title: 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.
  
  
  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.
  
  
  CONCLUSIONS
  As seven medicines were able to activate PPARγ, the anti-diabetic activity of them is likely to be mediated by this nuclear receptor.
  
  
  CONCLUSIONS
  Lots of the tested medicinal products had activation effects on activating PPARγEthyl acetate extracts of root bark of L.barbarum, rhizome of P.saustralis and fruit of G.siasinensis showed good PPARγ activation effect similar or higher than that of positive control, 0.5 μg/mL rosiglitazonePetroleum ether extracts of A.roxburghii, P. hookeri, P. sibiricum, E.brevicornu also can significantly activate PPARγ, the effects of them were higher than t0.5 μg/mL rosiglitazoneSchisandra chinensis (Turcz.) Baill., the fruit Cornus officinalis Siebold and Zucc., Alisma plantago-aquatica L. and the root of Trichosanthes Kirilowii Maxim., traditional anti-diabetic mediciness in China, had no effects on the activation of PPARγ. Abbreviations used: PPARγ: Peroxisome Proliferator-activated Receptors-γ, TCMs: Traditional Chinese medicines, TZDs: Thiazolidinediones, LBD: Ligand binding domain, DMSO: Dimethyl sulfoxide, FBS: Fetal bovine serum, DMEM: Dulbecco's modified Eagle's medium.
authors.affiliation: Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China.
authors.forename: Die
authors.initials: D
authors.lastname: Gao
authors.affiliation: Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China.
authors.forename: Yonglan
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China.
authors.forename: Fengqing
authors.initials: F
authors.lastname: Yang
authors.affiliation: Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China.
authors.forename: Yexin
authors.initials: Y
authors.lastname: Lin
authors.affiliation: Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China.
authors.forename: Qihui
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: Department of Pharmacy, College of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, P.R. China.
authors.forename: Zhining
authors.initials: Z
authors.lastname: Xia
keywords: Diabetes mellitus; different polarity extracts; peroxisome proliferator-activated receptor-γ; traditional anti-diabetic medicines