Stereoselective and Carrier-mediated Transport of Monocarboxylic Acids Across Caco-2 Cells

Overview

Journal Pharm Res

Specialties Pharmacology
Pharmacy

Date 1996 Dec 1

PMID 8987079

Citations 3

Authors

T Ogihara

I Tamai

H Takanaga

Y Sai

A Tsuji

Affiliations

Soon will be listed here.

Abstract

Purpose: To characterize the transport mechanism of monocarboxylic acids across intestinal epithelial cells by examining the stereoselectivity of the transcellular transport of several chiral monocarboxylic acids.

Methods: The transport of monocarboxylic acids was examined using monolayers of human adenocarcinoma cell line, Caco-2 cells.

Results: The permeability of L-[14C]lactic acid at a tracer concentration (1 microM) exhibited pH- and concentration-dependencies and was significantly greater than that of the D-isomer. The permeabilities of both L-/D-[14C]lactic acids involve saturable and nonsaturable processes; the saturable process showed a higher affinity and a lower capacity for L-lactic acid compared with the D-isomer, while no difference between the isomers was seen for the nonsaturable process. The transport of L-lactic acid was inhibited by chiral monocarboxylic acids such as (R)/ (S)-mandelic acids and (R)/(S)-ibuprofen in a stereoselective manner. Mutually competitive inhibition was observed between L-lactic acid and (S)-mandelic acid.

Conclusions: Some chiral monocarboxylic acids are transported across the intestinal epithelial cells in a stereoselective manner by the specific carrier-mediated transport mechanism.

Citing Articles

Gastrointestinal absorption of pimozide is enhanced by inhibition of P-glycoprotein.

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PMID: 33119612 PMC: 7595425. DOI: 10.1371/journal.pone.0232438.

N-in-one permeability studies of heterogeneous sets of compounds across Caco-2 cell monolayers.

Laitinen L, Kangas H, Kaukonen A, Hakala K, Kotiaho T, Kostiainen R Pharm Res. 2003; 20(2):187-97.

PMID: 12636156 DOI: 10.1023/a:1022262818573.

Application of fractal kinetics for carrier-mediated transport of drugs across intestinal epithelial membrane.

Ogihara T, Tamai I, Tsuji A Pharm Res. 1998; 15(4):620-5.

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