Abstract
Obesity is caused by an excess storage of body fat, resulting from a chronic imbalance between energy intake and expenditure. Gentiana lutea L. (GL) root has been reported to reduce lipid accumulation in the aortic wall of diabetic rats. Here, we performed fractionation and isolation of the bioactive constituent(s) that may be responsible for the antiadipogenic effects of the GL root extract. A single compound, loganic acid, was identified as a candidate component in the 30% ethanol extract of GL. Loganic acid treatment significantly decreased the adipocyte differentiation of 3T3-L1 preadipocytes in a dose-dependent manner. The expression of key adipogenesis-related genes such as adiponectin (Adipoq), peroxisome proliferator-activated receptor gamma (Pparg), lipoprotein lipase (Lpl), perilipin1 (Plin1), fatty acid binding protein 4 (Fabp4), glucose transporter type 4 (Slc2a4), CCAAT/enhancer-binding protein alpha (Cebpa), and tumor necrosis factor-alpha (Tnf) were significantly reduced following treatment with loganic acid. In vivo experiments in an ovariectomy-induced obesity mouse model showed that loganic acid (oral administration with 10 and 50 mg/kg/day) significantly inhibited body weight gain, total fat increase, fatty hepatocyte deposition in the liver, and adipocyte enlargement in the abdominal visceral fat tissues. These results suggest that loganic acid in the GL root extract has antiadipogenic effects in vitro and in vivo. Loganic acid may be beneficial for the prevention and treatment of obesity, particularly in menopausal obese women.
Highlights
Obesity is a chronic disease that can lead to abnormal or excessive body fat accumulation and is associated with various metabolic syndromes, including the hardening of blood vessels, a highMolecules 2018, 23, 1663; doi:10.3390/molecules23071663 www.mdpi.com/journal/moleculesMolecules 2018, 23, 1663 risk of type 2 diabetes, and cardiovascular diseases [1]
The inhibitory effect of a 30% ethanol extract of Gentiana lutea L. (GL) root on adipocyte differentiation was investigated by the assessment of the mRNA expression of adipogenesis-related genes, and by the assessment of lipid accumulation in 3T3-L1 cells
The treatment of 3T3-L1 cells with GL root extract significantly reduced the mRNA expression of the glucose transporter type 4 (GLUT4) (Slc2a4) and lipoprotein lipase (Lpl), and effectively reduced oil red O accumulation (Supplementary Figure S1)
Summary
Obesity is a chronic disease that can lead to abnormal or excessive body fat accumulation and is associated with various metabolic syndromes, including the hardening of blood vessels, a highMolecules 2018, 23, 1663; doi:10.3390/molecules23071663 www.mdpi.com/journal/moleculesMolecules 2018, 23, 1663 risk of type 2 diabetes, and cardiovascular diseases [1]. Obesity is a chronic disease that can lead to abnormal or excessive body fat accumulation and is associated with various metabolic syndromes, including the hardening of blood vessels, a high. Obesity is mostly caused by excessive food intake, insufficient exercise, and genetic susceptibility [2]. Some cases are caused by medications, endocrine disorders, or mental disorder [3]. If behavioral approaches are not suitable, pharmacological medications may be considered to reduce appetite or decrease fat absorption [4]. Pharmacotherapy for the treatment of obesity can effectively reduce body weight and the risk of medical comorbidities [5]. Numerous effective medications for weight loss are currently available, there are still limitations, including serious adverse effects and questionable long-term safety
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