New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707
| Autor: | Li Yeying, Tian-Hui Zhu, Yu-Cheng Gu, Ruolan Li, Mei Dong, Xinhua Lu, Yan-Nan Ji, Yufang Wang, Qing-Wen Shi, Xuexia Zhang, Guosheng Liu, Yan Fu, Qiqi Zhou, Francoise Sauriol, Zhiyu Ni |
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| Rok vydání: | 2021 |
| Předmět: |
biology
010405 organic chemistry General Chemical Engineering General Chemistry Aspergillus gorakhpurensis Fungus Protein tyrosine phosphatase biology.organism_classification 01 natural sciences In vitro 0104 chemical sciences HeLa 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Biochemistry Xanthone Ic50 values Cytotoxicity |
| Zdroj: | RSC Advances. 11:10144-10153 |
| ISSN: | 2046-2069 |
| DOI: | 10.1039/d1ra00788b |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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