Protopanaxatriol derivatives and their preparation methods and applications

A technology of protopanaxatriol and its derivatives, which is applied in the field of biomedicine, can solve the problems of few reaction sites, lack of active groups, and difficulty in preparing derivatives, etc., and achieve the effect of wide application and good anti-tumor activity

Active Publication Date: 2016-09-28
山东亚泰医疗器械有限公司
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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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  • Protopanaxatriol derivatives and their preparation methods and applications
  • Protopanaxatriol derivatives and their preparation methods and applications
  • Protopanaxatriol derivatives and their preparation methods and applications

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Embodiment 1, structural formula is the preparation of the compound of formula I, formula II, formula III, formula IV and formula V

[0022] 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 transformation include: Absidia, Cunninghamella, Mucor, Alternaria, Rhodotorula, Syncephalastrum or Rhizopus (Rhizopus) microorganisms; Among them, strains of Absidia and Mucor have stronger transforming ability. These strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC) or the China Institute of Food Fermentation Industrial Microbiology Collection Center (CICC), and stored on a solid slant medium in a refrigerator at 4 °C. Potato medium was selected as the fungal medium, and LB medium was selected as the bacterial medium.

[0023] Preparation of potat...

Embodiment 2

[0053] Embodiment 2 The antitumor activity of compound I, compound II, compound III, compound IV and compound V of the present invention

[0054] 1) Experimental materials

[0055] Instruments and reagents: CO 2 Incubator (Jouan IGO150); Microplate reader (Bio-TEK ELx800); Fluorescence inverted microscope (Olympus IX51); MTT cell proliferation and cytotoxicity detection kit (Biotech Institute), RPMI 1640 medium (Gibcol BRL ), RNase A, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

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Abstract

The invention discloses a protopanaxatriol derivative as well as a preparation method and application thereof. The structural formula of the protopanaxatriol derivative includes a formula I, a formula II, a formula III, a formula IV and a formula V. According to the invention, protopanaxatriol is successfully subjected to structure modification by utilizing a microbial transformation technology so as to obtain multiple novel compounds, and an in-vitro antitumor cell test proves that the compounds have preferable antitumor activity, can serve as active components of an antitumor drug and have wide application.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a protopanaxatriol derivative, a preparation method thereof and the medical use of the derivative. 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. Natural products have always been the source of human beings looking for effective active ingredients. In the process of new drug development, on the one hand, natural products with good activity can be directly used clinically; Finding and developing new high-efficiency and low-toxic drugs by means of modification is one of the most effective ways to develop new drugs that has been proven in practice. [0003] Ginsenosides, the main active ingredients in ginseng, have good anti-tumor effects. Whether it is in vitro cell tests or epidemiological investigations, the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00C12P33/12C12P33/06C12P33/02C12P33/00A61P35/00A61P35/02
CPCC07J9/00C12P33/00C12P33/02C12P33/06C12P33/12
Inventor 陈广通宋妍李建林葛红娟李杰黄金华
Owner 山东亚泰医疗器械有限公司
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