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Titolo:
Uptake properties of lamivudine (3TC) by a continuous renal epithelial cell line
Autore:
Leung, S; Bendayan, R;
Indirizzi:
Univ Toronto, Fac Pharm, Dept Pharmaceut Sci, Toronto, ON M5S 2S2, Canada Univ Toronto Toronto ON Canada M5S 2S2 t Sci, Toronto, ON M5S 2S2, Canada
Titolo Testata:
CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY
fascicolo: 1, volume: 79, anno: 2001,
pagine: 59 - 66
SICI:
0008-4212(200101)79:1<59:UPOL(B>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
IMMUNODEFICIENCY-VIRUS TYPE-1; BORDER MEMBRANE-VESICLES; ORGANIC CATION TRANSPORTER; FUNCTIONAL EXPRESSION; NUCLEOSIDE TRANSPORT; TETRAETHYLAMMONIUM TRANSPORT; ION-TRANSPORT; LLC-PK1 CELLS; KIDNEY; 3'-AZIDO-3'-DEOXYTHYMIDINE;
Keywords:
3TC; kidney; uptake; LLC-PK1; tubular elimination;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
49
Recensione:
Indirizzi per estratti:
Indirizzo: Bendayan, R Univ Toronto, Fac Pharm, Dept Pharmaceut Sci, 19 Russell St, Toronto, ON M5S 2S2, Canada Univ Toronto 19 Russell St Toronto ON Canada M5S2S2 2, Canada
Citazione:
S. Leung e R. Bendayan, "Uptake properties of lamivudine (3TC) by a continuous renal epithelial cell line", CAN J PHYSL, 79(1), 2001, pp. 59-66

Abstract

The purpose of this study was to characterize the renal uptake properties of the cytidine analog and antiretroviral agent 3TC. The uptake of radiolabelled 3TC was measured at 37 degreesC in a continuous porcine renal epithelial cell line (i.e., LLC-PK1 cells) grown as a monolayer on an impermeable support. 3TC (5 muM) uptake (37 degreesC) by the monolayer cells was saturable (K-m = 1.2 +/- 0.2 mM) but not significantly altered by various dideoxynucleoside analog drugs, nucleosides, and nucleoside transport inhibitors, suggesting that a nucleoside transporter is not involved in 3TC uptake. A number of endogenous organic cation probes and inhibitors significantly reduced 3TC uptake by the monolayer cells. Quinine, trimethoprim (TMP), and tetraethylammonium (TEA) inhibited 3TC uptake in a dose dependent manner with IC50 values of 0.6mM, 0.63mM, and 1.9 mM, respectively. In turn, the uptakeof the typical organic cation substrate TEA was inhibited by high concentrations of 3TC. An outwardly directed proton gradient significantly increased the uptake of 3TC by the monolayer cells, suggesting the involvement of aproton exchange process. Conversely, in the presence of monensin, a Na+/Hionophore, the uptake of 3TC was significantly reduced. These results suggest that the uptake of 3TC by a cultured renal epithelium may be mediated by an organic cation-proton exchanger. The observed clinical interaction between 3TC and trimethoprim may be explained by competition for a common renal organic cation tubular transporter.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 22:08:46