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Original Articles

PTP1B inhibitors from Ardisia japonica

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Pages 13-18 | Received 01 May 2003, Accepted 06 May 2003, Published online: 19 Aug 2006
 

Abstract

In bioassay-directed isolation from the whole plant of Ardisia japonica, sixteen known compounds: chrysophanol (1), physcion (2), oleanolic acid (3), euscaphic acid (4), tormentic acid (5), quercetin (6), quercitrin (7), myricitrin (8), kaempferol 3-O-α-l-rhamnopyranoside (9), cyclamiretin A 3-O-α-l-rhamnopyranosyl(1→4)-β-d-glucopyranosyl(1→2)-[β-d-glucopyranosyl(1→4)]-α-l-arabinopyranoside (10), (7E)-9-hydroxymegastigma-4, 7-dien-3-on-9-O-β-d-glucopyranoside (11), bergenin (12), norbergenin (13), rutin (14), kaempferol 3,7-O-α-l-dirhamnopyranoside (15), (−)-epigallacatechin 3-O-gallate (16) were obtained. Compounds 15, 9, 11 and 1416 have not been reported previously from this plant. Among these isolates, 2, 3, 6 and 12 showed moderate bioactivity against PTP1B in vitro with IC50 values of 121.50, 23.90, 28.12 and 157 μM, respectively.

Acknowledgements

The authors thank Professor Zhong-Yin Zhang (Department of Molecular Pharmacology, Albert Einstein College of Medicine, NY, USA) for providing the plasmid of PTPIB. This work was supported by the National Natural Science Fund of China (30100229) and the Science and Technology Development Fund of Shanghai, China (01QB14051), and these supports are gratefully acknowledged.

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