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Novel anti- hepatitis B virus medicine compounds-lamivudine and protocatechuic acid

A technology of lamivudine and protocatechuic acid, which can be used in drug combinations, antiviral agents, pharmaceutical formulations, etc., can solve the problem of no major progress in antiviral treatment, reduce drug toxicity accumulation, and reduce the risk of virus resistance , improve the effect of drug efficacy

Inactive Publication Date: 2008-07-23
HUBEI UNIV
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although traditional Chinese medicine preparations have made progress or even breakthroughs in adjuvant treatment of hepatitis B, restoration of liver function, adjustment of immune function, and anti-hepatic fibrosis, there has been no major progress in solving the fundamental problem of hepatitis B, that is, antiviral treatment
[0006] For the treatment of hepatitis B, no matter western medicine or traditional Chinese medicine, there is no completely effective medicine to suppress and kill the virus at present.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] HBsAg detection: (by the operation in step (2)) when protocatechuic acid is 50 μ g / mL, to HBsAg inhibitory rate is 27.3%; When lamivudine is 0.5 μ g / mL, to HBsAg inhibitory rate is 30.8%; When 50μg / mL combined with lamivudine 0.5μg / mL, the HBsAg inhibition rate was 50.4%.

Embodiment 2

[0040] HBeAg detection: (operation in step (3)) when protocatechuic acid is 5 μ g / mL, to HBeAg inhibitory rate is 17.6%; When lamivudine is 0.05 μ g / mL, to HBeAg inhibitory rate is 11.0%; Protocatechuic acid When 5μg / mL combined with lamivudine 0.05μg / mL, the HBeAg inhibition rate was 34.3%.

Embodiment 3

[0042] Fluorescence quantitative PCR of HBV DNA is measured: (by the operation in step (4)) when protocatechuic acid 50 μ g / mL, to HBV DNA inhibitory rate 16.9%; When lamivudine 0.05 μ g / mL, to HBV DNA inhibitory rate 53.5%; when protocatechuic acid 50μg / mL combined with lamivudine 0.05μg / mL, the HBV DNA inhibition rate was 61.4%.

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Abstract

The invention provides an anti-HBV medicine combination which has more remarkable treatment effect and safety and no toxic and side effect and can evidently increase the negative conversion ratio of HBSAg. The invention takes HepG2.2.15 as a target cell and adds lamivudinevir, protocatechuic acid and the compatibility preparation of lamivudinevir and protocatechuic acid with a proper concentration to cell culturing medium. The cell is cultured by a regular method and HBsAg and HBeAg secreted by the cell is detected by ELISA method, HBV DNA content is measured by fluorescent quantitation PCR, HBV resistance effect of the drug is judged by depression rate calculation method to determine the medical treatment effect on HBV and the preparation proportion of medicine combination. The proportion of lamivudinevir to protocatechuic acid is between 1 to 50 and 1 to 100 (mass ratio) and generally the dosage of lamivudinevir is 0.05-5Mug and the protocatechuic acid is 5-500 Mug. The medicine combination can evidently improve the depression effect of the lamivudinevir on Hepatitis B antigen and reduce the toxic and side effect of the lamivudinevir when being used separately.

Description

technical field [0001] The invention relates to a new drug combination for treating hepatitis B virus - lamivudine and protocatechuic acid, including the formula ratio of the drug combination and its experimental curative effect. Through the single-use and combined use of the drug combination for hepatitis B virus experimental research, it is confirmed that the drug combination has a better therapeutic effect on the hepatitis B virus than the single use of lamivudine and protocatechuic acid. Background technique [0002] Acute and chronic infection of hepatitis B virus (HBV) is an important cause of hepatocellular necrosis, hepatocellular inflammation, and primary hepatocellular carcinoma (HCC). Acute and chronic infection of hepatitis B virus (HBV) is an important cause of hepatocellular necrosis, hepatocellular inflammation, and primary hepatocellular carcinoma (HCC). About 0.5% of cases of acute infection will eventually lead to fatal acute hepatitis. Chronic infection ...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K31/192A61P1/16A61P31/12
Inventor 韩凤梅张晓雷朱文婷吴建国王恒松陈勇
Owner HUBEI UNIV
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