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Pentacyclic triterpenoid compound and application of plant extract containing same

A technology of pentacyclic triterpenes and plant extracts, which is applied in the application field of medicine and achieves the effects of small side effects, low cost and excellent anti-hepatitis C virus.

Inactive Publication Date: 2012-07-11
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Pentacyclic triterpenoids widely exist in nature, and it is currently known that they have anti-inflammatory, antibacterial, anti-tumor cell proliferation, induction of apoptosis, anti-AIDS effects, but these compounds are used to prepare anti-hepatitis C virus Drugs that have not been reported so far

Method used

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  • Pentacyclic triterpenoid compound and application of plant extract containing same
  • Pentacyclic triterpenoid compound and application of plant extract containing same
  • Pentacyclic triterpenoid compound and application of plant extract containing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0020] Example in vitro cell test

[0021] 1. Sample preparation

[0022] Betulinic acid and oleanolic acid samples were respectively dissolved in 100% dimethyl sulfoxide (DMSO) to a mother solution with a concentration of 20 mg / ml, and stored at 4°C. When testing, each stock solution was diluted with 100% DMSO to 5 mg / ml and 2 mg / ml solutions.

[0023] 2. Cell, virus and cell culture

[0024] This study employed a Huh7-derived cell line and an HCV strain capable of producing high-titer, infectious-competent HCV virus particles in the cells.

[0025] cells at 1 x 10 4 Cells / 100 μl / well were seeded in 96-well cell culture plates and cultured overnight. The HCV supernatant was diluted to 1×10 with complete medium DMEM (containing 10% fetal bovine serum, 100 U / ml penicillin, 100 μg / ml streptomycin) in DMEM. 3 ffu / ml, infect cells at 50ffu / well.

[0026] 3. HCV virus colony reduction experiment

[0027] Dilute sample solutions with different concentrations (1mg / ml, 0.5mg / ml...

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Abstract

The invention discloses a pentacyclic triterpenoid compound shown in a formula A or B and an application of a plant extract containing the pentacyclic triterpenoid compound in the preparation of a drug for resisting hepatitis virus C. The pentacyclic triterpenoid compound has the advantages of good treatment effect, low cost and less side effects; and the invention provides a new way for the treatment of the hepatitis C virus. In the formula A, R1 is H, OH or glucoside; R2 is H, OH or glucoside; R3 is CH3, CH2OH or glucoside; R4 is CH3, CH2OH or glucoside; R5 is CH3, COOH or glucoside. In the formula B, R1' is H, OH or glucoside; R2' is H, OH or glucoside; R3' is CH3, CH2OH or glucoside; R4' is CH3, CH2OH or glucoside; R5' is H or OH; R6' is H or CH3; T7' is H or CH3; R8' is H or OH; and R9' is CH3, COOH or glucoside. The formula A and the formula B are shown in the description.

Description

technical field [0001] The present invention relates to the application of a class of pentacyclic triterpenoids and plant extracts containing them in the field of medicine, in particular to the use of the pentacyclic triterpenoids and plant extracts containing them in the preparation of anti-hepatitis C virus medicines in the application. Background technique [0002] According to incomplete statistics, there are as many as 40 million hepatitis C antibody-positive patients in my country, and 80% of them will suffer from chronic hepatitis C. Hepatitis C is a liver disease that is transmitted through blood, sexual contact, mother to child and daily life contact. After HCV infection, like HBV infection, chronic hepatitis, liver cirrhosis and liver cancer are prone to occur. [0003] Currently, long-acting interferon combined with ribavirin is mainly used to treat hepatitis C patients with normal liver function, and the overall sustained virological response rate is 52%. Howe...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K36/536A61P31/14A61P1/16
Inventor 高雯李波翁小香张静成亮邵燕周靖欧阳丹薇吕峰孔德云
Owner SHANGHAI INST OF PHARMA IND
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