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Titolo:
INTERACTION OF STRUCTURALLY DIVERSE PESTICIDES WITH THE HUMAN MDR1 GENE-PRODUCT P-GLYCOPROTEIN
Autore:
BAIN LJ; LEBLANC GA;
Indirizzi:
N CAROLINA STATE UNIV,DEPT TOXICOL,BOX 7633 RALEIGH NC 27695
Titolo Testata:
Toxicology and applied pharmacology
fascicolo: 1, volume: 141, anno: 1996,
pagine: 288 - 298
SICI:
0041-008X(1996)141:1<288:IOSDPW>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
MULTIDRUG-RESISTANCE GENE; MULTIXENOBIOTIC RESISTANCE; FUNCTIONAL-ROLE; CYTO-TOXICITY; EXPRESSION; CELLS; RAT; CHOLESTASIS; BINDING; TISSUES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
L.J. Bain e G.A. Leblanc, "INTERACTION OF STRUCTURALLY DIVERSE PESTICIDES WITH THE HUMAN MDR1 GENE-PRODUCT P-GLYCOPROTEIN", Toxicology and applied pharmacology, 141(1), 1996, pp. 288-298

Abstract

P-glycoprotein (P-gp) is a 170-kDa membrane-bound glycoprotein shown to efflux a wide variety of chemicals, such as chemotherapeutic agentsand carcinogens. Experiments were conducted using B16/F10 murine melanoma cells transfected with the human MDR1 gene (B16/hMDR1 cells), which codes for P-gp, to determine whether this transporter may contribute to the cellular efflux of some pesticides, Thirty-eight pesticides representing several classes of compounds were evaluated for their potential to bind to P-gp, as measured by the inhibition of efflux of the P-gp substrate doxorubicin, Carbamate and pyrethroid insecticides exhibited little interaction with P-gp, while many of the organophosphorusand organochlorine pesticides significantly inhibited the efflux of doxorubicin. Pesticides that significantly inhibited the efflux of doxorubicin were then assessed for P-gp-mediated efflux. One pesticide, endosulfan, exhibited slight though significant transport mediated by P-gp, Competition experiments performed with the P-glycoprotein ligand [H-3]azidopine demonstrated that the P-gp inhibitory pesticides bound to P-gp, Both lipophilicity and molecular mass were major physical/chemical determinants in dictating pesticide binding to P-gp, with optimumbinding occurring with compounds having a log K-ow value of 3.6-4.5 and a molecular weight of 391-490 Da, The transport substrate endosulfan possessed optimal binding characteristics. These results demonstrated that many pesticides are capable of binding to P-gp; however, binding does not infer transport. (C) 1996 Academic Press, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 13/07/20 alle ore 11:09:59