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A kind of preparation method and application of cycloastragenol

A technology for cycloastragaloside and astragaloside IV is applied in the field of preparation of cycloastragaloside, which can solve the problems of insufficient relative bioavailability, limited drug development and promotion, etc., and achieves remarkable effect of anticancer adjuvant therapy, simple operation, and technological conditions. mild effect

Active Publication Date: 2015-11-25
SOUTHWEST JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When it is used in conjunction with anti-tumor chemotherapy drugs, it can better improve the tolerance of the human body to chemotherapy drugs and improve the quality of life of cancer patients; Insufficient relative bioavailability in vivo limits its development and promotion as a drug

Method used

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  • A kind of preparation method and application of cycloastragenol
  • A kind of preparation method and application of cycloastragenol
  • A kind of preparation method and application of cycloastragenol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] A. Oxidation

[0052]Take 780 mg (about 1 mmol) of astragaloside IV as a raw material, add water to it to form a suspension with a content of astragaloside IV of 0.01mol / L, add hydrochloric acid to adjust the pH of the suspension to 3-4, and add to the suspension Add oxidant—sodium periodate and react in the dark at 20°C for 48 hours, then add ethylene glycol to terminate the oxidation, wherein the molar ratio of astragaloside IV to oxidant is 1:10; then add Na 2 CO 3 Adjust the pH to 7-8, concentrate under reduced pressure until there is no alcohol smell, add an equal volume of n-butanol to extract 3 times, combine the n-butanol extraction part, wash twice with water, take the n-butanol part, evaporate the n-butanol to obtain the oxidized product.

[0053] B. Restore

[0054] Add the oxidation product obtained in step A to 30% aqueous methanol to disperse into a suspension, and the mass ratio of the added 30% aqueous methanol to astragaloside IV in step A is 1:0.7; ...

Embodiment 2

[0063] A. Oxidation

[0064] Get 1.5g (about 2mmol) astragaloside IV as a raw material, add water to it to configure a suspension with a content of astragaloside IV of 0.001mol / L, add sulfuric acid to adjust the pH of the suspension to 4-5, and add to the suspension Add an oxidizing agent——periodic acid to react in the dark at 5°C for 96 hours, then add ethylene glycol to terminate the oxidation, wherein the molar ratio of astragaloside IV to the oxidizing agent is 1:2; then add NaOH to adjust the pH to 8-9, Filter the reaction solution to obtain a filter cake, and rinse the filter cake with water several times to obtain the oxidation product

[0065] B. Restore

[0066] Disperse the oxidation product obtained in step A with water to form a suspension, and the mass ratio of the added water to astragaloside IV in step A is 1:20; then add sodium borohydride as a reducing agent, and after the reduction reaction for 12 hours, add 50% acetic acid The reaction is terminated until ...

Embodiment 3

[0075] A. Oxidation

[0076] Take 800mg (1mmol) astragaloside IV as a raw material, add 20% methanol aqueous solution to it to form a suspension with a content of astragaloside IV of 0.05mol / L, add phosphoric acid to adjust the pH of the suspension to 5-6, and add to the suspension Add an oxidant to the solution—periodic acid reacts in the dark at 25°C for 48 hours, then adds ethylene glycol to terminate the oxidation, and the molar ratio of astragaloside IV to the oxidant is 1:15; then add KHCO 3 Adjust the pH to 7-8, concentrate under reduced pressure until there is no alcohol smell, add an equal volume of n-butanol to extract 3 times, combine the n-butanol extraction part, wash twice with water, take the n-butanol part, evaporate the n-butanol to obtain the oxidized product.

[0077] B. Restore

[0078] Add 50% methanol aqueous solution to the oxidation product obtained in step A to disperse into a solution, and the mass ratio of the added 50% methanol aqueous solution to...

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Abstract

The invention discloses a preparation method and application of cycloastragenol. The preparation method of the cycloastragenol comprises the following steps: by using astragaloside or astrasieversianin as a raw material, oxidizing, reducing, hydrolyzing, extracting and purifying to obtain high-purity cycloastragenol. The method is simple to operate, gentle in condition, good in product quality and high in yield. The cycloastragenol can be applied to preparation of anticancer adjuvant therapeutic medicine. An anticancer adjuvane therapeutic medicine prepared by using the cycloastragenol as a pharmaceutical active ingredient has the anticancer adjuvant therapeutic effect of enhancing the anticancer therapeutic effect, reducing the toxicity of the anticancer medicine, preventing and treating the neutropenia caused by the anticancer medicine therapy.

Description

technical field [0001] The invention relates to a preparation method of cycloastragenol and its application, belonging to the field of medicine and chemical industry Background technique [0002] Cancer is one of the three major diseases that endanger human health. Its morbidity and mortality have risen to the first place in some countries. In my country, about 3.5 million people suffer from cancer and 2.5 million people die of cancer every year. Constantly growing, and gradually showing a younger trend. Cancer causes direct economic losses of more than 100 billion yuan to my country every year. Therefore, the development of anticancer drugs is an important way to improve the quality of human life, and it is also one of the major issues faced by medical workers. Many anti-cancer drugs that have been successfully developed at present have obvious therapeutic effects, but their toxic and side effects are also obvious. While killing cancer cells, they also kill normal cells in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J53/00A61P35/00
Inventor 周先礼郭璐肖峰黄帅单连海
Owner SOUTHWEST JIAOTONG UNIV
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