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Protopanoxadiol peroxide derivatives as well as preparation method and application thereof

A technology of peroxidation of panaxadiol and protopanaxadiol, which is applied in the field of biomedicine, can solve the problems of few reaction sites, difficulty in preparing derivatives, lack of active groups, etc., and achieves the effect of good antitumor activity

Active Publication Date: 2012-11-07
三蚁科技(广州)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, protopanaxadiol 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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  • Protopanoxadiol peroxide derivatives as well as preparation method and application thereof
  • Protopanoxadiol peroxide derivatives as well as preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0021] Embodiment 1, preparation of protopanaxadiol peroxidized derivatives of formula I, formula II and formula III of the present invention

[0022] The invention adopts a microbial transformation method, uses protopanaxadiol 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 ( Absidia ), Xiaogram silvery mildew ( Cunninghamella ), Mucor ( Mucor ), Alternaria ( Alternaria ), Acremonium ( Acremonium ), red yeast ( Rhodotorula ), Syncephalum ( Syncephalastrum ), Aspergillus ( Aspergillus ) or Rhizopus ( Rhizopus ) of the genus of microorganisms, among which Absidia mould( Absidia ), Acremonium ( Acremonium ), Rhizopus ( Rhizopus ), Aspergillus ( Aspergillus ) or Mucor ( Mucor ) strains of the genus. These strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC) or the C...

Embodiment 2

[0045] Example 2 Antitumor Activity of Protopanaxadiol Peroxidized Derivatives of Formula I, Formula II and Formula III

[0046] 1) Experimental materials

[0047] 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), RPM I 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 protopanoxadiol peroxide derivatives as well as a preparation method and an application of the protopanoxadiol peroxide derivatives. The structural formulae of the protopanoxadiol peroxide derivatives disclosed by the invention are shown in formulae I, II and III. In the method, the microbial conversion technology is utilized to modify structure of protopanoxadiol successfully so as to obtain various novel compounds. In-vitro anti-tumor cell test shows that the compounds have better anti-tumor activity, so that the compounds can be used as active components of the anti-tumor drug and have wide application.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a protopanaxadiol peroxidized 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. At present, most of the mainstream anti-tumor drugs commonly used in clinical practice are derived from natural medicines, or products obtained afte...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61P35/00C12P33/00C12R1/65C12R1/785C12R1/845C12R1/685C12R1/645
Inventor 陈广通杨雪凌勇翟旭光
Owner 三蚁科技(广州)有限公司
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