Journal
MOLECULES
Volume 25, Issue 11, Pages -Publisher
MDPI
DOI: 10.3390/molecules25112572
Keywords
Agrimonia pilosa L; alpha-glucosidase inhibitory activity; isocoumarin; flavonoid; structure-activity relationship; industrial source
Funding
- National Research Foundation of Korea (NRF) - Korean government (MEST) [NRF-2015R1D1A3A01020708]
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Agrimonia pilosa L. (AP) showed potent alpha -glucosidase inhibitory (AGI) activity, but it is uncertain what phytochemicals play a key factor. The phytochemical study of AP based on AGI activity led to the isolation of four isocoumarins; agrimonolide (1), agrimonolide-6-O-beta -d-glucopyranoside (2), desmethylagrimonolide (3), desmethylagrimonolide-6-O-beta -d-glucopyranoside (4), and four flavonoids; luteolin (5), quercetin (6), vitexin (7), and isovitexin (8). The four isocoumarins were isolated as alpha -glucosidase inhibitors for the first time. Isocoumarins, compound 1 (agrimonolide) and 3 (desmethylagrimonolide) showed strong alpha -glucosidase inhibitory activities with IC50 values of 24.2 and 37.4 mu M, respectively. Meanwhile, isocoumarin and flavonoid glycosides showed weak AGI activity. In the kinetic analysis, isocoumarins, compounds 1 and 3 showed non-competitive inhibition, whereas flavonoid, compound 6 showed competitive inhibition.
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