Anti-hepatitis B virus active constituents from Swertia chirayita

摘要

Four new compounds swerdachiralatone A (1), swertiachoside A (2), swertiachirdiol A (3) and swertiachoside B (4), together with twenty-six known ones were isolated from the ethanol extract of Swertia chirayita. Their structures were elucidated by extensive spectroscopic analyses (1D- and 2D-NMR, HRESIMS, UV, IR and [alpha](D)). All compounds were evaluated for anti-hepatitis B virus (anti-HBV) activities on HepG 2.2.15 cells line in vitro, of which compounds 14 and 19 showed inhibitory activity on hepatitis B surface antigen (HBsAg) secretion with IC50 values of 031 +/- 0.045 and 1.49 +/- 0.033 mM; compounds 14 and 28 exhibited activity against hepatitis Be antigen (HBeAg) secretion with IC50 values of 0.77 +/- 0.076 and 5.92 +/- 1.02 mM; and eight compounds (8,9,13,14,24-26,29) possessed activity against HBV DNA replication with IC50 values of 0.07-033 mM. In particular (+)-cycloolivil-4'-O-beta-D-glucopyranoside (14) exhibited inhibition not only on the secretions of HBsAg and HBeAg with IC50 values of 031 +/- 0.045 mM (SI = 4.29) and 0.77 +/- 0.076 mM (SI = 1.75), respectively, but also on HBV DNA replication with an IC50 value of 029 +/- 0.034 mM (SI = 4.66). (C) 2014 Elsevier B.V. All rights reserved.