Ai-Xue Zuo

Anti‐Hepatitis B Virus Active Lactones from the Traditional Chinese Herb: Swertia mileensis

Swerilactones H-K (1-4), which are four novel lactones with an unprecedented C29 skeleton, were isolated from Swertia mileensis (Qing-Ye-Dan), an endemic Chinese herb used for treating viral hepatitis. Their structures were determined by extensive spectroscopic and X-ray crystallographic diffraction analyses. Swerilactones H-K exhibit potent anti-hepatitis B virus activity against HBV DNA replication with IC(50) values ranging from 1.53 to 5.34 μM. For the first time, a plausible biogenetic pathway for swerilactones H-K, together with the previously reported swerilactones A-D is proposed. From a biogenetic point of view, swerilactones A-D are ascribed as secoiridoid dimers, and swerilactones H-K as secoiridoid trimers.

Swerilactones A and B, Anti-HBV New Lactones from a Tradtional Chinese Herb: Swertia mileensis as a Treatment for Viral Hepatitis

Swerilactones A (1) and B (2), two novel lactones with an unprecedented 6/6/6/6/6 pentacyclic ring system, were isolated from the traditional Chinese herb of Swertia mileensis with activity against the hepatitis virus. Their structures and relative stereochemistry were elucidated based on spectroscopic methods and further confirmed by X-ray single crystal diffraction analysis. In vitro antihepatitis B virus (HBV) assay on Hep G 2.2.15 cell line showed that compound 1 inhibited HBsAg and HBeAg secretion with IC(50) values of 3.66 and 3.58 mM, respectively.

Swerilactones C and D, anti-HBV New Lactones from a Traditional Chinese Herb: Swertia mileensis

Swerilactones C (1) and D (2), two novel diastereomeric lactones with an unprecedented 6/6/6/6/6 pentacyclic ring system, were isolated from the traditional Chinese herb Swertia mileensis. Their structures and relative stereochemistry were elucidated on the basis of spectroscopic methods and further confirmed by X-ray single-crystal diffraction analysis. In vitro antihepatitis B virus (HBV) assay on the Hep G 2.2.15 cell line showed that both compounds 1 and 2 exhibited inhibitory activities against the secretion of HBsAg (IC(50) = 1.24 and 2.96 mM, respectively) and HBeAg (IC(50) = 0.77 and 1.47 mM, respectively).

Three new phenolic glycosides from Curculigo orchioides G.

Three new phenolic glycosides, curculigosides F-H (1-3), were isolated from rhizomes of Curculigo orchioides Gaertn. Their structures were elucidated based on comprehensive spectroscopic analyses including IR, MS, 1D- and 2D NMR (HSQC, COSY, and HMBC). Curculigosides F-H (1-3) were evaluated for their anti-HBV activity in vitro using the HBV transfected Hep G2.2.15 cell line. Compound 1 exhibited weak activity with an IC(50) value of 2.08 mM on hepatitis B virus (HBV) e antigen (HBeAg) secretion of the HepG2.2.15 cell line.

Four new trace phenolic glycosides from Curculigo orchioides

Four new trace phenolic glycosides named orcinosides D (1), E (2), F (3), and G (4) were isolated from the rhizomes of Curculigo orchioides Gaertn. Based on comprehensive spectroscopic analyses including IR, FAB-MS, HR-ESI-MS, 1D- and 2D NMR (HSQC, HMBC), their structures were elucidated as orcinol-1-O-β-d-xylopyranoside (1), orcinol-1-O-β-d-apiofuranosyl-(1 → 2)-β-d-glucopyranoside (2), orcinol-3-O-β-d-apiofuranosyl-1-O-β-d-glucopyranoside (3), and 1-O-β-d-glucopyranosyl-4-ethoxyl-3-hydroxymethylphenol (4).

New phenolic glycosides from Curculigo orchioides and their xanthine oxidase inhibitory activities

Seven new phenolic glycosides including two heterocyclic phenolic derivatives orcinosides I-J (1-2) and five chlorophenolic glycosides curculigines J-N (3-7), together with nineteen known compounds were isolated from the rhizome of Curculigo orchioides. Based on extensive spectroscopic analyses (UV, IR, HRESIMS, 1D and 2D NMR), the structures of the new compounds were identified. Orcinoside I (1) and J (2) displayed xanthine oxidase inhibitory activities with IC50 values 0.25 and 0.62mM respectively.