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The Influence of the Nature of the Ligand on the Antitumor Activity and Cytotoxic Effect of Binuclear Dinitrosyl Iron Complexes
Biophysics Pub Date : 2020-09-01 , DOI: 10.1134/s0006350920050206
A. F. Vanin , L. A. Ostrovskaya , D. B. Korman , E. I. Nekrasova , O. O. Riabaya , N. V. Bluhterova , V. A. Rykova , M. M. Fomina

The influence of the nature of the ligands of nitric oxide-generating compounds, such as binuclear dinitrosyl iron complexes containing glutathione or mercaptosuccinate, on their tumor growth-inhibiting and cytotoxic effects has been studied in vivo and in vitro. The antitumor effect of the complex with glutathione exceeds that exerted by the complex with mercaptosuccinate. These complexes inhibit tumor growth (Lewis lung carcinoma) by 90 and 65%, respectively, compared to the control. These complexes are weakly cytotoxic against the MCF-7 human cancer cell line. The half-maximum inhibitory concentration of the complex with mercaptosuccinate at which the survival of cells is reduced by 50% (IC50) is 0.8 μmol/mL (640 μg/mL), whereas in the case of the complex with glutathione it is 2 μmol/mL (1600 μg/mL). It is assumed that the antitumor activity of iron complexes is determined by their ability to enter immunocompetent cells, which provide a direct route to tumor tissues.

中文翻译:

配体性质对双核二亚硝基铁配合物抗肿瘤活性和细胞毒作用的影响

体内和体外研究了产生一氧化氮的化合物的配体性质对它们的肿瘤生长抑制和细胞毒作用的影响,例如含有谷胱甘肽或巯基琥珀酸盐的双核二亚硝酰基铁配合物。谷胱甘肽复合物的抗肿瘤作用超过巯基琥珀酸盐复合物的抗肿瘤作用。与对照相比,这些复合物分别抑制了 90% 和 65% 的肿瘤生长(刘易斯肺癌)。这些复合物对 MCF-7 人癌细胞系的细胞毒性较弱。细胞存活率降低 50% (IC50) 时,巯基琥珀酸盐复合物的半数抑制浓度为 0.8 μmol/mL (640 μg/mL),而与谷胱甘肽复合物的半数抑制浓度为 2 μmol /mL (1600 μg/mL)。
更新日期:2020-09-01
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