Gene expression profiles of ABC transporters and cytochrome P450 3A in Caco-2 and human colorectal cancer cell lines

被引：30
|
作者：
Nakamura, T
Sakaeda, T
Ohmoto, N
Moriya, Y
Komoto, C
Shirakawa, T
Gotoh, A
Matsuo, M
Okumura, K [1 ]
机构：
[1] Kobe Univ, Sch Med, Dept Hosp Pharm, Chuo Ku, Kobe, Hyogo 6500017, Japan
[2] Kobe Univ, Sch Med, Dept Urol, Chuo Ku, Kobe, Hyogo 6500017, Japan
[3] Kobe Univ, Sch Med, Dept Clin Genet, Chuo Ku, Kobe, Hyogo 6500017, Japan
[4] Kobe Univ, Sch Med, Int Ctr Med Res, Chuo Ku, Kobe, Hyogo 6500017, Japan
来源：
PHARMACEUTICAL RESEARCH | 2003年 / 20卷 / 02期
关键词：
MDR1; multidrug resistance-associated protein (MRP); villin; in vitro screening model;
D O I：
10.1023/A:1022251910820
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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 concentrations of MDR1 mRNA to glyceraldehyde-3-phosphate dehydrogenase (GAPDH) mRNA. Results. MDR1 mRNA was expressed in HCT-15 LoVo and DLD-1 cells at similar or lower level to Caco-2. The expression of MRP1 mRNA in the cell lines tested was comparable with Caco-2. MRP2 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.
引用
收藏
页码：324 / 327
页数：4
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