PURPOSE: 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
PURPOSE: 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., MDR1MRP1 and CYP3A, whereas HCT-116 and SW620 cells were not acceptable for evaluation of absorption properties of drug candidates
Authors: K S Lown; R R Mayo; A B Leichtman; H L Hsiao; D K Turgeon; P Schmiedlin-Ren; M B Brown; W Guo; S J Rossi; L Z Benet; P B Watkins Journal: Clin Pharmacol Ther Date: 1997-09 Impact factor: 6.875
Authors: Danielle M Pastor; Lisa S Poritz; Thomas L Olson; Christina L Kline; Leonard R Harris; Walter A Koltun; Vernon M Chinchilli; Rosalyn B Irby Journal: Int J Clin Exp Med Date: 2010-02-22
Authors: Xiaomei I Liu; Jeremiah D Momper; Natella Y Rakhmanina; Dionna J Green; Gilbert J Burckart; Tim R Cressey; Mark Mirochnick; Brookie M Best; John N van den Anker; André Dallmann Journal: Clin Pharmacokinet Date: 2020-11 Impact factor: 6.447
Authors: Sisi Qin; Duan Liu; Manish Kohli; Liguo Wang; Peter T Vedell; David W Hillman; Nifang Niu; Jia Yu; Richard M Weinshilboum; Liewei Wang Journal: Clin Pharmacol Ther Date: 2017-11-22 Impact factor: 6.875