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Background: Cardiovascular diseases and diabetes are responsible for large number of deaths throughout the globe. Bitter gourd has the potential to become a component of the diet or a dietary supplement for diabetic and pre-diabetic patients owing to the presence of insulin like molecules. Recent investigations have suggested that bitter gourd extracts may ameliorate high fat diet induced obesity and hyperlipidemia in animal models. Moreover, its supplements in food result in lowering weight gain and visceral fat mass. Methods: The current study was designed to investigate the nutraceutical potential of skin, flesh and whole fruit of bitter gourd cultivars against hyperglycemia and hyperlipidemia. For the purpose, various bitter gourd cultivars were procured from local market. Bio-evaluation studies were carried out on biochemical parameters using rodent experiment model. Results: From results, it was revealed that maximum reduction in blood glucose skin 1.06%, flesh 2.65%, whole fruit 4.29%, total cholesterol skin 6.60%, flesh 6.04%, whole fruit 6.70%, low density lipoprotein skin 5.55%, flesh 6.81%, whole fruit 6.60%, and triglycerides skin 0.04%, flesh 3.38%, whole fruit 2.02%, were observed. Moreover, insulin skin 2.14%, flesh 3.52%, whole fruit 2.73%, production was slightly enhanced with improved levels of high density lipoprotein in whole fruit of bitter gourd. Conclusion: Overwhelmingly, it may be inferred here that bitter gourd holds the potential to significantly improve diabetic conditions and associated late complications with no ill effects on body organs. [ABSTRACT FROM AUTHOR]