Possible involvement of P-glycoprotein in the biliary excretion of grepafloxacin

Clinical and Experimental Pharmacology & Physiology
Ying Lan ZhaoTakaaki Hasegawa

Abstract

1. In the present study, we have examined the effects of the quinolones norfloxacin (NFLX), enoxacin (ENX), ofloxacin (OFLX), tosufloxacin (TFLX), lomefloxacin (LFLX), sparfloxacin (SPFX) and grepafloxacin (GPFX) on the efflux of doxorubicin from mouse leukaemia P388/ADR cells expressing P-glycoprotein. The relationship between their partition coefficients (hydrophobicity) and effluxing potencies was also elucidated. 2. Both TFLX and SPFX strongly increased the intracellular accumulation of doxorubicin (5 micromol/L) in P388/ADR cells, but had no effect on P388/S cells not expressing P-glycoprotein. The rank of order of the potency of the quinolones (TFLX > SPFX > GPFX > NFLX) was not related directly to their hydrophobicity. These results suggest that some quinolones can reverse anticancer drug resistance. 3. Because GPFX is more highly excreted into the bile than other known quinolones, the effects of doxorubicin (10 mg/kg) or the well-known inhibitors of P-glycoprotein, namely cyclosporine A (10 mg/kg) and erythromycin (100 mg/kg), on the biliary excretion of GPFX at steady state was studied in rats. 4. Doxorubicin, cyclosporine A and erythromycin significantly decreased the biliary clearance of GPFX. Cyclosporine A and eryt...Continue Reading

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Citations

Jan 28, 2004·European Journal of Pharmacology·Emiko AsakuraTakaaki Hasegawa
Dec 12, 2003·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·J L C M DorneA G Renwick
Jun 18, 2002·European Journal of Pharmacology·Ying Lan ZhaoTakaaki Hasegawa
Apr 18, 2002·Antimicrobial Agents and Chemotherapy·Ying Lan ZhaoTakaaki Hasegawa
Jun 2, 2009·Biological & Pharmaceutical Bulletin·Masafumi OhnishiTakaaki Hasegawa
Jun 2, 2009·Biological & Pharmaceutical Bulletin·Makoto AokiMasahiro Hayashi
May 28, 2010·Expert Opinion on Drug Metabolism & Toxicology·Eva ChoongChin B Eap
Jul 7, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Jh HuHy Liu
Jan 18, 2008·Journal of Pharmaceutical Sciences·Ana I AlvarezGracia Merino
Jan 11, 2007·British Journal of Pharmacology·J A Schrickx, J Fink-Gremmels
Jul 22, 2008·Journal of Veterinary Pharmacology and Therapeutics·A M HaritovaJ Fink-Gremmels
Oct 7, 2004·European Journal of Pharmacology·Akemi ShimizuTakaaki Hasegawa
Aug 3, 2010·Journal of Infection and Chemotherapy : Official Journal of the Japan Society of Chemotherapy·Tamon HayashiTakaaki Hasegawa
Oct 3, 2006·Biochimica Et Biophysica Acta·Valerie Gouaze-Andersson, Myles C Cabot
Nov 16, 2004·American Journal of Therapeutics·Vineet SikriAshim K Mitra

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