Application of betulinic acid derivative in preparation of antitumor drugs

An anti-tumor drug, betulinic acid technology, applied in the field of medicine, can solve the problems of few reaction sites, lack of active groups in the parent nucleus, special structure, etc., and achieves the effect of good anti-tumor activity and wide use

Active Publication Date: 2020-12-29
上海科肽生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, pentacyclic triterpenoids have a special structure, lack of active groups in the mother nucleus, and few reaction sites, so it is difficult to prepare derivatives that meet the requirements by conventional chemical reaction methods

Method used

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  • Application of betulinic acid derivative in preparation of antitumor drugs
  • Application of betulinic acid derivative in preparation of antitumor drugs
  • Application of betulinic acid derivative in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1, structural formula is the preparation of the compound of formula I-formula VI

[0018] The invention adopts a microbial transformation method, uses betulinic acid as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. Circinella genus strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC), using potato medium, and stored on a solid slant medium in a refrigerator at 4°C.

[0019] Taking Circinella muscae CGMCC 3.2695 as an example, the process of preparing the compound whose structural formula is formula I-formula VI is as follows:

[0020] 1) Fermentation, transformation and extraction

[0021] Put Circinella muscae CGMCC 3.2695 into two 250mL Erlenmeyer flasks (containing 100mL potato culture medium) as seed solution. After shaking and culturing on a shaker at 160 rpm and 26°C for 1 day, when the mycelium growth is in a vigorous ...

Embodiment 2

[0028] Embodiment 2 The antitumor activity of compound I, compound II, compound III, compound IV, compound V and compound VI of the present invention

[0029] 1) Experimental materials

[0030] 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 belongs to the field of medicines, and discloses a betulinic acid derivative or pharmaceutically acceptable salts thereof, and an application of the betulinic acid derivative or pharmaceutically acceptable salts in preparation of antitumor drugs. The betulinic acid is successfully subjected to structural modification by utilizing a microbial conversion technology to obtain a plurality of novel compounds, and in-vitro anti-tumor cell tests prove that the compounds have better anti-tumor activity, can be used as active ingredients of anti-tumor drugs and have wide application.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of betulinic acid derivatives in the preparation of antitumor drugs. Background technique [0002] Betulinic acid is a kind of pentacyclic triterpenes with special structure. Its structural feature is that the E ring is a five-membered carbon ring, and the 19th position of the E ring is replaced by an isopropyl group in an α-configuration, and the five rings are all arranged in trans. Such ingredients are mainly distributed in birch bark, jujube seed, asparagus, pulsatilla and other traditional Chinese medicinal materials, and are the main active ingredients of the above-mentioned traditional Chinese medicines. Modern pharmacological studies have found that betulinic acid has a significant anti-tumor effect, and has obvious inhibitory effects on various tumor cells such as lung cancer, ovarian cancer, cervical cancer, breast cancer, and melanoma. Different from the typic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61P35/00A61P35/02A61K31/56C12P33/00C12R1/645
CPCA61P35/00A61P35/02C07J63/008C12P33/00
Inventor 陈广通宋开南张永珍储呈娇宋妍陈婷婷
Owner 上海科肽生物科技有限公司
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