Aim To investigate the effects of valsartan on lectin-like oxidized low density lipoprotein receptor 1 （ LOX-1） expression induced by asymmetric dimethylarginine （ADMA） in cultured human umbilical vein endothelial cells （HUVEC）. Methods 15 μmol/L ADMA was added into the cultured HUVEC for 24 h, intracellular reactive oxygen species （ROS） generation was measured by DCFH-DA. NADPH p22phox subunit and LOX-1 mRNA transcription were detected by quantitative competitive reverse transcription-polymerase chain reaction （RT-PCR）. LOX-1 protein expression was detected by cell enzyme linked immunosorbent assay （ELISA）. Results Valsartan significantly decreased intracellular ROS generation, inhibited the transcription of p22phox, LOX-1 mRNA and LOX-1 protein expression compared with ADMA group （P<0.05）, and this effect was in a dose-dependent manner. Conclusions Valsartan inhibited expression of LOX-1 induced by ADMA, involving in inhibiting the expression of p22phox through decreasing intracellular ROS generation. This may be part of the mechanism of its anti-atherosclerotic effect independent of anti-hypertensive effect.