Benzoxazole-based Zn(II) and Cu(II) Complexes Overcome Multidrug-resistance in Cancer

Spengler Gabriella; Kincses Annamaria; Racz Balint; Varga Borisz; Watanabe Genki; Saijo Ryosuke; Sekiya Hiroshi; Tamai Eiji; Maki Jun; Molnar Joseph; Kawase Masami

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Benzoxazole-based Zn(II) and Cu(II) Complexes Overcome Multidrug-resistance in Cancer

机译：基于苯并恶唑的Zn（II）和Cu（II）配合物克服癌症中的多药抗性

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Background/Aim: Multidrug resistance (MDR) represents a significant impediment to successful cancer treatment. In this study, novel metal [Zn(II), Cu(II), Mg(II), Ni(II), Pd(II), and Ag(I)] complexes of 2-trifluoroacetonyl-benzoxazole previously synthesized and characterized by our group were tested for their MDR-reversing activity in comparison with the free ligands in L5178Y mouse T-lymphoma (MDR) cells transfected with human ATP-binding cassette sub family B member 1 (ABCB1; P-glycoprotein) gene. Materials and Methods: Cytotoxic and antiproliferative effects of the complexes were assessed by the thiazolyl blue tetrazolium bromide (MTT) method. Modulation of ABCB1 activity was measured by rhodamine 123 accumulation assay using flow cytometry. The apoptosis-inducing activity of some complexes was also tested on the multidrug resistant L5178Y mouse T-lymphoma cells, using the annexin-V/propidium iodide assay. Results: When compared to the free ligand, a remarkable enhancement in MDR reversal and cytotoxic activity was found for the Zn(II) and Cu(II) complexes. The activity of the complexes proved to be up to 29- and 5-fold higher than that of the ligands and the ABCB1 inhibitor verapamil as positive control, respectively. The complexes possessed a remarkable potential to induce apoptosis of MDR cells. Conclusion: Our results suggest that the Zn(II) and Cu(II) complexes display significant MDR-reversing activity in a dose-dependent manner and possess strong cytotoxic activity and a remarkable potential to induce apoptosis in MDR L5178Y mouse T-lymphoma cells.

机译：背景/目的：多药耐药性（MDR）代表成功癌症治疗的重大障碍。在该研究中，新的金属[Zn（II），Cu（II），Mg（II），Ni（II），Pd（II），和Ag（I）]复合物的2-三氟乙酰苯并恶唑先前合成和特征在一起与用L5178Y小鼠T淋巴瘤（MDR）细胞的游离配体相比，我们的MDR逆转活性测试了他们的MDR逆转活性，与人ATP结合盒亚家族B会员1（ABCB1; p-糖蛋白）基因转染。材料和方法：通过噻唑基蓝四溴溴化物（MTT）方法评估复合物的细胞毒性和抗增殖效应。使用流式细胞术通过罗丹明123累积测定法测量ABCB1活性的调节。使用附睾-V /碘化丙啶测定，在多药抗性L5178Y小鼠T淋巴瘤细胞上还测试了一些复合物的凋亡诱导活性。结果：与自由配体相比，发现MDR反转和细胞毒活性的显着增强用于Zn（II）和Cu（II）配合物。复合物的活性分别被证明高达29-和5倍，分别高于配体和ABCB1抑制剂维拉帕米作为阳性对照。复合物具有诱导MDR细胞凋亡的显着潜力。结论：我们的研究结果表明，Zn（II）和Cu（II）复合物以剂量依赖性方式显示出显着的MDR反转活性，并具有强烈的细胞毒性活性，并且具有诱导MDR L5178Y小鼠T淋巴瘤细胞凋亡的显着潜力。

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来源
《Anticancer Research: International Journal of Cancer Research and Treatment》 |2018年第11期|共7页
作者
Spengler Gabriella; Kincses Annamaria; Racz Balint; Varga Borisz; Watanabe Genki; Saijo Ryosuke; Sekiya Hiroshi; Tamai Eiji; Maki Jun; Molnar Joseph; Kawase Masami;
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作者单位

Univ Szeged Dept Med Microbiol &

Immunobiol Fac Med Szeged Hungary;

Univ Szeged Dept Med Microbiol &

Immunobiol Fac Med Szeged Hungary;

Univ Szeged Dept Med Microbiol &

Immunobiol Fac Med Szeged Hungary;

Univ Szeged Dept Med Microbiol &

Immunobiol Fac Med Szeged Hungary;

Matsuyama Univ Fac Pharmaceut Sci 4-2 Bunkyo Cho Matsuyama Ehime 7908578 Japan;

Matsuyama Univ Fac Pharmaceut Sci 4-2 Bunkyo Cho Matsuyama Ehime 7908578 Japan;

Matsuyama Univ Dept Infect Dis Coll Pharmaceut Sci Matsuyama Ehime Japan;

Matsuyama Univ Dept Infect Dis Coll Pharmaceut Sci Matsuyama Ehime Japan;

Matsuyama Univ Dept Infect Dis Coll Pharmaceut Sci Matsuyama Ehime Japan;

Univ Szeged Dept Med Microbiol &

Immunobiol Fac Med Szeged Hungary;

Matsuyama Univ Fac Pharmaceut Sci 4-2 Bunkyo Cho Matsuyama Ehime 7908578 Japan;

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正文语种 eng
中图分类肿瘤学;
关键词
Multidrug resistance; metal complex; benzoxazole; ABCB1; P-glycoprotein; mouse T-lymphoma; apoptosis;

机译：多药抗性;金属络合物;苯并恶唑;ABCB1;p-糖蛋白;小鼠T淋巴瘤;细胞凋亡;

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1. Benzoxazole-based Zn(II) and Cu(II) Complexes Overcome Multidrug-resistance in Cancer [J] . Spengler Gabriella, Kincses Annamaria, Racz Balint, Anticancer Research: International Journal of Cancer Research and Treatment . 2018,第11期

机译：基于苯并恶唑的Zn（II）和Cu（II）配合物克服癌症中的多药抗性
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Benzoxazole-based Zn(II) and Cu(II) Complexes Overcome Multidrug-resistance in Cancer

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