Enzymatic transformation of esculetin as a potent class of α-glucosidase inhibitors
- Authors
- Han, Jeong G.; Cho, J.-H.; Park, K.-I.; Kim, K.; Hoon, Kim T.
- Issue Date
- May-2023
- Publisher
- Elsevier Ltd
- Keywords
- Coumarin oligomer; Enzymatic transformation; Kinetic analysis; Polyphenol oxidase; α-Glucosidase
- Citation
- Bioorganic and Medicinal Chemistry Letters, v.88
- Indexed
- SCIE
SCOPUS
- Journal Title
- Bioorganic and Medicinal Chemistry Letters
- Volume
- 88
- URI
- https://scholarworks.gnu.ac.kr/handle/sw.gnu/59358
- DOI
- 10.1016/j.bmcl.2023.129302
- ISSN
- 0960-894X
- Abstract
- 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 α-glucosidase, with IC50 values of 0.7 ± 0.1 and 2.3 ± 0.3 μM, 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. © 2023 Elsevier Ltd
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