The essential oils (EOs) from leaves, stems, and whole plant of Piper boehmeriifolium were analyzed using GC/FID and GC/MS. The main constituents of P. boehmeriifolium EOs were β -caryophyllene, caryophyllene oxide, β -elemene, spathulenol, germacrene D, β -selinene, and neointermedeol. The antioxidant potential of the EOs were determined using DPPH • , ABTS •+ and FRAP assays. In ABTS •+ assay, the leaf oil exhibited a remarkable activity with an IC 50 value of 7.36 μg/mL almost similar to BHT (4.06 μg/mL). Furthermore, the antibacterial activity of the oils as well as their synergistic potential with conventional antibiotics were evaluated using microdilution and Checkerboard assays. The results revealed that the oils from different parts of P. boehmeriifolium inhibited the growth of all tested bacteria and the minimum inhibitory concentrations were determined to be 0.078-1.250 mg/mL. In combination with Chloramphenicol or Streptomycin, the oils showed significant synergistic antibacterial effects in most cases. Besides, the results of MTT assay indicated that the oil of the whole plant exhibited significant cytotoxic activities on human hepatocellular carcinoma cells (HepG2) and human breast cancer cells (MCF-7). In summary, the P. boehmeriifolium oils could be regarded as a prospective source for pharmacologically active compounds.