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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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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 about half a year, and it cannot improve The 5-year survival rate after surgery, and the side effects of chemotherapy are large, so it is only used as placebo therapy for advanced cases
Therefore, people have never stopped searching for anti-cancer drugs with better curative effect.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] 18kg of Panax notoginseng (specification: countless heads, purchased from Yunnan) is crushed into powder (100-200 mesh), soaked in 30kg of 95% ethanol for two days, filtered, the filtrate is concentrated to obtain Panax notoginseng ethanol extract, and the ethanol is recovered and reused to soak the filter residue Six times, finally accumulatively obtained 3.37kg of Panax notoginseng ethanol extract, dissolved it in water, extracted three times with petroleum ether, took the water phase and extracted four times with n-butanol, concentrated the n-butanol layer, and obtained Panax notoginseng total saponins n-butyl Alcoholic extract 1.78kg.

[0089] Get total saponin extract 100g and dissolve in 1300ml n-butanol, heat, stir, add sodium ethylate (chemically pure, purity: 80%) 132.6g (1.56mol, concentration: 1.2mol / L), feed oxygen, 90 ℃ react After 65 hours, the reaction was over. The reaction solution was cooled to room temperature, washed with water saturated with n-buta...

Embodiment 2

[0091] Get 100g of Panax notoginseng total saponins extract (prepared in Example 1) and dissolve in 1500ml n-amyl alcohol, heat, stir, add sodium n-butoxide (chemically pure, purity: 80%) 150g (1.56mol, concentration: 1.04 mol / L), pass compressed air, react at 100°C for 60 hours, and the reaction ends. 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, the ethyl acetate layer was washed with water, and dried. After concentration, it was purified by silica gel column chromatography [cyclohexane:ethyl acetate=10:1-1:1 (V / V) gradient elution] to obtain 8 g of protopanaxadiol (A2), with a purity of 97% as determined by HPLC. %;

Embodiment 3

[0093] Notoginsenoside (content: calculated as ginsenoside Rb3, 91.9%; purchased from Yunnan) 1000g was dissolved in 14L n-butanol, heated, stirred, and sodium ethylate (chemically pure, purity: 80%) 1190g (14.0mol, Concentration: 1.0mol / L), pass oxygen, react at 110°C for 55 hours, and the reaction ends. 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 was washed with water, dried, and evaporated to dryness. After purification 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 physicochemical data are consistent with literature values: J. Asakawa et al, Tetrahedron, 1977, 33, 1935-1939; Nagai, M. et al, Chem. Pharm. Bull, 1972, 20(6), 1212-1216.

[0094] The physi...

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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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