Anti-diabetic activity of swertiamarin is due to an active metabolite, gentianine, that upregulates PPAR-γ gene expression in 3T3-L1 cells.
We have previously shown the anti-diabetic effects of swertiamarin; however, pharmacokinetic analysis showed that swertiamarin had a plasma half-life of 1.3 h. Gentianine is an active metabolite of swertiamarin that possesses a pharmacophoric moiety. The aim of this study was to explore the possibility whether the anti-diabetic effect of swertiamarin is due to gentianine. Swertiamarin treatment had no significant effect on adipogenesis, or the mRNA expression of PPAR-γ and GLUT-4; however, there was a significant increase in the mRNA expression of adiponectin. On the other hand, treatment with gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-γ, GLUT-4 and adiponectin. These findings suggest, for the first time, that the anti-diabetic effect of swertiamarin is due to gentianine, an active metabolite of swertiamarin.
Department of Pharmacology, L. M. College of Pharmacy, Navrangpura, Ahmedabad, India.
Hitesh
H
Vaidya
Ramesh K
RK
Goyal
Sukhinder Kaur
SK
Cheema
D041721:3T3-L1 Cells; D050156:Adipogenesis / Q000187:drug effects; D052242:Adiponectin / Q000235:genetics / Q000378:metabolism; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects; D051275:Glucose Transporter Type 4 / Q000235:genetics / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D057888:Iridoid Glucosides / Q000494:pharmacology*; D051379:Mice; D047495:PPAR gamma / Q000235:genetics / Q000378:metabolism*; D011753:Pyrones / Q000494:pharmacology*; D015854:Up-Regulation
D052242:Adiponectin; D000470:Alkaloids; D051275:Glucose Transporter Type 4; D007004:Hypoglycemic Agents; D057888:Iridoid Glucosides; D047495:PPAR gamma; D011753:Pyrones; C495693:Slc2a4 protein, mouse; C013270:swertiamarin; C060402:gentianine