Objective: The study was undertaken to isolate biologically active compounds from Goniothalamus gardineri, a plant endemic to Sri Lanka. Methods: Roots and flowers of Goniothalamus gardineri were extracted into dichloromethane and methanol. A new acetogenin, gardinerin isolated by column chromatography of the dichloromethane extract was structurally characterized using NMR and Mass spectroscopies. It was found to be mosquito larvicidal (against 2nd instar larvae of Aedes aegypti), cytotoxic (in the brine shrimp assay) and antioxidant (DPPH assay). Results: Gardinerin exhibited potent mosquitolarvicidal activity (LC50 = 0.0744±0.37 ppm.), cytotoxicity (LC50 = 1.5±0.37 ppm) and antioxidant activity (IC50 =10.02±0.01 ppm). The same extract furnished (5R)-goniothalamin. The hexane extract of the flowers of G. gardineri yielded poriferesterol and stigmast-4, 22-dien-3-one.Conclusion: The endemic plant G. gardineri has yielded an acetogenin possessing highly potent antioxidant, cytotoxic and mosquitolarvicidal activity. Â