The objective of this study was to profile the chemical components and biological activity analysis of crude extract of Bryophyllum pinnatum and Oxalis corniculata. Results revealed that the analyzed plant materials encompass the high amount of total phenolic and flavonoids content and have significant antioxidant activities. Furthermore, methanol extracts are the potential source of α‐amylase, α‐glucosidase, lipase, tyrosinase and elastase inhibitors. High resolution mass spectrometry revealed the presence of diverse metabolites such as quercetin 3‐O‐α‐L‐rhamnopyranoside, myricetin 3‐rhamnoside, bersaldegenin 1,3,5‐orthoacetate, bryophyllin C, syringic acid, caffeic acid, p‐coumaric acid, and quercetin in B. pinnatum and isoorientin, swertisin, apigenin 7,4′‐diglucoside, vitexin, 4‐hydroxybenzoic acid, vanillic acid, ethyl gallate, 3,3′,4′‐trihydroxy‐5,7‐dimethoxyflavone, and diosmetin‐7‐O‐β‐D‐glucopyranoside in O. corniculata. Our finding suggested that these two plant species have high medicinal importance and are potential source of inhibitors for modern pharmaceuticals, nutraceuticals and cosmetics industries.