITIONAL CHINESE MEDICINE
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