کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2533401 1559049 2010 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Cytotoxic efficacy of a novel dinuclear platinum(II) complex in human breast cancer cells
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
Cytotoxic efficacy of a novel dinuclear platinum(II) complex in human breast cancer cells
چکیده انگلیسی

Evaluation of the cytotoxicity of a novel dinuclear platinum(II) complex of formula Pt2(2-picoline)4(berenil)2 employing a MTT assay and inhibition of [3H]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 breast cancer cells demonstrated that the complex was more of a potent antiproliferative agent than cisplatin. The DNA-binding ability of Pt2(2-picoline)4(berenil)2 estimated by an ethidium displacement assay indicated that the complex showed strong specificity for AT base pairs in the minor groove of DNA. Our study showed that Pt2(2-picoline)4(berenil)2 was a potent catalytic inhibitor of topoisomerase II in opposition to cisplatin. Pt2(2-picoline)4(berenil)2 was found to be a more active inhibitor of collagen biosynthesis than cisplatin. The up regulation of β1-integrin and insulin-like growth factor I (IGF-I) receptor expression by the complex was shown to be accompanied by an increase in the expression of mitogen activated protein kinases in breast cell lines. The phenomenon was related to the increased expression of nuclear factor-kappaB (ΝF-κΒ) by Pt2(2-picoline)4(berenil)2 as shown by the Western immunoblot analysis. Flow cytometric analysis and a fluorescent microscopy assay demonstrated that cell death appeared to result from apoptosis, with the possibility of secondary necrosis. The data presented suggested that Pt2(2-picoline)4(berenil)2 impaired growth and metabolism of breast cancer cells more efficiently than cisplatin. These results indicated also the different properties of Pt2(2-picoline)4(berenil)2 and cisplatin.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 643, Issue 1, 15 September 2010, Pages 34–41
نویسندگان
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