In vitro Screening and Evaluation of 37 Traditional Chinese Medicines for Their Potential to Activate Peroxisome Proliferator‑activated Receptors‑γ

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 barbarum, Anoectochilus sroxburghii, the rhizome of Phragmites australis, Pterocephalus hookeri, Polygonatum 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.

Keywords: Diabetes mellitus; different polarity extracts; peroxisome proliferator‑activated receptor‑γ; traditional anti‑diabetic medicines