کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2525513 | 1119617 | 2009 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Reversal effect of substituted 1,3-dimethyl-1H-quinoxalin-2-ones on multidrug resistance in adriamycin-resistant K562/A02 cells
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
پزشکی و دندانپزشکی
تومور شناسی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Reversal effect of substituted 1,3-dimethyl-1H-quinoxalin-2-ones on multidrug resistance in adriamycin-resistant K562/A02 cells Reversal effect of substituted 1,3-dimethyl-1H-quinoxalin-2-ones on multidrug resistance in adriamycin-resistant K562/A02 cells](/preview/png/2525513.png)
چکیده انگلیسی
QA1 and QA3 are the derivatives of substituted 1,3-dimethyl-1H-quinoxalin-2-ones that may selectively antagonize P-glycoprotein (P-gp) in multidrug resistance (MDR) cancer cells. Herein, we examined the reversal effect of two compounds on MDR in adriamycin (Adr)-induced resistant K562/A02 cells. MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) assay showed that QA1 and QA3 weakly inhibited the growth of tumor cells. However, the compounds increased Adr-induced cytotoxicity toward K562/A02 cells. The IC50 values of Adr toward K562/A02 were decreased in the presence of QA1 or QA3. The maximal reversal fold (RF) of QA1 and QA3 was reached 6.9 and 9.0, respectively. The action of QA1 and QA3 was also confirmed by the increase of intracellular Adr accumulation in K562/A02 cells. In mechanism study, the intracellular accumulation and efflux of Rh123 were measured using multilabel counter with excitation/emission wavelengths of 485/535Â nm. An increase of intracellular Rh123 and the decrease of efflux were observed in K562/A02 cells incubation with QA1 or QA3, indicating that the activity of P-gp was blocked. These results suggested that the derivatives of substituted 1,3-dimethyl-1H-quinoxalin-2-ones might reverse MDR in K562/A02 cells via inhibition activity of P-gp. QA1 and QA3 might be the candidate agents for reversing MDR of cancer.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biomedicine & Pharmacotherapy - Volume 63, Issue 3, March 2009, Pages 202-208
Journal: Biomedicine & Pharmacotherapy - Volume 63, Issue 3, March 2009, Pages 202-208
نویسندگان
Li-rui Sun, Xun Li, Yan-na Cheng, Hong-yu Yuan, Ming-hui Chen, Wei Tang, Stephen Geoffrey Ward, Xian-jun Qu,