Kritchevsky D, Tepper S A, Story J A
Lipids. 1977 Jan;12(1):16-21. doi: 10.1007/BF02532966.
Several of a series of linoleic acid amides have been reported to inhibit cholesterol-induced atherosclerosis in rabbits. The three amides which have been studied to the greatest extent are (in order of increasing activity) N-cyclohexyl linoleamide (AC23), N(alpha methylbenzyl) linoleamide (AC223), and N[aplha-phenyl-beta-(p-tolyl)ethyl] linoeamide (AC 485). We have found AC223 to inhibit cholesterol absorption in rats and to slightly inhibit exogenous but not endogenous cholesteremia in rabbits. In a fiber-free diet, AC223 reduces serum cholesterol and liver triglyceride levels. Rats were also fed a basal semipurified diet with and without AC223. Fecal excretion of labeled exogenous (as [ (14)C] cholesterol) or endogenous (as [14 C] mevalonolactone) steroid was 44 and 43% higher in drug treated groups. The mechanism of hypocholesteremic action of the linoleamides appears to involve inhibition of cholesterol absorption.
据报道，一系列亚油酸酰胺中的几种可抑制兔体内胆固醇诱导的动脉粥样硬化。研究程度最深的三种酰胺（按活性递增顺序）为N-环己基亚油酰胺（AC23）、N（α-甲基苄基）亚油酰胺（AC223）和N[α-苯基-β-（对甲苯基）乙基]亚油酰胺（AC 485）。我们发现AC223可抑制大鼠的胆固醇吸收，并轻微抑制兔体内外源性而非内源性胆固醇血症。在无纤维饮食中，AC223可降低血清胆固醇和肝脏甘油三酯水平。给大鼠喂食含或不含AC223的基础半纯化饮食。在药物治疗组中，标记的外源性（如[（14）C]胆固醇）或内源性（如[14 C]甲羟戊酸内酯）类固醇的粪便排泄量分别高出44%和43%。亚油酸酰胺降胆固醇作用的机制似乎涉及抑制胆固醇吸收。
