| Summary: | Our previous study found that desmethylxanthohumol (<b>1</b>) inhibited α-glucosidase in vitro. Recently, further investigations revealed that dehydrocyclodesmethylxanthohumol (<b>2</b>) and its dimer analogue rottlerone (<b>3</b>) exhibited more potent α-glucosidase inhibitory activity than <b>1</b>. 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 <b>4d</b> and <b>5d</b> irreversibly and potently inhibited α-glucosidase (IC<sub>50</sub> = 0.22 and 0.12 μM) and moderately inhibited DPP-4 (IC<sub>50</sub> = 23.59 and 26.19 μM), respectively. In addition, compounds <b>4d</b> and <b>5d</b> significantly promoted glucose consumption, with the activity of <b>5d</b> at 0.2 μM being comparable to that of metformin at a concentration of 1 mM.
|
|---|