New protein tyrosine phosphatase inhibitors from fungus F07ZB1707

Twelve new compounds, aspergorakhins A-L ( 1-12 ) coupled with one known xanthone leptosphaerin D ( 13 ), were isolated from the extract of soil-derived fungus Aspergillus gorakhpurensis F07ZB1707. Their structures were elucidated by spectroscopic data analysis including UV, IR, NMR, and HRESIMS. The absolute configurations of 5 and 8-11 were identified using ECD and OR calculations. All compounds were tested by enzyme inhibitory activity assay in vitro . Aspergorakhin A ( 1 ) showed selective activities against PTP1B and SHP1 over TCPTP with IC 50 values 0.57, 1.19, and 22.97 μM, respectively. Compounds 1 and 2 exhibited modest cytotoxicity against tumor cell lines A549, HeLa, Bel-7402, and SMMC-7721 with IC 50 values in the range of 6.75-83.4 μM. Twelve novel metabolites were isolated from Aspergillus gorakhpurensis F07ZB1707. Aspergorakhin A ( 1 ) showed selective activities against PTP1B and SHP1 over TCPTP with IC 50 values of 0.57, 1.19, and 22.97 μM, respectively.