New preaustinoids from a marine-derived fungal strain Penicillium sp. SF-5497 and their inhibitory effects against PTP1B activity.

Authors :: Park JS
Quang TH
Thi Thanh Ngan N
Sohn JH
Oh H
Source :: The Journal of antibiotics [J Antibiot (Tokyo)] 2019 Aug; Vol. 72 (8), pp. 629-633. Date of Electronic Publication: 2019 Apr 24.
Publication Year :: 2019
Abstract: Chemical investigation of the marine-derived fungal isolate Penicillium sp. SF-5497 resulted in the isolation of two new preaustinoid-related meroterpenoids, named preaustinoid A6 (1) and preaustinoid A7 (2), along with three known metabolites (3-5). Their structures were elucidated by extensive spectroscopic analyses, such as 1D and 2D NMR and MS data. Among these, compounds 1 and 3 inhibited PTP1B activity in a dose-dependent manner, with IC <subscript>50</subscript> values of 17.6 and 58.4 µM, respectively. Furthermore, kinetic analyses indicated that compound 1 inhibited PTP1B in a noncompetitive manner, with the K <subscript>i</subscript> value of 17.0 µM.

Subjects :: Dose-Response Relationship, Drug
Humans
Models, Molecular
Molecular Structure
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Penicillium chemistry
Protein Tyrosine Phosphatase, Non-Receptor Type 1 antagonists & inhibitors
Terpenes chemistry
Terpenes pharmacology

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