Pharmacological Evaluation of a β‐Hydroxyphosphonate Analogue of l‐Carnitine in Obese Zucker fa/fa Rats

• Published in: Basic & clinical pharmacology & toxicology Vol. 112; no. 4; pp. 222 - 228
• Main Authors: Reyes‐Esparza, Jorge, Mendoza‐Rivera, Brissa, la Cruz‐Cordero, Ricardo, Rosado, Jorge L., Duarte‐Vázquez, Miguel Á., Solis, Mario G., Vite‐Vallejo, Odón, Rodríguez‐Fragoso, Lourdes
• Format: Journal Article
• Language: English
• Published: Oxford Blackwell 01.04.2013
• Subjects: Animals; Biological and medical sciences; Carnitine - administration & dosage; Carnitine - analogs & derivatives; Carnitine - pharmacology; Cholesterol - metabolism; Disease Models, Animal; Dose-Response Relationship, Drug; Glucose - metabolism; Glycogen - metabolism; Insulin - metabolism; Leptin - metabolism; Liver - drug effects; Liver - metabolism; Male; Medical sciences; Metabolic diseases; Metabolic Syndrome - drug therapy; Obesity; Obesity - drug therapy; Pharmacology. Drug treatments; Rats; Rats, Zucker; Triglycerides - metabolism; Evaluation; Obesity; Vertebrata; Mammalia; Rat; Aminoacid; Analog; Animal; Rodentia; Nutrition disorder; Nutritional status; Carnitine
• ISSN: 1742-7835; 1742-7843
• DOI: 10.1111/bcpt.12019

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.