| Literature DB >> 33672038 |
Yinan Zhang1, Haibo Wang1, Yan Wu1, Xue Zhao1, Zhihong Yan1, Robert H Dodd1,2, Peng Yu1, Kui Lu1, Hua Sun1.
Abstract
Our previous study found that desmethylxanthohumol (1) inhibited α-glucosidase in vitro. Recently, further investigations revealed that dehydrocyclodesmethylxanthohumol (2) and its dimer analogue rottlerone (3) exhibited more potent α-glucosidase inhibitory activity than 1. The aim of this study was to synthesize a series of rottlerone analogues and evaluate their α-glucosidase and DPP-4 dual inhibitory activity. The results showed that compounds 4d and 5d irreversibly and potently inhibited α-glucosidase (IC50 = 0.22 and 0.12 μM) and moderately inhibited DPP-4 (IC50 = 23.59 and 26.19 μM), respectively. In addition, compounds 4d and 5d significantly promoted glucose consumption, with the activity of 5d at 0.2 μM being comparable to that of metformin at a concentration of 1 mM.Entities:
Keywords: DPP-4 inhibitor; glucose consumption; inhibitory mechanism; rottlerone; α-glucosidase inhibitor
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Year: 2021 PMID： 33672038 PMCID： PMC7919492 DOI： 10.3390/molecules26041024
Source DB: PubMed Journal: Molecules ISSN： 1420-3049 Impact factor: 4.411