Low-density lipoprotein (LDL) and high-density lipoprotein (HDL) oxidation are well known to increase the risk for atherosclerosis. In our ongoing research on natural products with inhibitory activities against oxidation of lipoproteins, fruits of Vitex rotundifolia were found to be highly active. There is no report on the effects on LDL and HDL oxidation. Herein, we investigated the inhibitory effects of V. rotundifolia fruit extract and its six compounds, which are: (1) artemetin, (2) casticin, (3) hesperidin, (4) luteolin, (5) vitexin, and (6) vanillic acid, against LDL and HDL oxidation. The LDL and HDL oxidations were determined by measuring production of conjugated dienes and thiobarbituric acid reactive substances, amount of hyperchromicity and carbonyl content, change in electrical charge, and apoA-I aggregation. In addition, the contents of the compounds in the extracts were analyzed using HPLC-DAD. Consequently, extracts of Vitex rotundifolia fruits and compounds 2 and 4 suppressed oxidation of LDL and HDL, showing inhibition of lipid peroxidation, decrease of negative charges in lipoproteins, reduction of hyperchromicity, decrease in carbonyl contents, and prevention of apoA-I aggregation. In particular, compounds 2 and 4 exhibited more potent inhibitory effect on oxidation of LDL and HDL than the extracts, suggesting their protective role against atherosclerosis via inhibition of LDL and HDL oxidation. The contents of artemetin, casticin, and vanillic acid in the extracts were 1.838 ± 0.007, 8.629 ± 0.078, and 1.717 ± 0.006 mg/g, respectively.
Keywords: Vitex rotundifolia fruits; atherosclerosis; casticin; high-density lipoprotein; low-density lipoprotein; luteolin; oxidation.