Application of andrographolide C15 substitution derivative in manufacturing anti-hepatitis drug

A technology of andrographolide and drug preparation, which is applied in the direction of drug combination, antiviral agent, pharmaceutical formula, etc., can solve the problems such as vaccines that have not been researched, and achieve the effect of clarifying the anti-BVDV activity in vitro

Active Publication Date: 2012-07-25
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current effective anti-HCV treatment is limited to interferon therapy or the combination therapy of interferon and ribavirin (ribavirin), and a vaccine that can effectively prevent HCV has not yet been developed

Method used

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  • Application of andrographolide C15 substitution derivative in manufacturing anti-hepatitis drug
  • Application of andrographolide C15 substitution derivative in manufacturing anti-hepatitis drug
  • Application of andrographolide C15 substitution derivative in manufacturing anti-hepatitis drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 In vitro anti-BVDV activity experiment of C15-substituted andrographolide derivatives

[0026] 1. Cell culture and drug treatment

[0027] Adopt MDBK (NBL-1) cells (purchased from Shanghai Typical Culture Collection Center, Chinese Academy of Sciences), bovine viral diarrhea virus (BVDV-AV69) (purchased from China Veterinary Drug Inspection Institute), study the drug of the present invention on the inoculation of BVDV virus Therapeutic effect on cytopathic diseases. Ribavirin (R; Henan Runhong Pharmaceutical Co., Ltd., batch number: 1102261) was used as a positive drug control. Suspension (1 × 10 5 / mL) were inoculated in 96-well plates (Costar, USA), 200 μL / well, and the culture medium contained 10 % fetal bovine serum (Zhejiang Tianhang Biotechnology Co., Ltd., batch number: 100524), 100 μg / mL streptomycin (Shenzhen Huayao Nanfang Pharmaceutical Co., Ltd., batch number: N09081), 100 IU / mL penicillin (produced by North China Pharmaceutical Co., Ltd., ba...

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Abstract

The invention discloses the application of an andrographolide C15 substitution derivative in manufacturing an anti-hepatitis drug, which belongs to the technical field of pharmaceutical chemistry. According to the invention, MDBK (mardin-darby bovine kidney cells) and BVDV (bovine viral diarrhea virus) are utilized to study the inhibitory action of the compound on cytopathic effect caused by the virus through an external screening model. Through the screening of a large number of andrographolide derivatives, the compound with a structure of general formula 1 is found to significantly inhibit MDBK cytopathic effect caused by the BVDV; the andrographolide C15 substitution derivative has high efficiency and low toxicity, thereby being used for manufacturing medicaments for treating and preventing hepatitis and having good prospect in development and application. The general formula 1 is shown in the description.

Description

technical field [0001] The invention relates to the medicinal use of andrographolide derivatives, in particular to the application of andrographolide C15-position substituted series derivatives in the preparation of anti-hepatitis C drugs, and belongs to the technical field of medicinal chemistry. Background technique [0002] Andrographolide (AD) is a plant of Andrographis paniculata [ Andrographis paniculata (Burm. f) Nees], which is one of the main active ingredients of the traditional Chinese medicine Andrographis paniculata, is mainly used in the treatment of upper respiratory tract infection, bacillary dysentery and other diseases in clinical practice. In recent years, studies have found that andrographolide also has anti-tumor, liver-protecting and gallbladder-protecting, anti-viral and other effects. Andrographolide and its derivatives have good prospects in anti-flavivirus, pestilence or hepatitis C virus (CN: 200580046253.1) and anti-SARS virus (CN: 03129127.9). ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K31/443A61P1/16A61P31/14
Inventor 戴桂馥徐海伟王亚楠刘宏民李伟义
Owner ZHENGZHOU UNIV
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