title: In vitro evaluation of dual agonists for PPARγ/β from the flower of Edgeworthia gardneri (wall.) Meisn.
abstract: BACKGROUND
  In Tibet, the flower of Edgeworthia gardneri (Wall.) Meisn., locally named "Lvluohua, [symbols: see text]", has been traditionally used to treat diabetes mellitus for many years.
  
  
  OBJECTIVE
  To evaluate the activity of dual agonists for PPARγ/β from the flower of E.gardneri in vitro.
  
  
  METHODS
  HeLa cells were transiently co-transfected with the re-constructed plasmids of pBIND-PPARγ-LBD or pBIND-PPARβ-LBD and rL4.35. The activities of crude extracts, secondary fractions and compounds from the flower of E.gardneri were evaluated with the transfected cells. Rosiglitazone (at 0.5 μg/mL) and L-165041 (at 0.5 μg/mL) were used as the positive controls for PPARγ and PPARβ respectively.
  
  
  RESULTS
  The results demonstrated that n-hexane, ethyl acetate and n-butanol extracts from the flower of E.gardneri were able to significantly activate PPARγ and PPARβ respectively, and the activity of ethyl acetate extract was much better. We further observed that, among the 11 secondary fractions of ethyl acetate extract, the fr. 9 could activate PPARγ and PPARβ significantly. Moreover, umbelliferone (from fr.9) and pentadecanoic acid could activate PPARγ and PPARβ at the same time.
  
  
  CONCLUSIONS
  The extracts from the flower of E.gardneri could significantly activate PPARγ and PPARβ. Besides, umbelliferone and pentadecanoic acid isolated from the flower of E.gardneri were the new agonists for PPARγ and PPARβ.
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China.
authors.forename: Die
authors.initials: D
authors.lastname: Gao
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China.
authors.forename: Yong-lan
authors.initials: YL
authors.lastname: Zhang
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China.
authors.forename: Pan
authors.initials: P
authors.lastname: Xu
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China.
authors.forename: Ye-xin
authors.initials: YX
authors.lastname: Lin
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China.
authors.forename: Feng-qing
authors.initials: FQ
authors.lastname: Yang
authors.affiliation: College of Pharmacy and Bioengineering, Chongqing University of Technology, Chongqing 400054, China.
authors.forename: Jian-hui
authors.initials: JH
authors.lastname: Liu
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China.
authors.forename: Hai-wen
authors.initials: HW
authors.lastname: Zhu
authors.affiliation: College of Chemistry and Chemical Engineering, Chongqing University, Chongqing, 400030, China. Electronic address: tcm_anal_cqu@163.com.
authors.forename: Zhi-ning
authors.initials: ZN
authors.lastname: Xia
mesh_terms: D005227:Fatty Acids / Q000302:isolation & purification / Q000494:pharmacology*; D035264:Flowers / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D047495:PPAR gamma / Q000819:agonists* / Q000235:genetics; D048068:PPAR-beta / Q000819:agonists* / Q000235:genetics; D010936:Plant Extracts / Q000494:pharmacology; D029645:Thymelaeaceae; D014468:Umbelliferones / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D005227:Fatty Acids; D047495:PPAR gamma; D048068:PPAR-beta; D010936:Plant Extracts; D014468:Umbelliferones; C031477:7-hydroxycoumarin; C117025:pentadecanoic acid
keywords: 7-Hydroxy-4’-methoxyflavone (pubChem CID: 5320693); Diabetes mellitus; Dual agonists; Edgeworthia gardneri (Wall.) Meisn; Ethyl acetate extract; PPARγ/β; daphnoretin (pubChem CID: 5281406); edgeworin (pubChem CID: 10925304); edgeworoside A (pubChem CID: 11958884); edgeworthin (ChemIDplus RN: 53947-90-3); pentadecanoic acid (pubChem CID: 13849); rutamontine (MeSH Unique ID: C480552); tiliroside (pubChem CID: 5320686); umbelliferone (pubChem CID: 5281426); β-adenosine (pubChem CID: 191); β-daucosterol (pubChem CID: 5742590); β-sitosterol (pubChem CID: 222284)