Highly Sensitive Measurement of P-Glycoprotein-Mediated Transport Activity in Caco-2 Cells

Wakuda, Hirokazu; Nejime, Namie; Tada, Yasuyuki; Kagota, Satomi; Umegaki, Keizo; Yamada, Shizuo; Shinozuka, Kazumasa

doi:10.1248/bpb.33.1238

Cited by 3 publications

(2 citation statements)

References 12 publications

(11 reference statements)

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“…Quantification of the intracellular concentration of rhodamine 123 in the Caco-2 cells was performed using fluorescent images at several time points (0, 10, 20, 30, and 60 min) by a chronological measurement program (EZ-C1; Nikon, Tokyo, Japan). The fluorescence intensity at 0 min was defined as 100 % [9,10].…”

Section: Quantification Of Rhodamine 123 By Time-lapse Confocal Lasermentioning

confidence: 99%

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Differential effects of mitogen-activated protein kinase pathway inhibitors on P-glycoprotein activation

Wakuda

Miyauch²,

Maruyama³

et al. 2015

ADMET DMPK

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Section: Quantification Of Rhodamine 123 By Time-lapse Confocal Lasermentioning

confidence: 99%

“…The confocal laser scanning microscopy-based assay was used to measure residual rhodamine 123 in the apical region of Caco-2 cells; this method is more sensitive than conventional methods that rely on microplate readers and fluorescence microscopy [9,10]. …”

Section: Introductionmentioning

confidence: 99%

Differential effects of mitogen-activated protein kinase pathway inhibitors on P-glycoprotein activation

Wakuda

Miyauch²,

Maruyama³

et al. 2015

ADMET DMPK

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P-gp inhibition and enhanced oral bioavailability of amikacin Sulfate: A novel approach using Thiolated Chito-PEGylated Lipidic Hybrids

El-Say,

Megahed,

Abdalla

et al. 2024

International Journal of Pharmaceutics

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Effects of Anticholinergic Drugs Used for the Therapy of Overactive Bladder on P-Glycoprotein Activity

Wakuda

Okura

Maruyama‐Fumoto

et al. 2019

Biological & Pharmaceutical Bulletin

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We evaluated the effects of anticholinergic drugs principally used for the therapy of overactive bladder (OAB) on the activity of P-glycoprotein, an efflux transport protein, in Caco-2 cells. The time-dependent changes in the fluorescence of residual rhodamine 123, a P-glycoprotein activity marker, in the apical region of Caco-2 cells were measured in the presence of anticholinergic drugs using time-lapse confocal laser scanning microscopy. The effect of anticholinergic drugs on human P-glycoprotein ATPase activity was also measured. The fluorescence of residual rhodamine 123 in untreated Caco-2 cells decreased over time. The gradual decrease in the fluorescence was significantly inhibited by treatment with cyclosporine A, darifenacin, and trospium. In contrast, oxybutynin, N-desethyl-oxybutynin (DEOB), propiverine, and its active metabolites (M-1, M-2), imidafenacin, solifenacin, or tolterodine had little effect on the efflux of rhodamine 123. P-Glycoprotein ATPase activity was increased by darifenacin. Darifenacin and trospium reduced the rhodamine 123 transfer across the apical cell membrane. These data suggest that darifenacin and trospium interact with P-glycoprotein. Additionally, darifenacin influenced P-glycoprotein ATPase activity. These results suggest that darifenacin may be a substrate of P-glycoprotein. This study is the first paper to test simultaneously the effects of 10 anticholinergic drugs used currently for the therapy of OAB, on the P-glycoprotein.

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Highly Sensitive Measurement of P-Glycoprotein-Mediated Transport Activity in Caco-2 Cells

Cited by 3 publications

References 12 publications

Differential effects of mitogen-activated protein kinase pathway inhibitors on P-glycoprotein activation

Differential effects of mitogen-activated protein kinase pathway inhibitors on P-glycoprotein activation

P-gp inhibition and enhanced oral bioavailability of amikacin Sulfate: A novel approach using Thiolated Chito-PEGylated Lipidic Hybrids

Effects of Anticholinergic Drugs Used for the Therapy of Overactive Bladder on P-Glycoprotein Activity

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