کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8548039 | 1561734 | 2018 | 28 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Nobiletin bioactivation in MDA-MB-468 breast cancer cells by cytochrome P450 CYP1 enzymes
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کلمات کلیدی
IC50CYP13-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide - 3- (4،5-dimethylthiazol-2-yl) -2،5-difenyltetrazolium bromide50% inhibitory concentration - 50٪ غلظت مهاریMTT - MTTBreast cancer - سرطان پستانFlavonoids - فلاونوئیدهاAntiproliferation - مبارزه با انفجارNobiletin - نوبیلتینHigh pressure liquid chromatography - کروماتوگرافی مایع با فشار بالاHPLC - کروماتوگرافی مایعی کارا
موضوعات مرتبط
علوم زیستی و بیوفناوری
علوم کشاورزی و بیولوژیک
دانش تغذیه
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Nobiletin is a fully methoxylated flavone that has demonstrated anticancer activity via multiple modes of action. In the present study, the metabolism and further antiproliferative activity of nobiletin was evaluated in the CYP1 expressing human breast cancer cell line MDA-MB-468 and the normal breast cell line MCF10A. Nobiletin was metabolized in MDA-MB-468â¯cells to a single-demethylated derivative assigned NP1. This metabolite was absent in MCF10A cells that did not express CYP1 enzymes. Nobiletin exhibited submicromolar IC50 (0.1â¯Â±â¯0.04â¯Î¼M) in MDA-MB-468â¯cells, whereas it was considerably less active in MCF10A cells (40â¯Î¼M). In MDA-MB-468â¯cells that were coincubated with the CYP1 inhibitor acacetin, an approximately 300-fold increase was noted in the IC50 (30â¯Â±â¯2.4â¯Î¼M) of nobiletin. In the presence of the CYP1 inhibitor acacetin, the conversion of nobiletin to NP1 was significantly reduced in MDA-MB-468â¯cells. Furthermore, a significant increase was noted in the population of the cells at the G1 phase, following treatment with nobiletin (10â¯Î¼M) for 24â¯h compared with the control cells treated with DMSO (0.1%) alone (55.9â¯Â±â¯0.14 vs. 45.6â¯Â±â¯1.96), whereas the cell cycle of MCF10A cells was not significantly altered under the same treatment conditions. Taken collectively, the results suggest that nobiletin is selectively bioactivated in MDA-MB-468 breast cancer cells via metabolism by the cytochrome P450 CYP1 family of enzymes.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Food and Chemical Toxicology - Volume 113, March 2018, Pages 228-235
Journal: Food and Chemical Toxicology - Volume 113, March 2018, Pages 228-235
نویسندگان
Somchaiya Surichan, Randolph R. Arroo, Ketan Ruparelia, Aristidis M. Tsatsakis, Vasilis P. Androutsopoulos,