Diethylenetriamine Pentaacetic Acid Derivative of Toremifene and In Vitro Evaluation in Human Breast Cancer Cell Line MCF-7

作者：Kilcar Ayfer Yurt^*; Muftuler F Zumrut Biber; Unak Perihan; Avci Cigir Biray; Gunduz Cumhur

来源：Cancer Biotherapy and Radiopharmaceuticals, 2011, 26(1): 105-111.

DOI：10.1089/cbr.2010.0860

• Breast tissue
• MCF-7 cell line
• TOR-DTPA
• toremifene (TOR)

Cytotoxic and apoptotic effects of toremifene-diethylenetriamine pentaacetic acid (TOR-DTPA), formed by conjugation of TOR and DTPA, on the MCF-7 cell line were evaluated. TOR-DTPA was synthesized and qualified via gas chromatography-mass spectrometry system, thin layer chromatography, and high performance liquid chromatography methods. To screen the biological properties of TOR-DTPA at determined concentrations, our ongoing effort was to evaluate apoptotic and cytotoxic effects on the MCF-7 cell line. Trypan blue dye exclusion test, XTT, ELISA, and TUNEL assays were utilized to evaluate cytotoxicity and apoptosis. TOR-DTPA has no cytotoxic and limited apoptotic effect on the MCF-7 cell line according to the results of in vitro studies. It is concluded that the lack of obvious apoptotic and cytotoxic effects allows the already proposed ligand, TOR-DTPA, to be improved as a novel hydrophilic ligand for breast imaging.

• 出版日期2011-2