PTP1B inhibitors from Saussrurea Lappa

Abstract

A new lignan glycoside, named 1,5-dihydroxypinoresinol-4′-O-β-d-glucopyranoside (1), has been isolated from the EtOH extract of the roots of Saussurea lappa, together with twenty known compounds: (+)-1-hydroxypinoresinol-1-O-β-d-glucopyranoside (2), fraxiresinol-4′-O-β-d-glucopyranoside (3), ( − )-olivil-4″-O-β-d-glucopyranoside (4), 4-allyl-2,6-dimethoxybenzene-1-O-β-d-glucopyranoside, syringin, costunolide-15-O-β-d-glucopyranoside, chlorogenic acid, aloe-emodin-8-O-β-d-glucopyranoside (5), rhein-8-O-β-d-glucopyranoside (6), chrysophanol (7), emodin, dehydrocostus lactone, costunolide, β-costic acid, reynosin, arbusculin A, α-cyclocostunolide, β-cyclocostunolide, santamarine and magnolialide. Three anthraquinones (5–7) showed moderate bioactivity against human Protein Tyrosine Phosphatase 1B (hPTP1B) in vitro.

Keywords:

• Saussurea lappa
• PTP1B inhibitors
• 1,5-Dihydroxypinoresinol-4′-O-β-d-glucopyranoside

Acknowledgements

The authors gratefully acknowledge the support of this work by the National Natural Science Foundation (30100229) and the Technology Development Fund of Shanghai, China (01QB14051).