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Literature DB >> 8467353

Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco-2 cell layers.

Abstract

The bidirectional transepithelial fluxes of ciprofloxacin, an antibacterial fluoroquinolone, across the human intestinal epithelial Caco-2 cell-line show marked asymmetry. Basal-to-apical flux of ciprofloxacin (10 microM) exceeds apical-to-basal flux indicating net secretion. Net ciprofloxacin secretion is abolished by azide/2-deoxy-D-glucose treatment, displays saturation kinetics (Km = 0.89 +/- 0.23 mM, Vmax 44.3 +/- 4.9 nmol cm-2.h) and competition by other fluoroquinolones. A specific, active secretion in Caco-2 epithelia may explain the transintestinal elimination of ciprofloxacin observed in pharmacokinetic studies in man.

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Year: 1993 PMID： 8467353 PMCID： PMC1908048 DOI： 10.1111/j.1476-5381.1993.tb12844.x

Source DB: PubMed Journal: Br J Pharmacol ISSN： 0007-1188 Impact factor: 8.739

9 in total

1. Transepithelial vinblastine secretion mediated by P-glycoprotein is inhibited by forskolin derivatives.

Authors: J Hunter; B H Hirst; N L Simmons
Journal: Biochem Biophys Res Commun Date: 1991-12-16 Impact factor: 3.575

2. Gastrointestinal secretion of ciprofloxacin. Evaluation of the charcoal model for investigations in healthy volunteers.

Authors: F Sörgel; K G Naber; U Jaehde; A Reiter; R Seelmann; G Sigl
Journal: Am J Med Date: 1989-11-30 Impact factor: 4.965

3. Transintestinal elimination of ciprofloxacin.

Authors: R Rohwedder; T Bergan; S B Thorsteinsson; H Scholl
Journal: Chemotherapy Date: 1990 Impact factor: 2.544

4. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability.

Authors: I J Hidalgo; T J Raub; R T Borchardt
Journal: Gastroenterology Date: 1989-03 Impact factor: 22.682

Review 5. Enhancement of xenobiotic elimination: role of intestinal excretion.

Authors: Z H Israili; P G Dayton
Journal: Drug Metab Rev Date: 1984 Impact factor: 4.518

6. Transepithelial transport of oral cephalosporins by monolayers of intestinal epithelial cell line Caco-2: specific transport systems in apical and basolateral membranes.

Authors: K Inui; M Yamamoto; H Saito
Journal: J Pharmacol Exp Ther Date: 1992-04 Impact factor: 4.030

7. Coronary heart disease risk factor profiles in black patients with non-insulin-dependent diabetes mellitus: paradoxic patterns.

Authors: M A Banerji; H E Lebovitz
Journal: Am J Med Date: 1991-07 Impact factor: 4.965

8. Polarized efflux of 2',7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein from cultured epithelial cell monolayers.

Authors: G K Collington; J Hunter; C N Allen; N L Simmons; B H Hirst
Journal: Biochem Pharmacol Date: 1992-08-04 Impact factor: 5.858

9. Epithelial secretion of vinblastine by human intestinal adenocarcinoma cell (HCT-8 and T84) layers expressing P-glycoprotein.

Authors: J Hunter; B H Hirst; N L Simmons
Journal: Br J Cancer Date: 1991-09 Impact factor: 7.640

9 in total

18 in total

Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco-2 cell layers.

1. Transepithelial vinblastine secretion mediated by P-glycoprotein is inhibited by forskolin derivatives.

2. Gastrointestinal secretion of ciprofloxacin. Evaluation of the charcoal model for investigations in healthy volunteers.

3. Transintestinal elimination of ciprofloxacin.

4. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability.

Review 5. Enhancement of xenobiotic elimination: role of intestinal excretion.

6. Transepithelial transport of oral cephalosporins by monolayers of intestinal epithelial cell line Caco-2: specific transport systems in apical and basolateral membranes.

7. Coronary heart disease risk factor profiles in black patients with non-insulin-dependent diabetes mellitus: paradoxic patterns.

8. Polarized efflux of 2',7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein from cultured epithelial cell monolayers.

9. Epithelial secretion of vinblastine by human intestinal adenocarcinoma cell (HCT-8 and T84) layers expressing P-glycoprotein.

1. Intestinal ciprofloxacin efflux: the role of breast cancer resistance protein (ABCG2).

2. Influence of renal failure on intestinal clearance of ciprofloxacin in rats.

3. Active intestinal elimination of ciprofloxacin in rats: modulation by different substrates.

4. Transepithelial transport of the fluoroquinolone ciprofloxacin by human airway epithelial Calu-3 cells.

5. Intestinal elimination of ofloxacin enantiomers in the rat: evidence of a carrier-mediated process.

6. Stereoselectivity of ofloxacin intestinal transport in the rat.

7. Sparfloxacin secretion across Caco-2 cells involves a multidrug resistance-like mechanism.

8. Involvement of multidrug resistance-associated protein 2 in intestinal secretion of grepafloxacin in rats.

9. Ciprofloxacin is actively transported across bronchial lung epithelial cells using a Calu-3 air interface cell model.

10. Mechanism underlying levofloxacin uptake by human polymorphonuclear neutrophils.