Diabetes mellitus is a lethal metabolic disorder in humankind, which induce chronic complications. The present study investigated the effects of ethyl acetate extract from C. procera (EAE) and its isolates on antioxidant and in vitro antidiabetic activities, along with effects of EAE on plasma blood glucose concentrations in STZ-diabetic rats. For the first time, two known metabolites- N-((2S,3R,E)-1,3-dihydroxyoctadec-4-en-2-yl)stearamide (1) and N-((2S,3R,4E,8E)-1,3-dihydroxyoctadeca-4,8-dien-2-yl)palmitamide (2) are reported from EAE. 1, 2 and EAE depicted significant DPPH, superoxide free radicals, α-glucosidase and α-amylase inhibitory profile, indeed, 1 and 2 showed mild inhibitory profile against aldose reductase. In addition, the EAE (200 mg/kg b.w) revealed significant reduction in plasma glucose, body weight, total cholesterol, total glycerides and LDL levels in STZ-induced diabetic rats. The HDL levels were markedly augmented in EAE treated diabetic rats, when compared with control group. EAE abolished the increased lipid peroxidation in pancreas, liver and kidneys. The histopathological examination of pancreas of EAE protected the Langerhans islets with the number of islet cells were found statistically significant, when compared to diabetic control pancreas. Our data suggest that the C. procera has a potentiality to act against diabetes (both, in vitro and in vivo models) by inhibiting particularly digestive enzymes namely α-glucosidase and α-amylase, however further studies are required for proper establishment of mechanism of action and validating clinical effects.