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The chemical composition and biological activities of the essential oil from Ficus tikoua Bur. were reported for the first time. Fifty-three compounds, accounting for 99.60% of the total essential oil composition, were identified and the main components were palmitic acid (51.13%) and linoleic acid (47.54%). The essential oil revealed significant antibacterial activity with the inhibition zones (7.89-10.59 mm), MIC (0.20-6.25 mg/mL) and MBC (0.20-12.50 mg/mL) against Staphylococcus aureus, Bacillus subtilis, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa and Proteus vulgaris. The essential oil exhibited significant cytotoxicity against A549, NCI-H1299, PC-3 and K562 tumor cells with the IC50 values of 131.08, 50.32, 120.58 and 31.68 µg/mL, respectively. The essential oil exhibited selective cytotoxic activity to human tumor cell lines, with a significantly lower cytotoxicity to human normal cell line (MRC-5, IC50 = 161.75 µg/mL) than to tumor cells. Additionally, palmitic acid, as the major compound, aslo revealed significant antibacterial and cytotoxic activities. [ABSTRACT FROM AUTHOR]