Abstract: The aim of this study was to evaluate the antioxidant and anticancer activities of lignans from Cinnamomum camphora leaves. Response surface methodology (RSM) was used to optimize ultrasonic wave assisted extraction of lignans based on single factor tests and establish the corresponding mathematical model. The lignans were separated and purified by the steps of concentration, extraction, chromatography-spectrum and so on. The structure was identified by ultraviolet chromatography, infrared spectroscopy, mass spectrometry and nuclear magnetia resonance.The purity of the compounds was determined using HPLC technique and they were used for further experiments. The antioxidant activity of lignans was studied in vitro by scavenging activity against DPPH· and ·OH. The effects of lignans on HepG2 liver cancer cells and human umbilical vein endothelial cell (HUVEC) were compared by MTS assay. The results were as follows: Liquid-to-solid ratio 1cells and human umbilical vein endothelial cell (HUVEC) were compared by MTS assay. The results were as follows: Liquid-to-solid ratio 1:22 g/mL, ultrasonic time 3 min, ethanol concentration 60% and extraction time 78 min, the yield of lignans was 45.31 mg/g. The purity of sesamin and pinoresinol-β-D-glucaside was 94.84%, 90.14% respectively. And the lignans had strong scavenging activity against DPPH· and·OH. Among them, the half inhibitory concentration(IC₅₀) of pinoresinol-β-D-glucaside for scavenging DPPH free radical and hydroxyl free radical was 0.31 mg/mL and 0.71 mg/mL, respectively; the IC₅₀ of sesamin for scavenging DPPH free radical and hydroxyl radical was 0.55 mg/mL and 0.94 mg/mL, respectively. Anticancer activity experiments showed that sesamin had stronger inhibition against HepG2 and HUVEC than pinoresinol-β-D-glucaside. The extraction process by RSM was reliable and the optimal conditions were achieved to get sesamin and pinoresinol-β-D-glucaside, and they had antioxidant and anticancer activities.