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Protopanaxadiol derivative and application thereof

A technology of protopanaxadiol and its derivatives, which is applied in the application fields of esters or solvates, protopanaxadiol derivatives and pharmaceutically acceptable salts thereof, in the preparation of drugs for treating and/or preventing tumors, and can solve the problem of can not be completely and effectively cured and other problems

Active Publication Date: 2013-11-13
南通药享科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

None of the existing tumor drugs can completely and effectively cure

Method used

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  • Protopanaxadiol derivative and application thereof
  • Protopanaxadiol derivative and application thereof
  • Protopanaxadiol derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1, the structural formula is the preparation of the protopanaxadiol derivative of formula I

[0030] 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, Cunninghamella, Mucor, Alternaria, Rhodotorula, Syncephalastrum, or Rhizopus (Rhizopus) genus microorganisms; Among them, strains of Absidia (Absidia) and Mucor (Mucor) genera 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.

[0031] Preparation of...

Embodiment 2

[0046] Embodiment 2 The antitumor activity of compound I of the present invention

[0047] 1) Experimental materials

[0048] 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 I1640 medium (Gibcol BRL ), RNase A, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

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PUM

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Abstract

The invention discloses a protopanaxadiol derivative and pharmaceutically-acceptable salts, esters or solvates thereof. The protopanaxadiol derivative and the pharmaceutically-acceptable salts, esters or solvates thereof have a structure shown in the formula I. The invention further discloses application of the protopanaxadiol derivative and the pharmaceutically-acceptable salts, esters or solvates thereof in the preparation of drugs for treating and / or preventing tumors, particularly cervical carcinoma, leukemia, neuroblastoma, prostatic carcinoma, liver cancer and mammary cancer.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a protopanaxadiol derivative and its pharmaceutically acceptable salt, ester or solvate and its application in the preparation of drugs for treating and / or preventing tumors. Background technique [0002] Malignant tumors are one of the main diseases that endanger human health. In my country, about 1.5 million people are newly diagnosed with tumors every year, and more than 800,000 people die of tumors every year. None of the existing tumor drugs can completely and effectively cure the disease. At the same time, due to the continuous discovery of new tumors, people are forced to find new anti-tumor drugs. [0003] 20(S)-Protopanaxadiol is a protopanaxadiol-type saponin, such as the aglycone of ginsenosides Rh2, Rg3, and C-K. 20(S)-Protopanaxadiol has obvious anti-tumor effect, can inhibit tumor cell proliferation, promote tumor cell apoptosis, induce tumor cell differentiation, impro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00C12P33/00A61K31/575A61P35/00C12R1/65
Inventor 陈广通宋妍杨雪葛红娟李建林
Owner 南通药享科技有限公司
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