期刊
ORGANIC LETTERS
卷 20, 期 6, 页码 1634-1637出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b00378
关键词
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资金
- National Science Foundation of China [81703369, 21572277]
- CAMS Innovation Fund for Medical Sciences [CIFMS-2016-I2M-3-012]
The enzymatic synthesis of coumarin C-glucosides by an engineered C-glycosyltransferase, MiCGTb-GAGM, was explored in vitro and in vivo. MiCGTb-GAGM exhibited a robust C-glucosylation capability toward structurally diverse coumarin derivatives. The whole-cell bioconversion of MiCGTb-GAGM was exploited for large-scale production of coumarin C-glucosides. Two C-glucosides exhibited potent SGLT2 inhibitory activities with IC50 values at 10(-6) M. These findings provide cost-effective and practical synthetic strategies to generate structurally diverse and novel bioactive coumarin C-glycosides for drug discovery.
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