Momordica charantia L. has been remained a well-known medicinal vegetable used traditionally. However, which part is most effective against which disorder, has been remained undiscovered yet. The objective of this study was to examine the antimicrobial, antihyperlipidemic and antihyperglycemic activities of peel, flesh, and seeds of bitter gourd, through in vitro and in vivo assays. Ethanolic extracts from powders of three fractions of bitter gourd were assessed for antimicrobial potential against bacterial and fungal strains, whereas, powders of these fractions were used to determine antihyperlipidemic and antihyperglycemic activity, in alloxan induced diabetic rats. Our results showed that BSE exhibited better antimicrobial activity against Bacillus cereus, whereas BFE exhibited better against Escherichia coli. Blood glucose was significantly lowered by all three powders in a dose dependent manner, when fed to diabetic rats, with the highest decrease by BSP, which reduced the glucose level from 296.20 ± 2.00 mg/dl to 123.10 ± 0.80 mg/dl, at 15 mg dose, after 28 days trial. Elevated levels of TC (101.18 ± 0.65 mg/dl), TG (83.69 ± 0.61 mg/dl) and LDL–C (25.90 ± 0.09 mg/dl) in positive control rats were lowered down in well manners by BSP at 15 mg dose, to 86.30 ± 0.53, 67.70 ± 0.53 and 19.32 ± 0.06 mg/dl, respectively. As compared to BFP and BPP, BSP showed significant involvement in antibacterial, antihyperglycemic, and antihyperlipidemic actions. Along with the edible flesh, peels and seeds, which are usually discarded as waste, could also be utilized for development of pharma foods capable of promoting health.