Application of ring E bromine substituted silybin in preparing medicaments for treating viral hepatitis B

A technology for silibinin and bromine substitution, applied in the field of medicine, can solve problems such as new uses that have not been effectively developed, and achieve the effects of being conducive to large-scale production, convenient synthesis, and easy-to-obtain raw material sources.
CN101829094AInactive Publication Date: 2010-09-15DALI UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
DALI UNIV
Publication Date
2010-09-15
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to application of ring E bromine substituted silybin in preparing medicaments for treating viral hepatitis B, in particular to application of a compound of a formula (1) and a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away hepatitis B surface antigens (HBsAg) and hepatitis e antigens (HBeAg) and suppressing the HBV (Hepatitis B Virus) DNA replication. The compound has definite activity on suppressing the HBsAg and the HBeAg, and in the presence of a concentration of 100 micrograms / milliliter, the intensities of the compound for clearing away the HBsAg and the HBeAg are respectively 38.2 percent and 39.1 percent which are respectively 2.4 times and 2.3 times of that of a positive control medicament (10,000 units / milliliter of alpha-interferon). Meanwhile, in the presence of the concentration, the suppression ratio of the compound on the HBV DNA is 36 percent which is close to that of the alpha-interferon. Accordingly, the flavone lignan or the pharmaceutically acceptable salt thereof are indicated to be capable of being used for preparing non-nucleoside medicaments for clearing away the HBsAg and the HBeAg, suppressing the HBV DNA replication and treating 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 silybin ester substituted by E ring bromine or a pharmaceutically acceptable salt thereof, which is used to prepare and reduce hepatitis B virus surface antigen HBsAg and hepatitis B e antigen HBeAg, and inhibit HBV DNA Use of medicines for replicating or treating hepatitis B virus infection. This flavonoid lignan has definite activity of inhibiting HBsAg and HBeAg, and its intensity of removing HBsAg and HBeAg is respectively 38.2% and 39.1% under the concentration of 100 micrograms / ml. 2.4 times and 2.3 times; meanwhile, at this concentration, it shows a 36% inhibitory rate to HBV DNA, which is close to α-interferon. The above pharmacodynamic results show that the flavonoid lignan or its pharmaceutically acceptable salt can be expected to be used in the preparation of non-nucleoside drugs for eliminating HBsAg and HBeAg, inhibiting HBV D...

Claims

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