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Pregled bibliografske jedinice broj: 478469

Differences in assessment of macrolide interaction with human MDR1 (ABCB1, P-gp) using rhodamine-123 efflux, ATPase activity and cellular accumulation assays


Munić, Vesna; Krelnerić, Željko; Mikac, Lara; Eraković Haber, Vesna
Differences in assessment of macrolide interaction with human MDR1 (ABCB1, P-gp) using rhodamine-123 efflux, ATPase activity and cellular accumulation assays // European journal of pharmaceutical sciences, 41 (2010), 1; 86-95 doi:10.1016/j.ejps.2010.05.016 (međunarodna recenzija, članak, znanstveni)


Naslov
Differences in assessment of macrolide interaction with human MDR1 (ABCB1, P-gp) using rhodamine-123 efflux, ATPase activity and cellular accumulation assays

Autori
Munić, Vesna ; Krelnerić, Željko ; Mikac, Lara ; Eraković Haber, Vesna

Izvornik
European journal of pharmaceutical sciences (0928-0987) 41 (2010), 1; 86-95

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Macrolide; MDR1; P-gp; P-glycoprotein; ABCB1; Cellular accumulation; Rhodamine-123 efflux; ATPase activity; MES-SA/Dx5; ABC transporter; Azithromycin; Erythromycin; Clarithromycin; Roxithromycin; Telithromycin

Sažetak
In this study five macrolide antibiotics (azithromycin, erythromycin, clarithromycin, roxithromycin and telithromycin) were compared based on their ability to interact with human MDR1 (ABCB1, Pglycoprotein), studied from two main aspects: by determining the influence of macrolide antibiotics on MDR1 function, as well as the influence of MDR1 on macrolide accumulation in MES-SA/Dx5 cells overexpressing human MDR1. At higher micromolar concentrations five tested macrolides were shown to inhibit MDR1 function in terms of rhodamine-123 efflux and verapamil-activated ATPase function, whereas at lower concentrations they activated MDR1 ATPase. They were confirmed to be substrates of MDR1 and to compete with each other, as well as with verapamil for transport via this transporter. Expression of MDR1 on cells decreased macrolide accumulation in cells from 2- to 80-fold with the most pronounced change observed for azithromycin and erythromycin. Moreover, presence of active MDR1 highly affected the relative ranking of tested macrolides according to their accumulation in cells. In conclusion, out of seven applied methods and assessed parameters, four of them gave similar rough evaluation on the strength of interaction of five macrolides with MDR1, with clarithromycin, roxithromycin and telithromycin showing stronger interaction than azithromycin and erythromycin.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija



POVEZANOST RADA


Ustanove
Fidelta d.o.o.

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


Uključenost u ostale bibliografske baze podataka:


  • EMBASE (Excerpta Medica)


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