期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 54, 期 43, 页码 12678-12682出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201506505
关键词
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资金
- National Natural Science Foundation of China [81273405]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing, China [2012X09301002-001-005]
The catalytic promiscuity of the novel benzophenone C-glycosyltransferase, MiCGT, which is involved in the biosynthesis of mangiferin from Mangifera indica, was explored. MiCGT exhibited a robust capability to regio- and stereospecific C-glycosylation of 35 structurally diverse druglike scaffolds and simple phenolics with UDP-glucose, and also formed O- and N-glycosides. Moreover, MiCGT was able to generate C-xylosides with UDP-xylose. The OGT-reversibility of MiCGT was also exploited to generate C-glucosides with simple sugar donor. Three aryl-C-glycosides exhibited potent SGLT2 inhibitory activities with IC50 values of 2.6 x, 7.6 x, and 7.6 x 10(-7) M, respectively. These findings demonstrate for the first time the significant potential of an enzymatic approach to diversification through C-glycosidation of bioactive natural and unnatural products in drug discovery.
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