New protein tyrosine phosphatase inhibitors from fungusAspergillus gorakhpurensisF07ZB1707

Abstract

Twelve new compounds, aspergorakhins A-L (1-12) coupled with one known xanthone leptosphaerin D (13), were isolated from the extract of soil-derived fungusAspergillus gorakhpurensisF07ZB1707. Their structures were elucidated by spectroscopic data analysis including UV, IR, NMR, and HRESIMS. The absolute configurations of5and8-11were identified using ECD and OR calculations. All compounds were tested by enzyme inhibitory activity assayin vitro. Aspergorakhin A (1) showed selective activities against PTP1B and SHP1 over TCPTP with IC50values 0.57, 1.19, and 22.97 μM, respectively. Compounds1and2exhibited modest cytotoxicity against tumor cell lines A549, HeLa, Bel-7402, and SMMC-7721 with IC50values in the range of 6.75-83.4 μM.