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Piliostigma malabaricum is used in traditional herbal remedies for diseases which informed this research to probe its leaf and flower constituents using gas chromatography-mass spectrometry technique. Twenty-two constituents were observed in each of the leaf and flower extracts. The leaf contained fatty acids (79.32%), hydrocarbons (6.63%), aldehyde (3.78%), amide (2.91%), ester (2.36%), alkaloids (1.72%), phosphate ester (1.27%), cyclic ether (1.04%) and alcohol (0.98%). The flower contained fatty acids (81.54%), ester (5.79%), alkaloids (3.62%), aldehyde (3.01%), hydrocarbons (2.44%), amide (2.17%), ketone (1.28%) and alcohol (0.15%). The extracts inhibited the growth of Escherichia coli and Staphylococcus aureus and the extent of inhibitions was comparable to that of gentamycin used as a standard antibacterial agent. The flower extract proved to be a more potent antibacterial than the leaf extract. This research provides evidence for P. malabaricum application in traditional herbal practices.