Inhibition of cholesterol ester transfer protein by CGS 25159 and changes in lipoproteins in hamsters

As a result of screening, several isoflavans were identified to be antagonists of cholesterol ester transfer protein (CETP) activity. The present study evaluates CGS 25159, a synthetic isoflavan, as a putative inhibitor of CETP activity of human and hamster plasma. Determined by [3H]CE transfer from...

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Veröffentlicht in:	Atherosclerosis 1997-01, Vol.128 (1), p.59-66
Hauptverfasser:	Kothari, Himanshu V, Poirier, Kevin J, Lee, Warren H, Satoh, Yoshitaka
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzopyrans - pharmacology Biological and medical sciences Carrier Proteins - antagonists & inhibitors CETP Cholesterol ester transfer protein Cholesterol Ester Transfer Proteins Cholesterol Esters - metabolism Cholesterol, Dietary - administration & dosage Cricetinae Dose-Response Relationship, Drug General and cellular metabolism. Vitamins Glycoproteins Golden Syrian hamster HDL-cholesterol Humans Hyperlipidemias - blood Isoflavan Lipids - blood Male Medical sciences Mesocricetus Pharmacology. Drug treatments
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Zusammenfassung:	As a result of screening, several isoflavans were identified to be antagonists of cholesterol ester transfer protein (CETP) activity. The present study evaluates CGS 25159, a synthetic isoflavan, as a putative inhibitor of CETP activity of human and hamster plasma. Determined by [3H]CE transfer from HDL to VLDL+LDL fraction or by fluorescent-CE transfer assay, CGS 25159 inhibited CETP in both human plasma bottom fraction (d=1.21 g/ml) and in plasma from Golden Syrian Hamsters with an IC50
ISSN:	0021-9150 1879-1484
DOI:	10.1016/S0021-9150(96)05981-3