Document Detail


Esculeogenin A, a new tomato sapogenol, ameliorates hyperlipidemia and atherosclerosis in ApoE-deficient mice by inhibiting ACAT.
MedLine Citation:
PMID:  17872457     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
OBJECTIVE: We recently identified esculeoside A, a new spirosolane-type glycoside, with a content in tomatoes that is 4-fold higher than that of lycopene. In the present study, we examined the effects of esculeoside A and esculeogenin A, a new aglycon of esculeoside A, on foam cell formation in vitro and atherogenesis in apoE-deficient mice. METHODS AND RESULTS: Esculeogenin A significantly inhibited the accumulation of cholesterol ester (CE) induced by acetylated low density lipoprotein (acetyl-LDL) in human monocyte-derived macrophages (HMDM) in a dose-dependent manner without inhibiting triglyceride accumulation, however, it did not inhibit the association of acetyl-LDL to the cells. Esculeogenin A also inhibited CE formation in Chinese hamster ovary cells overexpressing acyl-coenzymeA (CoA): cholesterol acyl-transferase (ACAT)-1 or ACAT-2, suggesting that esculeogenin A suppresses the activity of both ACAT-1 and ACAT-2. Furthermore, esculeogenin A prevented the expression of ACAT-1 protein, whereas that of SR-A and SR-BI was not suppressed. Oral administration of esculeoside A to apoE-deficient mice significantly reduced the levels of serum cholesterol, triglycerides, LDL-cholesterol, and the areas of atherosclerotic lesions without any detectable side effects. CONCLUSIONS: Our study provides the first evidence that purified esculeogenin A significantly suppresses the activity of ACAT protein and leads to reduction of atherogenesis.
Authors:
Yukio Fujiwara; Naoko Kiyota; Masaharu Hori; Sayaka Matsushita; Yoko Iijima; Koh Aoki; Daisuke Shibata; Motohiro Takeya; Tsuyoshi Ikeda; Toshihiro Nohara; Ryoji Nagai
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-09-13
Journal Detail:
Title:  Arteriosclerosis, thrombosis, and vascular biology     Volume:  27     ISSN:  1524-4636     ISO Abbreviation:  Arterioscler. Thromb. Vasc. Biol.     Publication Date:  2007 Nov 
Date Detail:
Created Date:  2007-10-18     Completed Date:  2007-11-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9505803     Medline TA:  Arterioscler Thromb Vasc Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2400-6     Citation Subset:  IM    
Affiliation:
Department of Medical Biochemistry, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Honjo, 1-1-1, Kumamoto 860-8556, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Atherosclerosis / drug therapy*
CHO Cells
Cells, Cultured
Cholesterol Esters / metabolism
Cricetinae
Cricetulus
Esculin / pharmacology*
Foam Cells / drug effects*
Humans
Hypercholesterolemia / drug therapy*
Macrophages / drug effects
Mice
Mice, Knockout
Plant Extracts / pharmacology*
Sapogenins / pharmacology*
Sterol O-Acyltransferase / drug effects*
Chemical
Reg. No./Substance:
0/Cholesterol Esters; 0/Plant Extracts; 0/Sapogenins; 531-75-9/Esculin; EC 2.3.1.26/Sterol O-Acyltransferase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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