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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Synthesis, anti-proliferative and apoptosis-inducing studies of palladacycles containing a diphosphine and a Sn, As-based chelate ligand
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Synthesis, anti-proliferative and apoptosis-inducing studies of palladacycles containing a diphosphine and a Sn, As-based chelate ligand

机译：含有二膦和Sn的钯和Sn，螯合配体的合成，抗增殖和凋亡诱导研究

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摘要

Cleavage of the bromide bridges in [Pd2(mu-Br)(2){kappa(2)(Sn, As)-2-MeBrSnC6F4AsPh2}(2)] (1) by diphosphine ligands gave the mono-and dinuclear palladacycles [Pd(L) Br{kappa(2)(Sn, As)-2-MeBrSnC(6)F(4)AsP(h)2}] [L = dppe (2) dppm (3), ortho-dppBz (4)] and [Pd2Br2(para-dppBz){kappa(2)(Sn, As)-2-MeBrSnC6F4AsPh2}(2)] (5). The interactions of these complexes with DNA (CT-DNA) and proteins (human serum albumin) were studied by UV-Vis and fluorescence spectroscopy, respectively. The results confirmed the interaction of these palladium complexes with CT-DNA through groove binding, and their strong binding affinity to HSA. The anti-proliferative activities of complexes 1-5 were tested against four human cancer cell lines (HeLa, A549, PC-3, and HT1080) and normal keratinocytes (HaCaT). Among the series, the palladium(II) complex containing the 1,2-bis(diphenylphosphino) benzene ligand (4) showed the highest cytotoxicity against HeLa, PC-3 and HT1080 cells, with IC50 values of 0.25 +/- 0.08, 0.85 +/- 0.11, and 0.66 +/- 0.15 mu M, respectively. Interestingly, compound 4 exhibited lower cytotoxic activity toward normal HaCaT cells (IC50 = 4.65 +/- 0.16 mu M). Additionally, this complex exhibited lower toxicity and better anti-cancer activity than cisplatin. Further mechanistic studies, including Hoechst staining and flow cytometry, confirmed that complex 4 induced G2/M phase cell cycle arrest and apoptotic cell death in HeLa cells.
机译：二膦配体的[PD2（MU-BR）（2）（2）（2）（2）（2）（2）（SN，AS）-2-MEBRSNC6F4ASPH2}（2）]（2）]（1）中的溴化物桥的切割给予单核钯粘连[PD （L）BR {kappa（2）（SN，AS）-2-MEBRSNC（6）F（4）ASP（H）2}] [L = DPPE（2）DPPM（3），Ortho-DPPBZ（4） [pd2br2（para-dppbz）{kappa（2）（sn，As）-2-mebrsnc6f4asph2}（2）]（5）。通过UV-Vis和荧光光谱法分别研究了这些配合物与DNA（CT-DNA）和蛋白质（人血清白蛋白）的相互作用。结果证实了这些钯配合物与CT-DNA通过沟槽结合的相互作用，以及它们对HSA的强结合亲和力。复合物1-5的抗增殖活性针对四种人癌细胞系（Hela，A549，PC-3和HT1080）和正常角质形成细胞（HACAT）进行测试。在该系列中，含有1,2-双（二苯基膦基）苯配体（4）的钯（II）络合物显示出对HELA，PC-3和HT1080细胞的最高细胞毒性，IC50值为0.25 +/- 0.08,0.85 +/- 0.11和0.66 +/- 0.15 mu m。有趣的是，化合物4表现出朝向正常HACAT细胞的细胞毒性活性（IC50 = 4.65 +/-0.16μm）。此外，这种复杂性表现出低于顺铂的毒性和更好的抗癌活性。进一步的机械研究，包括Hoechst染色和流式细胞术，证实了综合体4诱导的G2 / M期细胞周期停滞和HeLa细胞中的凋亡细胞死亡。

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