Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and high-density lipoprotein-induced cholesterol efflux in macrophages.
作者： Azuma Yukimasa , Kawasaki Takashi , Ikemoto Kiyohito , Ohno Katsutoshi , Yamada Toshihiro
DOI: 10.1254/JJP.79.159
关键词:
摘要: Abstract We investigated the effects of a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, NTE-122 (trans-1,4-bis[[1-cyclohexyl-3-(4-dimethylamino phenyl)ureido]methyl]cyclohexane), on ACAT activities in macrophages originating from several species and high-density lipoprotein (HDL)-induced cholesterol efflux phorbol 12-myristate 13-acetate (PMA)-treated THP-1 cells. inhibited cell-free human PMA-treated cells mouse J774.1 with IC50 values 0.88 360 nM, respectively. competively activity also cellular cells, rat peritoneal 3.5, 84 6800 Furthermore, prevented accumulation incubated acetylated low density lipoprotein, simultaneously HDL, while it caused significant amount free absence even presence HDL. enhanced HDL-induced established foam converted These results suggest that NTE-122, capable inhibiting macrophage humans more strongly than those other species, exhibits anti-atherogenic by preventing cell formation enhancing regression humans.
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