Anti‐diabetic Activity of Swertiamarin is due to an Active Metabolite,Gentianine, that Upregulates PPAR‐γ Gene Expression in 3T3‐L1 cells |
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| Authors: | Hitesh Vaidya Ramesh K Goyal Sukhinder Kaur Cheema |
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| Affiliation: | 1. Department of Pharmacology, L. M. College of Pharmacy, , Navrangpura, Ahmedabad, 380009 India;2. Department of Biochemistry, Memorial University, , St. John's, NL, A1B3X9 Canada;3. Director (Pharmacology and Clinical Research), SPP School of Pharmacy and Technology Management, Narsee Monjee Institute of Management Studies, , Mumbai, 400 058 India |
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| Abstract: | 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. Copyright © 2012 John Wiley & Sons, Ltd. |
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| Keywords: | Diabetes swertiamarin gentianine PPAR‐γ GLUT‐4 adiponectin |
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