title: Gene expression profiles of ABC transporters and cytochrome P450 3A in Caco-2 and human colorectal cancer cell lines.
abstract: OBJECTIVE
  The mRNA levels of MDR1 (P-glycoprotein), multidrug resistance-associated proteins (MRP1, MRP2), cytochrome P450 3A (CYP3A) and villin in human colorectal cell lines (HCT-15, LoVo DLD-1, HCT-116 and SW620) were quantitatively compared with those in Caco-2 cells.
  
  
  METHODS
  The mRNA levels were determined by real time quantitative polymerase chain reaction and expressed as the relative concen trations of MDR1 mRNA to glyceraldehyde-3-phosphate dehydro genase (GAPDH) mRNA. RESULTSl MDR1 mRNA was expressed in HCT-15 LoVo and DLD-1 cells at similar or lower level to Caco-2. The expression of MRP mRNA in the cell lines tested was comparable with Caco-2. MRP. mRNA was detected only in HCT-116 and SW620 at significantly lower level than Caco-2. CYP3A mRNA was detected in HCT-15 LoVo, DLD-1 and SW620 at similar level to Caco-2.
  
  
  CONCLUSIONS
  HCT-15 LoVo and DLD-1 cells express proteins important for regulating the intestinal absorption of drugs, i.e., MDR1 MRP1 and CYP3A, whereas HCT-116 and SW620 cells were not acceptable for evaluation of absorption properties of drug candidates
authors.affiliation: Department of Hospital Pharmacy, School of Medicine, Kobe University, Chuo-ku, Kobe 650-0017, Japan.
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Nakumura
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Sakaeda
authors.forename: Nobuko
authors.initials: N
authors.lastname: Ohmoto
authors.forename: Yuka
authors.initials: Y
authors.lastname: Moriya
authors.forename: Chiho
authors.initials: C
authors.lastname: Komoto
authors.forename: Toshiro
authors.initials: T
authors.lastname: Shirakawa
authors.forename: Akinobu
authors.initials: A
authors.lastname: Gotoh
authors.forename: Masafumi
authors.initials: M
authors.lastname: Matsuo
authors.forename: Katsuhiko
authors.initials: K
authors.lastname: Okmura
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000096:biosynthesis* / Q000235:genetics; D001189:Aryl Hydrocarbon Hydroxylases / Q000096:biosynthesis* / Q000235:genetics; D018938:Caco-2 Cells; D015179:Colorectal Neoplasms / Q000201:enzymology / Q000378:metabolism*; D051544:Cytochrome P-450 CYP3A; D020869:Gene Expression Profiling / Q000379:methods; D015972:Gene Expression Regulation, Neoplastic; D006801:Humans; D010089:Oxidoreductases, N-Demethylating / Q000096:biosynthesis* / Q000235:genetics; D012333:RNA, Messenger / Q000096:biosynthesis / Q000235:genetics; D014407:Tumor Cells, Cultured
chemical_list: D018528:ATP-Binding Cassette Transporters; D012333:RNA, Messenger; D001189:Aryl Hydrocarbon Hydroxylases; D051544:Cytochrome P-450 CYP3A; D010089:Oxidoreductases, N-Demethylating