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Preparation method and application of 20 (R)-panaxatriol derivative

A technology of panaxatriol and derivatives, 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 good anti-tumor activity and wide application

Active Publication Date: 2016-09-21
SHENZHEN SUN BIO SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, 20(R)-panaxatriol 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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  • Preparation method and application of 20 (R)-panaxatriol derivative
  • Preparation method and application of 20 (R)-panaxatriol derivative
  • Preparation method and application of 20 (R)-panaxatriol derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1, structural formula is the preparation of the compound of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI and formula XII

[0041] The invention adopts a microbial transformation method, uses 20(R)-panaxatriol 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 funga...

Embodiment 2

[0067] Example 2 The structural formula of the present invention is the anti-tumor activity of the compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI and formula XII.

[0068] 1) Experimental materials

[0069] 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 20 (R)-panaxatriol derivative and a preparation method and application thereof. Structural formulas of the 20 (R)-panaxatriol derivative are formulas I, II, III, IV, V, VI, VII, VIII, IX, X, XI and XII. Microbial conversion technology is utilized, 20 (R)-panaxatriol is structurally modified successfully, and various novel compounds are obtained; in-vitro anti-tumor cell experiments verify that the compounds have high anti-tumor activity, can serve as active ingredients of anti-tumor drugs and have wide application range.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a 20(R)-panaxatriol derivative, a preparation method thereof, and a medical application 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] Modern pharmacological studies have shown that 20(R)-panaxatriol has a good tumor-inhibiting effect, and can also enhance the curative effect of chem...

Claims

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Application Information

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IPC IPC(8): C07J17/00A61K31/58A61P35/00C12P33/20C12P33/06C12P33/12C12R1/645C12R1/785C12R1/65C12R1/845
CPCC07J17/00C12P33/06C12P33/12C12P33/20
Inventor 陈广通宋妍李建林葛红娟李杰颜森森
Owner SHENZHEN SUN BIO SCI & TECH CO LTD
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