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

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dc.contributor.authorSang ku Lee-
dc.contributor.authorJong Min Han-
dc.contributor.authorHyun Jung Kim-
dc.contributor.authorEung Soo Kim-
dc.contributor.authorTae Sook Jeong-
dc.contributor.authorWoo Song Lee-
dc.contributor.authorKyung Hyun Cho-
dc.date.accessioned2017-04-19T09:01:20Z-
dc.date.available2017-04-19T09:01:20Z-
dc.date.issued2004-
dc.identifier.issn0960-894X-
dc.identifier.uri10.1016/j.bmcl.2004.06.101ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/6590-
dc.description.abstractA 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.-
dc.publisherElsevier-
dc.titleSynthesis 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-
dc.title.alternativeSynthesis 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-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.number18-
dc.citation.endPage4681-
dc.citation.startPage4677-
dc.citation.volume14-
dc.contributor.affiliatedAuthorSang ku Lee-
dc.contributor.affiliatedAuthorJong Min Han-
dc.contributor.affiliatedAuthorHyun Jung Kim-
dc.contributor.affiliatedAuthorEung Soo Kim-
dc.contributor.affiliatedAuthorTae Sook Jeong-
dc.contributor.affiliatedAuthorWoo Song Lee-
dc.contributor.affiliatedAuthorKyung Hyun Cho-
dc.contributor.alternativeName이상구-
dc.contributor.alternativeName한종민-
dc.contributor.alternativeName김현정-
dc.contributor.alternativeName김응수-
dc.contributor.alternativeName정태숙-
dc.contributor.alternativeName이우송-
dc.contributor.alternativeName조경현-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, vol. 14, no. 18, pp. 4677-4681-
dc.identifier.doi10.1016/j.bmcl.2004.06.101-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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