New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707

Yannan Ji; Qiqi Zhou; Guosheng Liu; Tianhui Zhu; Yufang Wang; Yan Fu; Yeying Li; Ruolan Li; Xuexia Zhang; Mei Dong; Françoise Sauriol; Yucheng Gu; Qingwen Shi; Xinhua Lu; Zhiyu Ni

doi:10.1039/D1RA00788B

New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707†

Yannan Ji,

^a Qiqi Zhou,

^a Guosheng Liu,

^a Tianhui Zhu,

^a Yufang Wang,^a Yan Fu,^a Yeying Li,^b Ruolan Li,^b Xuexia Zhang,^b Mei Dong,^c Françoise Sauriol,^d Yucheng Gu,

^e Qingwen Shi,

*^ac Xinhua Lu

*^b and Zhiyu Ni

*^f

Author affiliations

* Corresponding authors

^a School of Pharmaceutical Sciences, Hebei Medical University, Shijiazhuang 050017, China
E-mail: shiqingwen405@163.com

^b New Drug Research & Development Center of North China Pharmaceutical Group Corporation, National Microbial Medicine Engineering & Research Center, Hebei Industry Microbial Metabolic Engineering & Technology Research Center, Key Laboratory for New Drug Screening Technology of Shijiazhuang City, Shijiazhuang 050015, China
E-mail: luxinhua89@yeah.net

^c Hebei Key Laboratory of Forensic Medicine, Collaborative Innovation Center of Forensic Medical Molecular Identification, Hebei Medical University, Shijiazhuang 050017, China

^d Department of Chemistry, Queen's University, Kingston, Canada

^e Syngenta Jealott's Hill International Research Centre, Bracknell, Berkshire, UK

^f The Affiliated Hospital of Hebei University, School of Basic Medical Science, Hebei University, Baoding 071000, China
E-mail: nizhiyu@hbu.edu.cn

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.

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New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707†

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