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DiOC2(3) Is Not a Substrate for Multidrug Resistance Protein (MRP)-mediated Drug Efflux

DiOC2(3) Is Not a Substrate for Multidrug Resistance Protein (MRP)-mediated Drug Efflux

H Minderman, U Vanhoefer, K Toth, M B Yin, M D Minderman, C Wrzosek, M L Slovak, Y M Rustum

Cytometry. 1996 Sep 1;25(1):14-20.

PMID: 8875050

Abstract:

Multidrug resistance (MDR) is often related to expression of P-glycoprotein (Pgp) or Multidrug Resistance Protein (MRP). Pgp-mediated MDR can be evaluated by determining cellular retention of fluorescent substrates by flow cytometry. This study determined if agents used to evaluate Pgp function also can be used to evaluate MRP function. Cellular retention of doxorubicin (Dox), Rhodamine-123 (Rh-123), and 3,3'-diethyloxacarbocyanine iodide (DiOC2(3)) were studied in MRP-expressing cell lines (HL60/Adr and HT1080/DR4), whereas a Pgp expressing cell line (A2780/Dx5) served as a positive control. Overexpression of Pgp correlated inversely with retention of Dox, Rh-123, and DiOC2(3); however, under identical experimental conditions (1 h reincubation in drug-free medium), no retention difference of the three agents was detected between parental and MRP-expressing resistant cells. Upon extending the reincubation time to 4 h, an efflux of Rh-123 and Dox in the resistant lines became apparent and even more pronounced after 24h; however, still no efflux was detectable for DiOC2(3). Incubation of the cells with a modulator of MDR, PAK-104P, negated the observed drug efflux in Pgp and MRP expressing cells, which correlated with increased sensitivity of the MDR lines to doxorubicin. Thus both Dox and Rh-123 can be used to evaluate MRP-function, but DiOC2(3) can not.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP905964	3,3′-Diethyloxacarbocyanine iodide		905-96-4	Price

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