期刊
PHYTOCHEMISTRY
卷 170, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2019.112224
关键词
Aspergillus deflectus Fennell & Raper; Moniliaceae; Azaphilones; Deflectin-type; Protein tyrosine phosphatase inhibitor
资金
- National Natural Science Foundation of China [81872770]
- Foundation of Education Department, Hebei Province [ZD2018088]
Six undescribed azaphilones, deflectins C1-C3, deflectins D1-D2, and deflectin E, along with five known azaphilones were obtained from a solid culture of the wild fungus Aspergillus deflectus NCC0415. Their structures were determined by HRESIMS, NMR and ECD analyses, together with the GIAO C-13 NMR calculation method. All compounds displayed strong or moderate inhibitory activity against protein tyrosine phosphatases SHP2 and PTP1B. Structure-activity relationship analysis of these azaphilones suggested that the length of the ketone aliphatic side chain would affect their SHP2 and PTP1B inhibitory activity. In addition, the presence of a Delta(8(12)) double bond on gamma-lactone ring and the presence of CH3-2' in fatty chains may increase their inhibitory activity.
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