Objective To study the hypoglycemic target of orientin and isoorientin and their activities in vitro.Methods The structure of diabetes-related target proteins was obtained from the www.rcsb.org database,and the binding of orientin and isorientin to diabetes-related target proteins was evaluated by virtual molecular docking score,the inhibitory effects of orientin and isoorientin on α-glucosidase,SGLT2,and PTP1B in vitro were evaluated by using 1-NBDG,PNDG and PNPP as substrates.Results The molecular docking scores of orientin with α-glucosidase,SGLT2,and PTP1B were-5.67,-9.32,and-4.75,respectively.Molecular docking scores of isoorientin with α-glucosidase,SGLT2,and PTP1B were-5.34,-8.63,and-4.93,respectively,while the molecular docking scores of positive control drug and target were-5.58,-9.79 and-9.28,respectively.The inhibition rates of orientin on α-glucosidase,SGLT2,and PTP1B were(16.7±5.8)%,(15.4±1.2)%,and(3.0±0.5)%,respectively.The inhibitory rates of isoorientin on α-glucosidase,SGLT2,and PTP1B were(11.8±3.8)%,(9.4±1.1)%,and(-3.8±0.6)%,respectively.The inhibition rates of α-glucosidase,SGLT2,and PTP1B in positive control were(63.7±5.8)%,(92.7±8.8)%,and(73.4±8.3)%,respectively.Conclusion Orientin and isorientin showed certain inhibitory activities on SGLT2 and α-glucosidase,and had little inhibitory effect on PTP1B,and oriorientin was slightly stronger than isorientin in vitro,orientin may be a potential lead compound for a class of hypoglycemic agents with dual-target effects.
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