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Application of pentacyclic triterpene compound and medicine composition

A technology of pentacyclic triterpenoids and compounds, which is applied in the application of pentacyclic triterpenoids and the field of pharmaceutical compositions, can solve the problems of high toxicity and side effects, insufficient drug efficacy, poor bioavailability, etc., and achieve high inhibitory activity Effect

Inactive Publication Date: 2016-04-20
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a class of BCL-XL inhibitors that can be used to prepare BCL- The pentacyclic triterpenoid compound of the XL inhibitor, the pentacyclic triterpenoid compound of the present invention can also be used to prepare a medicine for treating diseases caused by impaired apoptosis, especially cancer

Method used

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  • Application of pentacyclic triterpene compound and medicine composition
  • Application of pentacyclic triterpene compound and medicine composition
  • Application of pentacyclic triterpene compound and medicine composition

Examples

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Embodiment 1

[0047] The polypeptide QEDIIRNIARHLAQVGDSMDRSIPPG (the sequence of the peptide is shown in SEQ ID NO: 1 in the sequence listing) is the BH3 region of the BID protein, which is synthesized by Jill Biochemical (Shanghai) Co., Ltd., and its N-terminus is subjected to 5-carboxyfluorescein (5 -FAM) labeling, in order to facilitate fluorescence detection and improve the sensitivity of detection, the peptide structure of the obtained substrate peptide is shown in formula E:

[0048]

[0049] The BCL-XL protein used in the examples is obtained after fusion expression of His tag and enzyme digestion and purification. ABT-737 was purchased from Selleckchem Company in the United States, with the structure shown in formula F, product number: S1002; norzeramaldehyde was purchased from Shanghai Chunyou Biotechnology Co., Ltd., product number: P0820; tripterygium was purchased from Shanghai A Latin Biochemical Technology Co., Ltd., product number: 1125828.

[0050]

[0051] Prepare 50...

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Abstract

The invention discloses application of a pentacyclic triterpene compound and a medicine composition, and further discloses the pentacyclic triterpene compound shown in the formula A or the formula B in the specification, and application of a stereoisomer or a tautomer or pharmaceutically acceptable salt or solvate or polymorph of the pentacyclic triterpene compound in preparing medicine for treating diseases (especially cancer) caused by cell apoptosis or cell damage and a BCL-XL inhibitor. R1, R2, R3, R4, R5, R7, R8, R9, R10 and R11 are independently selected from one of hydroxyl, hydrogen, halogen, COR13, COOR14, C1-C4 alkoxy and C1-C4 alkyl, and R6, R12, R13 and R14 are independently selected from hydrogen or C1-C5 alkyl. The pentacyclic triterpene compound has higher inhibitory activity on binding between BCL-XL and pro-apoptosis protein and has guiding significance on design and research and development of the medicine.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application and pharmaceutical composition of a pentacyclic triterpenoid compound. Background technique [0002] The BCL-XL protein is a protein of the BCL-2 (B-cell lymphoma / leukemia-2) family. The BCL-2 gene was first discovered in 1984 in follicular non-Hodgkin B-cell lymphoma. BCL-2 family proteins play an important regulatory role in the mitochondrial pathway of apoptosis, and can be divided into three families according to their structure and function: BCL-2 family, BAX family and BH3-only family. Among them, the proteins in the BCL-2 family (BCL-2, BCL-XL, MCL-1, BCL-W, etc.) play the role of anti-apoptosis, and the members of the latter two families play the role of promoting apoptosis. Structurally speaking, the proteins of these three families all contain at least one BCL-2 homology (BCL-2homology, BH) domain, in which the first two families have three sequence ...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P35/00A61P35/02
CPCA61K31/56
Inventor 康经武徐美
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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