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Titolo:
Inhibition of intestinal absorption of 5-methyltetrahydrofolate by fluoxetine
Autore:
Amilburu, A; Idoate, I; Ponz, F; Larralde, J;
Indirizzi:
Univ Navarra, Fac Farm, Dept Fisiol & Nutr, Navarra, Spain Univ Navarra Navarra Spain Fac Farm, Dept Fisiol & Nutr, Navarra, Spain Hosp Virgen del Camino, Dept Bioquim, Pamplona, Spain Hosp Virgen del Camino Pamplona Spain no, Dept Bioquim, Pamplona, Spain
Titolo Testata:
JOURNAL OF PHYSIOLOGY AND BIOCHEMISTRY
fascicolo: 2, volume: 57, anno: 2001,
pagine: 71 - 79
SICI:
1138-7548(200106)57:2<71:IOIAO5>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
BRUSH-BORDER MEMBRANE; RAT SMALL-INTESTINE; FOLATE TRANSPORT; FOLIC-ACID; VESICLES; SERUM; DRUG; PURIFICATION; JEJUNUM; CACO-2;
Keywords:
folate; intestinal absorption; fluoxetine;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Ponz, F Univ Navarra, Fac Farm, Dept Fisiol & Nutr, Navarra, Spain Univ Navarra Navarra Spain , Dept Fisiol & Nutr, Navarra, Spain
Citazione:
A. Amilburu et al., "Inhibition of intestinal absorption of 5-methyltetrahydrofolate by fluoxetine", J PHYSIOL B, 57(2), 2001, pp. 71-79

Abstract

The in vitro uptake of 5-methyltetrahydrofolate (5-MeTHF) by rat and humanintestine is dose-dependently inhibited by the antidepressant drug fluoxetine (FLX). In rat jejunum rings, 0.2 rnM FLX inhibited the uptake of 5-MeTHF (0.25 muM) by 32% (15 min) and 49% (45 min). In brush border membrane vesicles (BBMV) from rat jejunum, 0.2 mM FLX inhibited the folate uptake at the overshoot (90 s) by 40%. Similar inhibition was observed with human Caco-2 cells and duodenal biopsies. FLX action is exerted on the active transport component of the folate uptake, since the drug has no effect when the passive diffusion component becomes prominent by high substrate concentration,or by 0-4 degreesC incubation or by addition of the folate transport inhibitor DIDS (1 mM). The kinetic analysis with rat BBMV suggests a non-competitive inhibition of the 5-MeTHF transport by FLX, with apparent values for K-M = 0.89 muM, Vmax = 1.89 pmol/mg prot./10 s, and K-I = 0.21 mM. After 21 days of treatment with FLX (10 mg/kg/day), the folate uptake by jejunum rings or by BBMV from the treated rats was diminished, and the folate levels in erythrocytes and serum were also decreased.

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Documento generato il 25/01/20 alle ore 03:24:29