Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 88, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2023.129302
Keywords
Enzymatic transformation; Polyphenol oxidase; Coumarin oligomer; alpha-Glucosidase; Kinetic analysis
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This study demonstrates a rapid and simple enzymatic transformation of the coumarin esculetin using polyphenol oxidase derived from Agaricus bisporus. Five new oxidized metabolites, esculetinins A-E, were produced along with a known compound isoeuphorbetin. The esculetin oligomers 2 and 3 showed significantly enhanced inhibitory activities against α-glucosidase with competitive modes of action.
A rapid and simple enzymatic transformation of the representative coumarin esculetin (1) with polyphenol oxidase originating from Agaricus bisporus afforded five new oxidized metabolites, esculetinins A (2), B (3), C (4), D (5), and E (6), together with the known compound isoeuphorbetin (7). The structures of the oligomerized transformation products were established on the basis of spectroscopic interpretations. The esculetin oligomers 2 and 3 revealed highly enhanced inhibitory activities against a-glucosidase, with IC50 values of 0.7 +/- 0.1 and 2.3 +/- 0.3 mu M, respectively, as compared to the original esculetin. Kinetic analysis also exhibited that the two new potent metabolites 2 and 3 have competitive modes of action.
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