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Application of leonurine in preparation of anti-hepatitis B virus drugs

A technology of leonurine and hepatitis B virus, applied in the field of medicine, can solve the problems of multiple side effects of interferon, high virus rebound rate, low HBsAg clearance rate and the like

Pending Publication Date: 2021-09-28
FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Currently, approved drugs for the treatment of chronic hepatitis B virus infection (CHB) include nucleoside analog reverse transcriptase inhibitors (NUCs) and interferon, which exhibit significant antiviral activity, but due to low clearance of HBsAg , NUCs have a high rate of viral rebound after drug withdrawal, and there are many side effects of interferon [Gish RG, Given BD, et al. Chronicepatitis B: Virology, natural history, current management and a glimpse at future opportunities. 2015], including influenza-like syndrome symptoms, headache, myalgia, fatigue, depression and local injection site reactions, etc., the overall treatment effect is not satisfactory

Method used

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  • Application of leonurine in preparation of anti-hepatitis B virus drugs
  • Application of leonurine in preparation of anti-hepatitis B virus drugs
  • Application of leonurine in preparation of anti-hepatitis B virus drugs

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Embodiment 1

[0031] Hep G2.2.15 cell line: The human hepatoblastoma cell line Hep G2.2.15 stably expressing HBV was used. HepG2.2.15 cells were placed at 37°C, 5% concentration of CO 2 Cultured under conditions, screened and passaged under G418 drug pressure, all experiments were carried out in accordance with cell experiment specifications, and obtained permission from the Molecular Virus Laboratory of Fudan University School of Basic Medical Sciences, all cell grouping experiments were performed with the same starting conditions and random grouping conduct.

[0032] Drugs: G418 Sulfate (450-130-ZL, WISENT, 20mL) was used to maintain the continuous and stable expression of HBsAg and HBeAg in Hep G2.2.15 cells, and Leonurine (24697-74-3, HPLC>98%) and Lamivudine (134678-17 -4, Macklin, 5g) were dissolved in DMSO (D2650, Sigma-Aldrich, 100mL), and evenly added to the cell culture medium, and the different dose groups were adjusted to the corresponding final concentration gradient of mother...

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Abstract

The invention belongs to the technical field of medicines, and relates to a compound aiming at hepatitis B virus surface antigen (HBsAg), in particular to a leonurine hydrochloride (Leonurine) (CAS: 24697-74-3) aiming at hepatitis B virus surface antigen (HBsAg). The compound is a monomer extracted and chemically synthesized from traditional Chinese medicine motherwort, and tests show that the compound can effectively reduce the HBsAg in vitro supernatant and has an effect on reducing the hepatitis B e antigen (HBeAg) in vitro supernatant. The compound leonurine can be used for targeted reduction of extracellular HBsAg and HBeAg, and provides support for research and development of therapeutic drugs and methods for effective reduction of HBsAg and HBeAg in HBV persistent infection.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to compound medicines against hepatitis B virus, in particular to compound medicines against hepatitis B virus surface antigen (HBsAg). It specifically relates to a compound leonurine hydrochloride (Leonurine) (CAS: 24697-74-3) directed at the surface antigen of hepatitis B virus (HBsAg). Tests have shown that the compound leonurine can effectively reduce HBsAg in vitro. , and has the effect on reducing the supernatant hepatitis B e antigen (HBeAg) in vitro, and can prepare anti-hepatitis B virus medicine. Background technique [0002] Hepatitis B virus (HBV) infection has been reported to be a worldwide health problem, and it is estimated that approximately 260 million people worldwide are chronically infected with HBV [WHO 2019]. In 2015, it was reported that the global death toll from viral hepatitis reached 1.34 million, which was comparable to the death toll from tuberculosis, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/235A61K45/06A61P1/16A61P31/20
CPCA61K31/235A61K45/06A61P1/16A61P31/20
Inventor 赵超荆沙
Owner FUDAN UNIV
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