Xanthones with Anti-Hepatitis B Virus Activity from Swertia mussotii

Abstract

Two new xanthones, 8-O-β-D-glucopyranosyl-1-hydroxy-2,3,5-trimethoxyxanthone (1) and 8-O-[β-D-xylopyranosyl-(1 → 6)-β-D-glucopyranosyl]-1-hydroxy-2,3,5-trimethoxyxanthone (2), along with eighteen known xanthones (3–20) were isolated from Swertia mussotii. Their structures were elucidated on the basis of extensive spectroscopic analyses (1D- and 2D-NMR, HRESIMS, UV, IR, [α]_D). All compounds were evaluated for their anti-hepatitis B virus activities on HepG 2.2.15 cells line in vitro, and compounds 3–10 exhibited significant activity inhibiting hepatitis B virus DNA replication with IC₅₀ values from 0.01 mM to 0.13 mM. Compounds 3–5 showed remarkable activity with IC₅₀ values of 0.77, > 0.98, and 0.21 mM for HBsAg, and < 0.62, 0.35, and 0.04 mM for HBeAg, respectively. Meanwhile, the effects of different substitutions on the anti-hepatitis B virus activity of xanthones from S. mussotii were discussed.

Key words

Swertia mussotii - Gentianaceae - xanthones - anti-HBV activity

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