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Cembrane diterpenoids from the soft coral Sarcophyton trocheliophorum Marenzeller as a new class of PTP1B inhibitors.

Abstract：

:A detailed investigation of the South China Sea soft coral Sarcophyton trocheliophorum Marenzeller yielded, along with six known terpenes (6-11), the new sarcophytonolides N-R (1-5), whose structures have been elucidated by detailed spectroscopic analysis. Sarcophytonolides N-R are mono- or bicyclic cembranoids characterized by the presence of three/four double bonds and oxidized methyl groups. Some of the isolated compounds showed significant inhibitory activity against human protein tyrosine phosphatase 1B (PTP1B) enzyme, a key target for the treatment of type-II diabetes and obesity, and some preliminary structure-activity relationships have been drawn. This is the first report on the anti-PTP1B activity of cembrane diterpenoids.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Liang LF,Gao LX,Li J,Taglialatela-Scafati O,Guo YW

doi

10.1016/j.bmc.2013.06.043

subject

Has Abstract

pub_date

2013-09-01 00:00:00

pages

5076-80

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00574-9

journal_volume

21

pub_type

杂志文章

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