Application of ring A substituted silybin ester in preparing medicaments for treating viral hepatitis B

A technology for the use of silibinin, which is applied in the field of the use of A ring to replace silibinin ester for the preparation of drugs for the treatment of viral hepatitis B, can solve the problems that the new use has not been effectively developed, and achieve the benefits of large-scale production, The effect of convenient source, huge social benefit and economic benefit
CN101829101BInactive Publication Date: 2012-05-23DALI UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
DALI UNIV
Publication Date
2012-05-23
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to application of ring A substituted silybin ester in preparing medicaments for treating viral hepatitis B, in particular to application of silybin ester flavonolignan substituted by ethoxycarbonyl methyl on the ring A or a pharmaceutically acceptable salt thereof for preparing medicaments for reducing the hepatitis B virus surface antigen (HBsAg), suppressing the HBV (Hepatitis B Virus) DNA replication and treating HBV infection diseases. The flavonolignan has quite obvious activity on suppressing the HBsAg, and in the presence of a concentration of 100 micrograms / milliliter, the intensity of the flavonolignan for clearing away the HBsAG exceeds that of alpha-interferon which is a positive control medicament by 3.3 times. Meanwhile, in the presence of a concentration of 20 micrograms / milliliter, suppression ratio of the compound to the HBV DNA is close to 60 percent. The pharmacodynamical results indicate that the flavonolignan or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicaments for treating the HBV infection diseases.
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Description

technical field

[0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a kind of silybin ester flavonoid lignan or its pharmaceutically acceptable salt which is substituted by ethoxyformyl methyl group on the A ring for the preparation of HBV surface-reducing Antigen HBsAg medicine, inhibition of HBV DNA replication, the purposes of medicine for treating hepatitis B virus infection disease, this flavonoid lignan has very significant activity of inhibiting HBsAg, and its clearing HBsAg intensity exceeds positive control medicine ( 10000 units / mL of α-interferon) 3.3 times; meanwhile, the compound showed an inhibition rate of nearly 60% on HBV DNA at a concentration of 20 μg / mL. The above pharmacodynamic results show that the flavonoid lignan or its pharmaceutically acceptable salt can be expected to be used in the preparation of drugs for reducing the surface antigen of hepatitis B virus, inhibiting HBV DNA repli...

Claims

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