Pyrocincholic acid 3β-O-β-d-quinovopyranosyl-28-O-β-d-glucopyranoside suppresses adipogenesis and regulates lipid metabolism in 3T3-L1 adipocytes

Abstract

Obesity is crucially involved in many metabolic diseases, such as type 2 diabetes, cardiovascular disease and cancer. Regulating the number or size of adipocytes has been suggested to be a potential treatment for obesity. In this study, we investigated the effect of pyrocincholic acid 3β-O-β-d-quinovopyranosyl-28-O-β-d-glucopyranoside (PAQG), a 27-nor-oleanolic acid saponin extracted from Metadina trichotoma, on adipogenesis and lipid metabolism in 3T3-L1 adipocytes. The 3T3-L1 pre-adipocytes were incubated with vehicle or PAQG for 6 days in differentiation process. PAQG significantly reduced the adipogenesis, adiponectin secretion and the expression level of key transcription factors related to adipogenesis, such as PPARγ, C/EBPβ, C/EBPα, and FABP4. Moreover, PAQG increased the levels of FFA and glycerol in medium and reduced TG level in mature adipocytes. Interestingly, PAQG not only promoted the activation of AMPK and genes involved in fatty oxidation including PDK4 and CPT1a, but also inhibited those genes involved in fatty acid biosynthesis, such as SREBP1c, FAS, ACCα and SCD1. In conclusion, PAQG inhibits the differentiation and regulates lipid metabolism of 3T3-L1 cells via AMPK pathway, suggesting that PAQG may be a novel and promising natural product for the treatment of obesity and hyperlipidemia.Graphical Abstract Electronic supplementary materialThe online version of this article (doi:10.1007/s13659-017-0127-9) contains supplementary material, which is available to authorized users.

Adipogenesis Inhibitory Activity of Hypersampsone P from Hypericum subsessile

“…In skeleton muscles, AMPK is activated in response to exercise and its activators has been proved as a potential target for obesity and T2DM [19,20]. There is increasing evidence that AMPK inhibits the expression of PPAR and FABP4 and blunts adipogenesis in adipocytes [20][21][22]. It was reported that Euphorbiasteroid blunted the differentiation of human preadipocytes by enhancing the phosphorylation of AMPK for down-regulating PPARγ and fatty acid biosynthesis include sterol regulatory element-binding transcription factor 1 (SREBP1c), fatty acid synthase (FAS), acetyl-CoA carboxylase (ACC)α and stearoyl-CoA desaturase (SCD) [23].…”