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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
18
pubmed:dateCreated
2004-8-24
pubmed:abstractText
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 IC(50) around 60 and 95 microM, 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 microM, compound 1 and 2, respectively. Additionally, decrease of HDL-particle size under presence of LDL was inhibited by the 1 at 307 microM 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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0960-894X
pubmed:author
pubmed:issnType
Print
pubmed:day
20
pubmed:volume
14
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4677-81
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:15324887-Alanine, pubmed-meshheading:15324887-Animals, pubmed-meshheading:15324887-Antioxidants, pubmed-meshheading:15324887-Aspartic Acid, pubmed-meshheading:15324887-Cell Line, pubmed-meshheading:15324887-Cell Survival, pubmed-meshheading:15324887-Cinnamates, pubmed-meshheading:15324887-Electrophoresis, Agar Gel, pubmed-meshheading:15324887-Humans, pubmed-meshheading:15324887-Lipoproteins, HDL, pubmed-meshheading:15324887-Lipoproteins, LDL, pubmed-meshheading:15324887-Mice, pubmed-meshheading:15324887-Phenylalanine, pubmed-meshheading:15324887-Rats, pubmed-meshheading:15324887-Sterol O-Acyltransferase, pubmed-meshheading:15324887-Structure-Activity Relationship, pubmed-meshheading:15324887-Thiobarbituric Acid Reactive Substances, pubmed-meshheading:15324887-Time Factors
pubmed:year
2004
pubmed:articleTitle
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.
pubmed:affiliation
National Research Laboratory of Lipid Metabolism and Atherosclerosis, Korea Research Institute of Bioscience and Biotechnology, 52 Eoun-dong, Yuseong-gu, Daejeon 305-333, South Korea.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't