کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2481704 1556258 2009 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Expression and activity of the efflux transporters ABCB1, ABCC2 and ABCG2 in the human colorectal carcinoma cell line LS513
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Expression and activity of the efflux transporters ABCB1, ABCC2 and ABCG2 in the human colorectal carcinoma cell line LS513
چکیده انگلیسی

The human colorectal carcinoma cell line LS513 exhibits epithelial morphology, adherent properties and can grow subcutaneously to form tumors in nude mice. Thus, it is a potential model for mouse xenograft efficacy studies. The present study characterized the expression and activity of P-gp, BCRP and MRP2 in LS513 cells.We investigated the expression of these ATP-binding cassette transporters by Western blot and their activity was also examined using cell culture inserts, where the LS513 cells were grown to confluence for 9 days. The transport of model substrates of P-gp (amprenavir, ritonavir and topotecan), BCRP (topotecan) and MRP2 (SN-38) was studied in the apical to basolateral (A–B) and basolateral to apical (B–A) directions. P-gp, BCRP and MRP2 could be detected by western blot. The LS513 cells exhibited markedly higher transport in the B–A direction than in the A–B direction for the probe substrates tested, with efflux ratios (ERs; B–A/A–B) of 10, 21, 40 and 50 for amprenavir, ritonavir, topotecan and SN38, respectively. The ER could be significantly reduced with the addition of inhibitors of P-gp (GF120918), BCRP (FTC), and MRP2 (MK571), confirming the activity of these transporters in the LS513 cells.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 37, Issues 3–4, 28 June 2009, Pages 463–468
نویسندگان
, , ,