Nalazite se na CroRIS probnoj okolini. Ovdje evidentirani podaci neće biti pohranjeni u Informacijskom sustavu znanosti RH. Ako je ovo greška, CroRIS produkcijskoj okolini moguće je pristupi putem poveznice www.croris.hr
izvor podataka: crosbi

Differences in assessment of macrolide interaction with human MDR1 (ABCB1, P-gp) using rhodamine-123 efflux, ATPase activity and cellular accumulation assays (CROSBI ID 165274)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

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

Podaci o odgovornosti

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

engleski

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

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.

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

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

Podaci o izdanju

41 (1)

2010.

86-95

objavljeno

0928-0987

10.1016/j.ejps.2010.05.016

Povezanost rada

Farmacija

Poveznice
Indeksiranost