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Verruculides A and B, two new protein tyrosine phosphatase 1B inhibitors from an Indonesian ascidian-derived Penicillium verruculosum.

Abstract：

:Two new merosesquiterpenes, verruculides A (1) and B (2), were isolated from a culture broth of the Indonesian ascidian-derived Penicillium verruculosum TPU1311, together with three known congeners, chrodrimanins A (3), B (4), and H (5). The structures of 1 and 2 were assigned on the basis of their spectroscopic data (1D and 2D NMR, HRMS, UV, CD, and IR). Compound 2 had a linear sesquiterpene moiety and was considered to be the derivative of the biosynthetic precursor for 1 and 3-5. Compounds 1, 3, and 5 inhibited the activity of protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 8.4, 8.5, and 14.9 μM, respectively. Compound 2 showed 40% inhibition at 23.1 μM, while 4 was not active at 20.7 μM.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yamazaki H,Nakayama W,Takahashi O,Kirikoshi R,Izumikawa Y,Iwasaki K,Toraiwa K,Ukai K,Rotinsulu H,Wewengkang DS,Sumilat DA,Mangindaan RE,Namikoshi M

doi

10.1016/j.bmcl.2015.06.026

subject

Has Abstract

pub_date

2015-08-15 00:00:00

pages

3087-90

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00619-8

journal_volume

25

pub_type

杂志文章

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