Department of Biosynthetic Medicinal Chemistry,
School of Pharmaceutical Sciences, Fudan
University, Shanghai 200032, PR China.
Abstract
Natural products provide a large reservoir of
potentially active agents with anti-hepatitis B
virus (HBV) activity. We examined the effect of
the polyphenolic extract from Geranium
carolinianum L. (PPGC) on HBV replication both in
vitro and in vivo. In the human HBV-transfected
liver cell line HepG(2) 2.2.15, PPGC effectively
suppressed the secretion of the HBV antigens in a
dose-dependent manner with IC(50) values of 46.85
microg/ml for HBsAg and 65.60 microg/ml for HBeAg
at day 9. Consistent with the HBV antigen
reduction, PPGC (100 microg/ml) also reduced HBV
DNA level by 35.9%. In the duck hepatitis B virus
(DHBV) infected ducks, after PPGC was dosed
intragastricly (i.g.) once a day for 10 days, the
plasma DHBV DNA level was reduced, with an ED(50)
value of 47.54 mg/kg. In addition, Southern blot
analysis confirmed the in vivo anti-HBV effect of
PPGC in ducks and PPGC also reduced the plasma
and the liver DHBV DNA level in a dose-dependent
manner. Furthermore, significant improvement of
the liver was observed after PPGC treatment, as
evaluated by the histopathological analysis.
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