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Derivative of protopanoxatriol, prepn. method and application thereof

A technology of protopanaxatriol and derivatives, which is used in pharmaceutical formulations, drug combinations, steroids, etc., can solve the problems of few reaction sites, difficulty in preparing derivatives, lack of active groups, etc., and achieve good antitumor activity. , the effect of a wide range of uses

Inactive Publication Date: 2006-09-13
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, protopanaxatriol belongs to tetracyclic triterpenoids, lacks active groups, and has few reaction sites. It is difficult to prepare derivatives that meet the requirements by conventional chemical reaction methods.

Method used

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  • Derivative of protopanoxatriol, prepn. method and application thereof
  • Derivative of protopanoxatriol, prepn. method and application thereof
  • Derivative of protopanoxatriol, prepn. method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0022] Embodiment 1, structural formula is the preparation of the compound of formula II, formula III and formula IV

[0023] The invention adopts a microbial conversion method, uses protopanaxatriol as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. Microorganisms capable of transforming include Cunninghamella, Aspergillus, Mucor, Trichoderma, Syncephalastrum, or Rhizopus; among them, the transforming ability is relatively strong Mucor (Mucor) and Rhizopus (Rhizopus) belong to bacterial strains.These bacterial strains can all be purchased from Chinese Academy of Sciences Microorganism Culture Collection Management Center (CGMCC) and China Food Fermentation Research Institute Industrial Microbiology Collection Management Center (CICC), at The solid slant medium was stored in a refrigerator at 4°C. Potato medium was used for fungal culture, and LB medium was used for bacterial culture.

[0024] Prep...

Embodiment 2

[0052] Embodiment 2, the antitumor activity of the compound of the present invention

[0053] 1. Experimental materials

[0054] Instruments and reagents: Microplate reader is TECAN porous spectrophotometer (U.S.A); CO 2 The gas incubator is BB5060 UV clean type CO 2 The incubator (Heraeus Co.); the high-speed refrigerated centrifuge is TGL-16G high-speed refrigerated centrifuge (Shanghai Scientific Instrument Factory). All chemical reagents used were of analytical grade (Beijing Chemical Reagent Factory); cell culture media were purchased from Sigma Chemical Company (St.Louis, MO, USA) and Hyclone Company (Logan, Utah, USA)

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Abstract

The invention discloses the ramification of the protopanaxatriol and a method of the production and the appliance. The formula of the ramification of the protopanaxatriol is the formula I, thereinto, R1 is -OH or H; R2 is -CH3 or -CH20H; R3 is -CH3 or -CH20H. The invention adopts the technique of the microbial conversion to the structure qualification of the protopanaxatriol, Then a great variety of new compounds are gained. With the verification of the vitro resisting tomour cell test, the compound has the better function of the anti-tumor activity and can be used for the active constitution of the antineoplastic. The compound has the broad purpose.

Description

technical field [0001] The present invention relates to compounds and their preparation methods and applications, in particular to protopanaxatriol derivatives and their preparation methods, as well as the medical use of the derivatives. Background technique [0002] Malignant tumors are one of the major diseases that endanger human health. The research and development of anti-tumor drugs has always been an important research content in the field of medicine. So far, most of the mainstream anti-tumor drugs commonly used in clinic are derived from natural medicines, or products obtained after structural modification of natural medicines as lead compounds. Such as plant-derived vincristine, podophyllotoxin-modified etoposide, and paclitaxel, which is popular all over the world, indicate that natural products are still an important source of antitumor drugs. [0003] Ginseng is a well-known traditional Chinese medicine, which occupies an important position in the traditional C...

Claims

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Application Information

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IPC IPC(8): C07J9/00C12P33/00A61K31/575A61P35/00
Inventor 郭洪祝田茵果德安
Owner PEKING UNIV
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