关键词: AMP-activated protein kinase (AMPK) Biovip Glinus oppositifolius Tox-off acetyl-CoA carboxylase (ACC) traphanoside GO1

Mesh : Humans Hep G2 Cells Sterol Regulatory Element Binding Protein 1 / metabolism AMP-Activated Protein Kinases / metabolism Molluginaceae Lipid Metabolism Fatty Acid Synthases / metabolism Acetyl-CoA Carboxylase / metabolism

来  源:   DOI:10.1248/bpb.b22-00892

Abstract:
Glinus oppositifolius is an endemic herbaceous plant found in tropical Asian countries and is native in Vietnam. It is used in traditional folk medicine because of its flavor and antiseptic and laxative effects. In the current research, the effects of Tox-off, Biovip, and the purified compounds isolated from G. oppositifolius in the previous study were evaluated on the activation of adenosine 5\'-monophosphate-activated protein kinase (AMPK)-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) in C2C12 myoblasts. In addition, the most potent active compounds, traphanoside-GO1 (TRA-GO1) and TRA-GO5 have validated the reduction of fatty acid synthase (FAS) and sterol regulatory element binding protein (SREBP)-1c in HepG2 cells. We found that Tox-off and Biovip significantly increased the phosphorylation of AMPK and ACC in C2C12 myoblasts. Furthermore, TRA-GO1 and TRA-GO5 significantly increased the AMPK activation and phosphorylation of its downstream substrate ACC in a concentration-dependent way compared to the dimethyl sulfoxide (DMSO) control. Besides, the protein level of FAS and SREBP-1c decreased by TRA-GO1 and TRA-GO5 in a concentration-dependent manner. Taken together, our results showed that the increased AMPK and ACC phosphorylation by active components of G. oppositifolius may activate the AMPK signaling pathways, which are useful for the anti-obesity and its related metabolic disorders.
摘要:
Glinusoppositifolius是一种在热带亚洲国家发现的特有草本植物,原产于越南。由于其风味,防腐和通便作用,因此被用于传统民间医学。在目前的研究中,Tox-off的影响,Biovip,并对先前研究中分离出的纯化化合物对C2C12成肌细胞中腺苷5'-单磷酸活化蛋白激酶(AMPK)活化蛋白激酶(AMPK)和乙酰辅酶A羧化酶(ACC)的活化进行了评估。此外,最有效的活性化合物,天花苷-GO1(TRA-GO1)和TRA-GO5验证了HepG2细胞中脂肪酸合成酶(FAS)和固醇调节元件结合蛋白(SREBP)-1c的降低。我们发现Tox-off和Biovip显着增加C2C12成肌细胞中AMPK和ACC的磷酸化。此外,与二甲基亚砜(DMSO)对照相比,TRA-GO1和TRA-GO5以浓度依赖性方式显著增加其下游底物ACC的AMPK活化和磷酸化。此外,TRA-GO1和TRA-GO5以浓度依赖性方式降低FAS和SREBP-1c的蛋白水平。一起来看,我们的结果表明,通过G的活性成分增加的AMPK和ACC磷酸化可以激活AMPK信号通路,这对于抗肥胖及其相关的代谢紊乱是有用的。
公众号