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β-羟膦酸类似物左旋肉碱在肥胖 Zucker fa/fa 大鼠中的药效学评价。

Pharmacological evaluation of a β-hydroxyphosphonate analogue of l-carnitine in obese Zucker fa/fa rats.

机构信息

Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, México.

出版信息

Basic Clin Pharmacol Toxicol. 2013 Apr;112(4):222-8. doi: 10.1111/bcpt.12019. Epub 2012 Nov 30.

DOI:10.1111/bcpt.12019
PMID:23039375
Abstract

In this study, we evaluated the effect of an analogue of l-carnitine on parameters involved with Metabolic Syndrome in obese Zucker rats. Twenty-four rats were treated for 5 weeks with l-carnitine (300 mg/kg) and its analogue at two concentrations (100 and 250 mg/kg) to assess their impact on glucose, triglycerides and cholesterol in liver and blood samples, as well as the amount of liver glycogen. Liver slices were also analysed. The analogue reduced the levels of glucose, triglycerides and cholesterol in liver and the level of triglycerides in serum. At 100 mg/kg, the analogue proved more effective than l-carnitine in improving the biochemical alterations present in liver. The amount of liver glycogen content was higher in obese animals treated with both l-carnitine and the analogue. No changes on insulin and leptin were observed in animals treated. l-carnitine and its analogue reduced the microvesicular fatty infiltration in liver. This study demonstrated that the analogue tested is more potent and efficient than l-carnitine and improves the pharmacological profile of l-carnitine.

摘要

在这项研究中,我们评估了左旋肉碱类似物对肥胖 Zucker 大鼠代谢综合征相关参数的影响。24 只大鼠接受左旋肉碱(300mg/kg)及其两种浓度(100 和 250mg/kg)类似物治疗 5 周,以评估其对肝和血样中葡萄糖、甘油三酯和胆固醇以及肝糖原含量的影响。还分析了肝切片。类似物降低了肝中葡萄糖、甘油三酯和胆固醇的水平以及血清中甘油三酯的水平。在 100mg/kg 时,类似物在改善肝中存在的生化改变方面比左旋肉碱更有效。用左旋肉碱和类似物治疗的肥胖动物的肝糖原含量较高。用两种药物治疗的动物的胰岛素和瘦素均未发生变化。左旋肉碱及其类似物减少了肝中的微泡脂肪浸润。这项研究表明,所测试的类似物比左旋肉碱更有效且更高效,并改善了左旋肉碱的药理学特性。

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