Inhibition of lipid droplet accumulation in mouse macrophages by stemphone derivatives.
From a study on the biological activity of fungal stemphones and their derivatives, five derivatives having an O-alkyl moiety at C-11 of stemphone C were found to inhibit lipid droplet accumulation in macrophages without any cytotoxic effect. Among the derivatives, those having O-isopropyl and O-isobutyl were the most potent inhibitors by blocking the synthesis of both cholesteryl ester (CE) and triacylglycerol (TG), the main constituents of lipid droplets in macrophages.
Koyama
Nobuhiro
N
School of Pharmacy, Kitasato University, Tokyo, Japan.
Kobayashi
Kakeru
K
Yamazaki
Hiroyuki
H
Tomoda
Hiroshi
H
D000818:Animals; D050197:Atherosclerosis / Q000378:metabolism / Q000517:prevention & control; D016227:Benzoquinones / Q000494:pharmacology*; D002784:Cholesterol / Q000378:metabolism; D002788:Cholesterol Esters / Q000096:biosynthesis; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors / Q000378:metabolism; D005487:Foam Cells / Q000187:drug effects / Q000378:metabolism*; D050356:Lipid Metabolism / Q000187:drug effects*; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors / Q000378:metabolism; D014280:Triglycerides / Q000096:biosynthesis
D016227:Benzoquinones; D002788:Cholesterol Esters; D014280:Triglycerides; C087469:stemphone; D002784:Cholesterol; C516957:DGAT2 protein, mouse; D051048:Diacylglycerol O-Acyltransferase; D002785:Sterol O-Acyltransferase; C493492:sterol O-acyltransferase 1