The early stage of atherosclerosis is characterized by the aggregation of foam cells, so called a fatty streak, in the inner arterial wall. CAY10487 inhibits formation of fatty streak lesions of the thoracic aorta in high cholesterol-fed rabbits without affecting plasma lipid profiles or significantly inhibiting ACAT-1 or ACAT-2 activity.1,2 The percent area occupied by the atherosclerotic lesion in rabbits supplemented with 0.05% CAY10487 in the diet was 16.1% compared to 53.5% in control rabbits.1 CAY10487 also exhibits antioxidant activity, inhibiting copper-mediated oxidation of low-density lipoprotein by about 75% at a concentration of 2 µM.2
1
Lee, S., Lee, C., Oh, J., et al. Anti-atherogenic effects of 3,4-dihydroxy hydrocinnamides. Bioorg Med Chem Lett132681-2682(2003).
2
Lee, S., Han, J., Kim, H., et al. Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA: Cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size. Bioorg Med Chem Lett144677-4681(2004).
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COC(=O)[C@H](C)NC(=O)\C=C/c1ccc(O)c(O)c1
Background Reading
Lee, S., Han, J., Kim, H., et al. Synthesis of cinnamic acid derivatives and their inhibitory effects on LDL-oxidation, acyl-CoA: Cholesterol acyltransferase-1 and -2 activity, and decrease of HDL-particle size. Bioorg Med Chem Lett144677-4681(2004).
Lee, S., Lee, C., Oh, J., et al. Anti-atherogenic effects of 3,4-dihydroxy hydrocinnamides. Bioorg Med Chem Lett132681-2682(2003).
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