Ferrer-Lorente Raquel, Cabot Cristina, Fernández-López José-Antonio, Alemany Marià
Department of Nutrition and Food Science, Faculty of Biology, University of Barcelona, Spain.
J Pharmacol Sci. 2007 Jun;104(2):176-82. doi: 10.1254/jphs.fp0061441. Epub 2007 Jun 8.
Oleoyl-estrone (OE) decreases appetite, maintains energy expediture, induces lipolysis (sparing protein), and decreases cholesterolemia and insulin resistance. Rimonabant (SR141716) is a cannabinoid-receptor inhibitor that decreases appetite and mobilizes fat. We studied whether their combination improves their slimming effects. Male overweight rats received daily gavages of 5.3 mg/kg OE, 10 mg/kg rimonabant, or both drugs during 10 days. Body weight and composition, energy balance, adipose tissue weight, and serum hormones and metabolites were measured. OE halved food intake and maintained energy expenditure at the expense of body fat. Rimonabant effects on appetite and energy balance were less marked, resulting in lower lipid mobilization. OE and rimonabant followed the OE pattern, with no additive or synergic effects. Glycemia was maintained, but OE decreased insulin, GLP-1, and cholesterol, whilst rimonabant increased cholecystokinin and cholesterol, and decreased NEFA. Both drugs decreased leptin and triacylglycerols; ghrelin was unchanged. The results hint at different mechanisms of action of both drugs: we can assume that OE effects do not involve the cannabinoid pathway. OE does not seem to act, either, after 10 days, through the secretion of ghrelin or the intestinal appetite-controlling peptides tested.
油酰雌酮（OE）可降低食欲、维持能量消耗、诱导脂肪分解（保护蛋白质），并降低胆固醇血症和胰岛素抵抗。利莫那班（SR141716）是一种大麻素受体抑制剂，可降低食欲并动员脂肪。我们研究了它们的组合是否能增强减肥效果。雄性超重大鼠在10天内每天接受5.3毫克/千克OE、10毫克/千克利莫那班或两种药物的灌胃。测量了体重和组成、能量平衡、脂肪组织重量以及血清激素和代谢物。OE使食物摄入量减半，并以身体脂肪为代价维持能量消耗。利莫那班对食欲和能量平衡的影响不太明显，导致较低的脂质动员。OE和利莫那班遵循OE模式，没有相加或协同作用。血糖得以维持，但OE降低了胰岛素、胰高血糖素样肽-1（GLP-1）和胆固醇，而利莫那班增加了胆囊收缩素和胆固醇，并降低了非酯化脂肪酸（NEFA）。两种药物均降低了瘦素和三酰甘油；胃饥饿素未发生变化。结果提示两种药物的作用机制不同：我们可以假设OE的作用不涉及大麻素途径。10天后，OE似乎也不是通过胃饥饿素的分泌或所检测的肠道食欲控制肽起作用的。
