title: [Screening active components in compound danshen based on PXR-CYP3A4: an experimental study].
abstract: OBJECTIVE
  To screen active components in Compound Danshen (CD) based on pregnane X receptor-cytochrome P450 3A4 (PXR-CYP3A4).
  
  
  METHODS
  By using PXR-CYP3A stable transfection human hepatoblastoma G2 (HepG2) cell lines engineering cell strain combined reporter genes technology, active components that induce or inhibit PXR-CYP3A4 paths in CD were screened, and confirmed at the level of enzymic activities. The experiment was divided into the positive control group (RIF 10 micro mol/L), the DMSO group (DMSO 0.1%), each dose of treatment groups (ginsenoside Rc, Rf, Rb2, Rg2, F2, F1, tanshinone I , isoborneol 5, 10, 25, 50, 100, and 200 micro mol/L; each with six duplicates). Cells medium was removed 36, 48, and 60 h after treatment. The activity of CYP3A4 was then determined in the supernant and the fold induction was calculated.
  
  
  RESULTS
  Compared with the DMSO group, the fold induction increased when ginsenoside Rc, Rf, Rb2, Rg2, F2, F1, tanshinone I , and isoborneol 50 and 100 micro mol/L was respectively intervened for 36, 48, and 60 h (P <0.05). When cells were treated with isoborneol 200 micro mol/L for 48 and 60 h,the fold induction of ginsenoside Rb2, Rg2, and F1 was significantly higher than that of the RIF group (P <0.05). Enzymic activity results showed that ginsenoside Rc, Rf, Rb2, F2, and F1 could increase the enzyme activity of CYP3A4 at 48 h (P <0.05).
  
  
  CONCLUSIONS
  Ginsenoside Rc, Rf, Rb2, F2, F1, tanshinone I, and isoborneol in DC could induce CYP3A4 enzymes.
authors.forename: Yong
authors.initials: Y
authors.lastname: Xiao
authors.forename: Zeng-chun
authors.initials: ZC
authors.lastname: Ma
authors.forename: Yu-gaung
authors.initials: YG
authors.lastname: Wang
authors.forename: Hong-ling
authors.initials: HL
authors.lastname: Tan
authors.forename: Hao-sheng
authors.initials: HS
authors.lastname: Liu
authors.forename: Xian-xie
authors.initials: XX
authors.lastname: Zhang
authors.forename: Bei-bei
authors.initials: BB
authors.lastname: Lu
authors.forename: Xiang-lin
authors.initials: XL
authors.lastname: Tang
authors.forename: Qian-de
authors.initials: QD
authors.lastname: Linag
authors.forename: Cheng-rong
authors.initials: CR
authors.lastname: Xiao
mesh_terms: D045784:Abietanes; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism*; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D017930:Genes, Reporter; D036145:Ginsenosides / Q000378:metabolism; D056945:Hep G2 Cells; D006801:Humans; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid / Q000378:metabolism*; D027561:Salvia miltiorrhiza; D014162:Transfection
chemical_list: D045784:Abietanes; D004365:Drugs, Chinese Herbal; D036145:Ginsenosides; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; C021751:tanshinone; C044462:ginsenoside Rc; C048026:ginsenoside Rb2; C028972:dan-shen root extract; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human