FAS and SREBP-1c Inhibition via AMPK Activation in HepG2 Cells by Biovip, Tox-off, and Traphanoside GO1 from Glinus oppositifolius

• Published in: Biological & pharmaceutical bulletin Vol. 46; no. 8; pp. 1057 - 1064
• Main Authors: Nguyen, Vinh Hue Thi, Do, Ha Thi, Tran, Hien Thi, Vu, Huong Thuy, Nguyen, Thu Thi, Vu, Diep Thi, Nguyen, Ha Ly Thi, Nguyen, Huy Van, Tran, Quang Luc, Nguyen, Van Anh Thi
• Format: Journal Article
• Language: English
• Published: Japan The Pharmaceutical Society of Japan 01.08.2023; Japan Science and Technology Agency
• Subjects: acetyl-CoA carboxylase (ACC); Acetyl-CoA Carboxylase - metabolism; Adenosine kinase; AMP; AMP-activated protein kinase (AMPK); AMP-Activated Protein Kinases - metabolism; Biovip; Cell activation; Coenzyme A; Dimethyl sulfoxide; Fatty Acid Synthases - metabolism; Fatty-acid synthase; Glinus oppositifolius; Hep G2 Cells; Humans; Kinases; Lipid Metabolism; Metabolic disorders; Molluginaceae; Myoblasts; Phosphorylation; Protein kinase; Proteins; Sterol Regulatory Element Binding Protein 1 - metabolism; Sterol regulatory element-binding protein; Tox-off; traphanoside GO1; Tox-off; Glinus oppositifolius; acetyl-CoA carboxylase (ACC); AMP-activated protein kinase (AMPK); Biovip; traphanoside GO1
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.b22-00892

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.