title: 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.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, PR China.
authors.forename: Tuan-Wu
authors.initials: TW
authors.lastname: Cao
authors.forename: Chang-An
authors.initials: CA
authors.lastname: Geng
authors.forename: Yun-Bao
authors.initials: YB
authors.lastname: Ma
authors.forename: Kang
authors.initials: K
authors.lastname: He
authors.forename: Hong-Ling
authors.initials: HL
authors.lastname: Wang
authors.forename: Ning-Jia
authors.initials: NJ
authors.lastname: Zhou
authors.forename: Xue-Mei
authors.initials: XM
authors.lastname: Zhang
authors.forename: Yan-Duo
authors.initials: YD
authors.lastname: Tao
authors.forename: Ji-Jun
authors.initials: JJ
authors.lastname: Chen
mesh_terms: D000998:Antiviral Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002460:Cell Line; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D013057:Spectrum Analysis; D029967:Swertia / Q000737:chemistry*; D044004:Xanthones / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D044004:Xanthones