Biocatalytic C‑Glucosylation of Coumarins Using
an Engineered C‑Glycosyltransferase
Posted on 2018-02-22 - 18:49
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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Chen, Dawei; Chen, Ridao; Xie, Kebo; Yue, Tian; Zhang, Xiaolin; Ye, Fei; et al. (2018). Biocatalytic C‑Glucosylation of Coumarins Using
an Engineered C‑Glycosyltransferase. ACS Publications. Collection. https://doi.org/10.1021/acs.orglett.8b00378
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AUTHORS (7)
DC
Dawei Chen
RC
Ridao Chen
KX
Kebo Xie
TY
Tian Yue
XZ
Xiaolin Zhang
FY
Fei Ye
JD
Jungui Dai