<p>The phytochemical investigation of chloroform extract from <i>Piper betle</i> var. <i>haldia</i>, Piperaceae, leaves has resulted in the isolation of two new chemical constituents which were identified as 1-<i>n</i>-dodecanyloxy resorcinol (<b>H1</b>) and desmethylenesqualenyl deoxy-cepharadione-A (<b>H4</b>), on the basis of spectroscopic data 1D NMR (<sup>1</sup>H and <sup>13</sup>C) and 2D NMR (<sup>1</sup>H-<sup>1</sup>H COSY and HMBC) as well as ESI-MS, FT-IR and HR-ESI-MS analyses. Compounds <b>H1</b> and <b>H4</b> showed excellent antioxidant DPPH free radical scavenging activity with IC<sub>50</sub> values of 7.14 μg/mL and 8.08 μg/mL compared to ascorbic acid as a standard antioxidant drug with IC<sub>50</sub> value of 2.52 μg/mL, respectively. Evaluation of cytotoxic activity against human hepatoma cell line (PLC-PRF-5) showed moderate effect with the GI<sub>50</sub> values of 35.12 μg/mL for <b>H1</b>, 31.01 μg/mL for <b>H4</b>, compared to Doxorubicin<sup>®</sup> as a standard cytotoxic drug with GI<sub>50</sub> value of 18.80 μg/mL.</p
