In vitro screening and evaluation of 37 traditional chinese medicines for their potential to activate peroxisome proliferator-activated receptors-γ

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Abstract
Pharmacognosy Magazine,2016,12,46,120-127.
Published:March 2016
Type:Original Article
Authors:
Author(s) affiliations:

Die Gao, Yonglan Zhang, Fengqing Yang, Yexin Lin, Qihui Zhang, Zhining Xia
Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China

Abstract:

Background: Peroxisome proliferator-activated receptors (PPAR)-γ is widely used as an attractive target for the treatment of type 2 diabetes mellitus. Thiazolidinediones, the agonists of PPARγ, has been popularly utilized as insulin sensitizers in the therapy of type 2 diabetes whereas numerous severe side-effects may also occur concomitantly. Objective: The PPARγ activation activity of different polar extracts, including petroleum ether, ethyl acetate, n-butanol, residual of ethanol, the precipitate part of water and the supernatant of water extracts, from 37 traditional Chinese medicines were systematically evaluated. Materials and Methods: HeLa cells were transiently co-transfected with the re-constructed plasmids of GAL4-PPARγ-ligand binding domain and pGL4.35. The activation of PPARγ by different polarity extracts were evaluated based on the PPARγ transactivation assay and rosiglitazone was used as positive control. Results: Seven medicines (root bark of Lycium barbarumAnoectochilus sroxburghii, the rhizome of Phragmites australisPterocephalus hookeriPolygonatum sibiricum, fruit of Gleditsia sinensis, and Epimedium brevicornu) were able to significantly activate PPARγ. Conclusion: As seven medicines were able to activate PPARγ, the anti-diabetic activity of them is likely to be mediated by this nuclear receptor.

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