3,4-dihydroxy Hydrocinnamic acid (L-Aspartic acid dibenzyl ester) amide inhibits human ACAT-1 and ACAT-2 (Acyl-Coenzyme A cyltransferase-1 and -2) equally with an IC50 of about 60 μM. ACAT-1 and ACAT-2 catalyze the formation of long chain fatty acyl-coenzyme A and cholesterol esters from cholesterol, and may play a role in the development of atherosclerosis. This chemical inhibits human ACAT-1 and ACAT-2 with an IC50 values of 95 and 81 μM, respectively and also inhibits copper-mediated oxidation of low density lipoproteins by 91% at a concentration of 2 μM.
1 Rudel, L.L., Lee, R.G., Cockman, T.L. Acyl coenzyme A: Cholesterol acyltransferase types 1 and 2: structure and function in atherosclerosis. Curr Opin Lipidol 12 121-127 (2001). 2 Lee, R.G., Willingham, M.C., Davis, M.A., et al. Differential expression of ACAT1 and ACAT2 among cells within liver, intestine, kidney, and adrenal of nonhuman primates. J Lipid Res 41 1991-2001 (2000). 3 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 Medicinal Chem Letters 14 4677-4681 (2004).
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