New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis 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 ab...

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Detalles Bibliográficos
Autores principales: Ji, Yannan, Zhou, Qiqi, Liu, Guosheng, Zhu, Tianhui, Wang, Yufang, Fu, Yan, Li, Yeying, Li, Ruolan, Zhang, Xuexia, Dong, Mei, Sauriol, Françoise, Gu, Yucheng, Shi, Qingwen, Lu, Xinhua, Ni, Zhiyu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8695591/
https://www.ncbi.nlm.nih.gov/pubmed/35423499
http://dx.doi.org/10.1039/d1ra00788b
Descripción
Sumario: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.

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