Facultad de Ciencias Experimentales y Técnicas, Universidad San Pablo-CEU, P.O. Box 67, 28660 Boadilla del Monte, Madrid, Spain.
Environ Toxicol Pharmacol. 1996 Dec 20;2(4):351-7. doi: 10.1016/s1382-6689(96)00069-5.
The release of both glycerol and free fatty acids (FFA) into a medium by epididymal fat pad pieces from fed rats incubated in Krebs Ringer bicarbonate-albumin buffer supplemented or not with epinephrine decreased more in the presence of etofibrate than in the presence of equimolecular doses of nicotinic acid or clofibrate. The first drug was the only one to stimulate the rate of fatty acid re-esterification when incubations were done under basal conditions. By 3 h after their acute oral administration all three drugs decreased plasma FFA levels, although the effect from etofibrate was largest, the drugs enhanced or decreased plasma glycerol levels depending on both the dose and the time after treatment. Plasma triglycerides also decreased at 3 h after oral drug administration, and this effect was similar with etofibrate and nicotinic acid but less with clofibrate. With the exception of a decrease at 7 h after the highest dose (1.2 mmol/kg) of either etofibrate or nicotinic acid (but not clofibrate), plasma cholesterol levels remained stable at 7 h after the respective treatments. Thus, the hypocholesterolemic effect of these drugs seems secondary to their hypotriglyceridemic effect, which would be a consequence of their respective antilipolytic actions, and follows an efficiency sequence of etofibrate, nicotinic acid and clofibrate.
用 Krebs-Ringer 重碳酸盐-白蛋白缓冲液培养的 fed 大鼠附睾脂肪垫组织，在添加或不添加肾上腺素的情况下，释放甘油和游离脂肪酸 (FFA) 进入培养基，在 presence of etofibrate 的情况下比在 equimolecular doses of nicotinic acid 或 clofibrate 中的情况下减少得更多。当在基础条件下进行孵育时，第一种药物是唯一一种刺激脂肪酸再酯化速率的药物。在急性口服给药后 3 小时，所有三种药物都降低了血浆 FFA 水平，尽管 etofibrate 的效果最大，但药物根据剂量和治疗后时间的不同，会增加或降低血浆甘油水平。口服药物后 3 小时，血浆甘油三酯也降低，这种效果与 etofibrate 和烟酸相似，但与 clofibrate 不同。除了在最高剂量（1.2 mmol/kg）的 etofibrate 或烟酸（但不是 clofibrate）后 7 小时降低之外，血浆胆固醇水平在各自治疗后 7 小时保持稳定。因此，这些药物的降胆固醇作用似乎是其降甘油三酯作用的次要作用，这是它们各自的抗脂肪分解作用的结果，并且遵循 etofibrate、烟酸和 clofibrate 的效率顺序。
