Growing evidence indicates that oxidized low density lipoprotein (LDL) may promote atherogenesis. Therefore, inhibition of LDL oxidation may impede this process. The inhibitory effected on the susceptibility of human LDL to Cu²+ or macrophages induced oxidation was investigated by monitoring thiobarbituric acid reactive substances (TBARS). Organosulfur compounds of garlic oil contains diallyldisulfide, diallyltrisulfide, diallyltetrasulfide, and diallyl pentasulfide in order. Garlic oil inhibited LDL oxidation by Cu²+, or macrophages in a dose dependently, with a 20~60 μg, as increased TBARS assay. Garlic oil, at 60 μM, almost completely inhibited macrophages induced increase in electrophoretic mobility of LDL. When compared with several other antioxidants, probucol showed highest ability,and then garlic oil showed a much higher ability than natural occurring antioxidants, α-tocopherol and ascorbic acid. The results suggested that garlic oil might play the inhibitory effects in the process of LDL oxidation.