Phytochemical study on the stem bark of P. arborescens has isolated six secondary metabolites from the crude extracts by using column chromatography, while identification was performed by using Gas Chromatography - Mass Spectrometry (GC-MS), Nuclear Magnetic Resonance (NMR) and Fourier Transform Infrared (FTIR). The isolated metabolites were identified as caryophyllene oxide (1), α-bisabolol (2), benzamide 2-(methylamino) (3), 2-ethylpiperidine (4), piperine (5) and methyl eugenol (6). Toxicity test on the four crude extracts of P. arborescens shows a high cytotoxicity against Artemia salina brine shrimp with LC50 values ranging from 13.12 to 58.70 µg/mL. Greater cytotoxicity of the crude extracts of P. arborescens indicated the presence of potent cytotoxic components in this Piper spp. Antioxidant assay of P. arborescens against 2-diphenyl-1-picrylhydrazyl (DPPH) indicated moderate antioxidant activities of methanol, dichloromethane, chloroform and hexane crude extracts with EC50 values of 21.68, 23.82, 32.88 and 36.88 µg/mL, respectively.