Objective: To undertake metabolite profiling of various plant parts of Citrullus colocynthis, and assess antioxidant and wound healing activities of fractions for therapeutical applications. Methods: Extracts from leaves, stem, root, fruit pulp and seeds were analyzed using gas chromatography-mass spectrometry and high performance liquid chromatography. Variation in antioxidant potential was assayed by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay. The extract with highest antioxidant potential was subjected on in-vivo wound healing activity using excision wound model. Results: Metabolite profiling of Citrullus colocynthis identified 70 chemically diverse metabolites from different plant parts by using a combination of GC-MS and HPLC. Concentration of colocynthin, a principal active secondary metabolite, ranged from 3.15 mg/g dry weight to 242.00 mg/g dry weight, the lowest being in leaves and highest in fruit pulp. DPPH radical scavenging activity of free radical (IC