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Title 

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

Authors 

Sang ku LeeJong Min HanHyun Jung KimEung Soo KimTae Sook JeongWoo Song LeeKyung Hyun Cho

Publisher 

Elsevier

Issue Date 

2004

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 18, pp. 4677-4681

Keywords 

3,4 dihydroxyhydrocinnamic acid(aspartic acid dibenzyl ester)amide4 hydroxycinnamic acid(phenylalanine methyl ester)amide4 hydroxycoumarin derivativecholesterol acyltransferasedrug effectdrug synthesisoxidationaspartic acidlipoproteins, LDLsterol o-acyltransferase

Abstract 

A series of cinnamic acid derivatives were prepared and their biological activities were evaluated in lipoprotein metabolism. Among the tested compounds, 4-hydroxycinnamic acid (l-phenylalanine methyl ester) amide (1) and 3,4-dihydroxyhydrocinammic acid (l-aspartic acid dibenzyl ester) amide (2) showed potent anti-atherogenic and anti-oxidant activities. A series of cinnamic acid derivatives were synthesized and their biological abilities on lipoprotein metabolism were examined. Among the tested compounds, 4-hydroxycinnamic acid (l-phenylalanine methyl ester) amide (1) and 3,4-dihydroxyhydrocinammic acid (l-aspartic acid dibenzyl ester) amide (2) inhibited human acyl-CoA:cholesterol acyltransferase-1 and -2 activities with apparent IC50 around 60 and 95 μM, respectively. Compounds 1 and 2 also served as an antioxidant against copper mediated low-density lipoproteins (LDL) oxidation with apparent IC 50 = 52 and 3 μM, compound 1 and 2, respectively. Additionally, decrease of HDL-particle size under presence of LDL was inhibited by the 1 at 307 μM of final concentration. Treatment of the 1 or 2 did not influence normal growth of RAW264.7 without detectable cytotoxic activity from a cell viability test. These results suggest that the new cinnamic acid derivatives possess useful biological activity as an anti-atherosclerotic agent with inhibition of cellular cholesterol storage and transport by the both ACAT, inhibition of LDL-oxidation, HDL particle size rearrangement.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2004.06.101

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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