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New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707.

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 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.

SUBMITTER: Ji Y

PROVIDER: S-EPMC8695591 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707.

Ji Yannan Y Zhou Qiqi Q Liu Guosheng G Zhu Tianhui T Wang Yufang Y Fu Yan Y Li Yeying Y Li Ruolan R Zhang Xuexia X Dong Mei M Sauriol Françoise F Gu Yucheng Y Shi Qingwen Q Lu Xinhua X Ni Zhiyu Z

RSC advances 20210310 17

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 sele ...[more]

PMID: 35423499

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