Abstract
The most common cause of chronic viral hepatitis worldwide is from the Hepatitis B virus (HBV). Screening the safe and effective anti-HBV compounds in traditional Chinese medicine provides a large opportunity for the development of anti-HBV drugs. We found the ethanol extract of H. japonica had the besr inhibitory effects on HBeAg secretion from 20 species of medicinal plants In this study, silica gelSephadex LH-20. and a thin layer of chromatography were used to screen and isolate active anti-hepatitis B virus compounds from Hypericum japonica that was extracted with 60% ethanol. Four compounds were separated from the ethyl acetate extract of H•japonica and their structures were identified by spectral chemical and structural analyses. In addition, using HepG2 2.2.15 cell line with the cytotoxicity and inhibitory effecting on the secretion of HBeAg and HBsAg of the 4 isolated compounds were examined by MTT and enzyme-linked immunosorbent assays. The four isolated compounds were determined and 1,3,6,7-tetrahydroxy-9H-xanthen-9-one (Compound 4) exhibited the highest activity in inhibiting secretion of HBeAg in HepG2 2.2.15cells. The results indicated a 67.66% of inhibition rate, 40.25 μg /mL of IC50 value and TI＞2. We conducted a qualitatively evaluated research using duck hepatitis B virus model in vivo, the results indicated that ethanol extracts of H. japonica had anti-HBV effects and almost no sign of disease rebound after drug withdrawing.But the compound 4 has no direct inhibitory effect on HBV-DNA in duck experiment.
Highlights
The Hepatitis B virus (HBV) was discovered in 1966, but even after 50 years, it is still a major global public health problem[1], especially in Asian and African countries
In this Duck-Model, Beijing ducks were infected with duck hepatitis B virus (DHBV) used to evaluate antiHBV activity in this study
We conducted a qualitatively evaluated research using DHBV model in vivo, Ethanol extracts from F. dibotrys, P. saxatile and H. japonica, as well as the compound 4
Summary
The Hepatitis B virus (HBV) was discovered in 1966, but even after 50 years, it is still a major global public health problem[1], especially in Asian and African countries. A great progress is being made in the treatment of the HBV with the development of effective and well-tolerated nucleotide analogues (NAs). There are still no highly effective anti-HBV drugs to remove the HBVDNA from chronic infections completely. The clinical anti-HBV drugs have some side effects. Anti-HBV drugs of constituents from traditional Chinese herbs have some unique advantages such as high efficiency, low toxicity, and multi-target points. Screening safe and effective anti-HBV constituents in herbs is an important and necessary aspect within the research of anti-HBV drugs. We screened out four herbs within this study: (Hypericum japonica, Fagopyrum dibotrys (D.Don) Hara, Areca catechu L and Parmelia saxatile Its inhibition rate was the highest out of the four herbs that were screened
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