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MDR1 polymorphisms G2677T in exon 21 and C3435T in exon 26 fail to affect rhodamine 123 efflux in peripheral blood lymphocytes
Author(s) -
Oselin Kersti,
Gerloff Thomas,
Mrozikiewicz Przemyslaw M.,
Pähkla Rein,
Roots Ivar
Publication year - 2003
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1046/j.1472-8206.2003.00163.x
Subject(s) - efflux , rhodamine 123 , p glycoprotein , biology , flow cytometry , microbiology and biotechnology , whole blood , rhodamine , single nucleotide polymorphism , genotype , exon , pharmacology , endocrinology , gene , genetics , immunology , fluorescence , multiple drug resistance , drug resistance , physics , quantum mechanics
P‐glycoprotein (Pgp) is a member of the ABC‐transporter family, and in humans, is encoded by the MDR1 gene. Recently, several single‐nucleotide polymorphisms in the MDR1 gene were identified. The aim of the present study was to evaluate the effect of the MDR1 genetic polymorphisms G2677T and C3435T on Pgp activity in CD56 + and CD4 + peripheral blood cells. Using flow cytometry, rhodamine 123 (Rh123) efflux was determined in 46 male healthy volunteers. Median Rh123 fluorescence in control sample, after baseline dye uptake, was set as 100%. Rh123 fluorescence in efflux samples, exposed to different efflux periods, was used to calculate the percentage of Rh123 retained in the cells in comparison with control. There was no significant difference in Rh123 efflux in CD56 + cells after 5, 10, 15, and 30 min efflux between individuals with different MDR1 genotypes. Also, in CD4 + cells after 15, 30, 60, and 90 min, Rh123 efflux did not reveal statistically different results for the three genotypes at 2677 and 3435. Rh123 efflux was not enhanced by a 10‐day rifampin administration, as determined in 15 individuals before and after rifampin treatment. In conclusion, we found no impact of the MDR1 G2677T and C3435T polymorphisms on Pgp activity in CD56 + and CD4 + peripheral blood lymphocytes.