The inhibition of PPARОі activity could be a promising therapy for obesity and steatosis.

Our data demonstrate that PPT is a novel PPARОі antagonist. TR-FRET assay revealed that PPT was specifically bound to PPARОі LBD, which was further confirmed by the molecular docking study. A reporter gene assay showed that PPT specifically inhibited the transactivity of PPARОі, but not PPAR О±, ОІ/Оґ and LXR О±, ОІ. These effects were confirmed with genetically obese ob/ob mice. In high-fat diet-induced obesity (DIO) mice, PPT reduced body weight and serum lipid levels, improved insulin resistance, as well as morphology and lipid accumulation, particular macrovesicular steatosis, in the livers. Here, we identified that protopanaxatriol (PPT), a major ginseng constituent, inhibited rosiglitazone-supported adipocyte differentiation of 3T3-L1 cells by repressing the expression of lipogenesis-related gene expression. However, the molecular mechanisms how ginseng and its components participate in the regulation of lipogenesis are still largely unclear. Ginseng has been used as food and traditional herbal medicine for the treatment of various metabolic diseases. Obesity is prevalent worldwide and is highly associated with metabolic disorders, such as insulin resistance, hyperlipidemia and steatosis.

Molecular docking ppt