Use of 15-methano-substituted-andrographolide derivative in preparing anti-hepatitis B medicine

A technology of andrographolide, hepatitis B, applied in the directions of drug combination, antiviral agent, pharmaceutical formula, etc., can solve the problems such as no relevant reports, and achieve the effect of expanding the range of options

Active Publication Date: 2009-04-29
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The novel α-glucosidase inhibitor 15-methylene substituted andrographolide derivative synthesized with andrographolide (AD) as the lead compound has been reported in the patent CN: 200510107247.4, which is the applicant's previous research results. In the later stage, more in-depth research was carried out on it, and the research showed that this type of compound has a significant anti-HBV effect in vitro, and there is no relevant report on its application as a drug for the treatment and prevention of hepatitis B (anti-HBV) at present.

Method used

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  • Use of 15-methano-substituted-andrographolide derivative in preparing anti-hepatitis B medicine
  • Use of 15-methano-substituted-andrographolide derivative in preparing anti-hepatitis B medicine
  • Use of 15-methano-substituted-andrographolide derivative in preparing anti-hepatitis B medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1 In vitro anti-HBV activity experiment of 15-methylene substituted andrographolide derivatives

[0014] 1. Cell Culture and Drug Treatment

[0015] The human liver cancer cell line HepG2.2.15 cell (provided by Henan Academy of Medical Sciences) that adopts hepatitis B virus gene transfection detects that the medicine of the present invention is effective against HBV surface antigen (HBsAg) and HBV in the HepG2.2.15 cell culture supernatant. Effect of core antigen (HBeAg) and HBV DNA content. The 2.2.15 cell suspension was inoculated in a 48-well plate (Costar, USA), and the cell number was 1.25×10 4 / well, add 0.5mL RPMI1640 culture solution, the culture solution contains 10% fetal bovine serum (Tianjin Haoyang Biological Products Technology Co., Ltd., batch number: XA080329), 380 μg / mL G418 (Invitrogen Life Technologies, USA), 100 μg / mL streptomycin (1 million units / bottle, produced by North China Pharmaceutical Co., Ltd., batch number: 060606), 100 IU / mL pe...

Embodiment 2

[0033] The acute toxicity experiment of embodiment 2 ADD-2

[0034] Animal: Clean grade Kunming mice, weighing 20±2g, half male and half male, certificate number: 0009898 Henan Province

[0035] Provided by Experimental Animal Center.

[0036] Drug: 15-methylene substituted andrographolide derivatives of the present invention

[0037] Experimental method: Take 20 mice weighing 20±2g, half male and half male, and randomly divide them into ADD-2 low-dose group and ADD-2 high-dose group, with 10 mice in each group. After the animals were fasted for 12 hours (drinking water was not restricted), the doses of 2.00 g / kg and 5.00 g / kg of ADD-2 were administered by intragastric administration respectively, and the intragastric administration volume was 0.2 mL / 10 g. Observe and record the poisoning performance of the animals. Weigh once a week. Continuous observation for 14 days, the results are shown in Table 3.

[0038] Experimental results: The mice did not show obvious signs of...

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Abstract

The invention discloses the medical application of a 15-methylene replaced andrographolide derivant as shown in general formula 1, more particularly relates to the application thereof in preparing anti-hepatitis B virus drugs, pertaining to the pharmaceutical chemistry field. HepG2.2.15 cells are used for detecting the secretory volumes of HBsAg and HBeAg and the HBV DNA level related to viral particles in the supernatant liquid of a nutrient solution, and the result shows that the 15-methylene replaced andrographolide derivant has good in-vitro anti-HBV effect. The 15-methylene replaced andrographolide derivant has better development and application prospect by being applied in preparing drugs used for treating and preventing Hepatitis B.

Description

technical field [0001] The invention relates to the medicinal use of andrographolide, in particular to the anti-hepatitis B virus drug effect of 15-methylene substituted andrographolide derivatives, and belongs to the field of medicinal chemistry. Background technique [0002] Andrographolide is a diterpene lactone compound extracted from Andrographis paniculata (Burm.f.) Nees. It is one of the main active ingredients of Andrographis paniculata (Burm.f.) Nees. It is mainly used clinically to treat upper respiratory tract infection and bacillary dysentery. In recent years, modern pharmacological studies have found that andrographolide not only has antibacterial and anti-inflammatory effects, but also has anti-tumor, liver-protecting and gallbladder-protecting, and anti-viral effects. There have been many reports on the antiviral research of Andrographis paniculata and its extracts. Andrographis paniculata extract can effectively treat respiratory tract infection and viral pn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P1/16A61P31/12
Inventor 刘宏民戴桂馥王庆端徐海伟郑立运马文艳赵进汤臻刘改枝
Owner ZHENGZHOU UNIV
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