New protein tyrosine phosphatase inhibitors from fungus <em>Aspergillus gorakhpurensis</em> F07ZB1707

RSC Adv. 2021 Mar 10;11(17):10144-10153. doi: 10.1039/d1ra00788b. eCollection 2021 Mar 5.


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 IC50 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 IC50 values in the range of 6.75-83.4 μM.

PMID:35423499 | PMC:PMC8695591 | DOI:10.1039/d1ra00788b

Source: Industry