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Ruellia tuberosa  L. is a folk remedy in the treatment of diabetes mellitus. However, its hypoglycemic activity has not been investigated so far. In the present study, the antidiabetic mechanism of the n-hexane fraction of methanolic extract (HFME) of this plant was investigated  in silico ,  in vitro , and  in vivo .  In silico  study was performed using AutoDock4.2 software.  In vitro     α -amylase inhibitory activity was investigated by starch-iodine method. A single dose of 450 mg/kg HFME for 14 days was subjected to an antidiabetic screening  in vivo  by a multiple low dose streptozotocin (MLD-STZ) induced rats. Molecular modeling results show that Betulin exhibited noncompetitive  α -amylase inhibitory activities. The effect of HFME elicited significant reductions of diabetic rat blood glucose. A single dose administration of HFME inhibited  α -amylase activity  in vivo  ( P  < 0.01) compared to a diabetic control group. Moreover, this extract strongly inhibited the  α -amylase activity  in vitro  (IC 50  0.14 ± 0.005 mg/mL). It is concluded that HFME exerted an antidiabetic effect via  α -amylase inhibitor. Our findings provide a possible hypoglycemic action of  R. tuberosa  L. as an alternative therapy in the management of diabetes.

Antidiabetic Activity ofRuellia tuberosaL., Role ofα-Amylase Inhibitor:In Silico,In Vitro, andIn VivoApproaches