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首页> 外文期刊>RSC Advances >Impact of chelation on anticancer activities of organometallic ruthenium(ii) complexes containing 2,5-di(1H-pyrazol-1-yl)-1,4-benzoquinone: synthesis, structure, DNA/protein binding, antioxidant activity and cytotoxicity
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Impact of chelation on anticancer activities of organometallic ruthenium(ii) complexes containing 2,5-di(1H-pyrazol-1-yl)-1,4-benzoquinone: synthesis, structure, DNA/protein binding, antioxidant activity and cytotoxicity

机译：螯合对含有2,5-二（1H-吡唑-1-基）-1,4-苯醌：合成，结构，DNA /蛋白结合，抗氧化活性和细胞毒性的影响对含有2,5-二（1H-吡唑-1-基）的抗癌络合物的影响

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To gain some insight into the influence of chelation on anticancer activities, two new bivalent organometallic ruthenium complexes, [Ru(L)Cl(CO)(PPh _(3) ) _(2) ] ( 3 ) and [Ru(L)Cl(CO)(AsPh _(3) ) _(2) ] ( 4 ), (HL = 2,5-di(1 H -pyrazol-1-yl)-1,4-benzoquinone) were synthesized, structurally characterized comprehensively by elemental analysis, IR, electronic, ~(1) H/ ~(13) C NMR spectral studies and their biological activities (DNA/protein interactions, antioxidant and cytotoxic activity studies) have been investigated and compared with that of appropriate precursor complexes [RuHCl(CO)(PPh _(3) ) _(3) ] ( 1 ), [RuHCl(CO)(AsPh _(3) ) _(3) ] ( 2 ) and the ligand LH . The crystal structures of both the new complexes 3 and 4 were determined by single crystal X-ray diffraction studies, which unveil that the central ruthenium ion adopted distorted octahedral geometry with L as a monobasic bidentate donor and the chelator was observed to undergo C–H activation at one of the ortho positions leading to the formation of a five-membered metallacycle. DNA/protein interactions of the complexes have been examined by photophysical studies, which demonstrated a non-intercalative binding mode of the complexes with DNA and the complexes strongly quench the fluorescence intensity of bovine serum albumin (BSA) through the mechanism of static quenching. The new complexes demonstrated better binding affinity with DNA/protein. The compounds were evaluated for their free radical scavenging ability involving DPPH radicals, hydroxyl radicals, nitric oxide radicals, superoxide anion radicals and hydrogen peroxide. The results showed that the new complexes 3 and 4 possess significant radical scavenging ability and outperform the standard antioxidants vitamin C and BHT. The results of in vitro cytotoxicity of the complexes tested against B16F10, HeLa, A549, MCF7 and SKOV3 cells by SRB assay were compared with the standard drug cisplatin and that the new complexes 3 and 4 showed better activity in inhibiting the growth of the cancer cells. The influence of chelation was seen in all the biological activities studied and the new ruthenium chelates 3 and 4 were found to be superior to the precursor complexes 1 , 2 and the ligand LH in DNA/protein binding properties, radical scavenging ability and cytotoxicity.
机译：为了探讨螯合对抗癌活性的影响，两种新的二价有机金属钌配合物，[Ru（l）cl（co）（pph _（3））_（2）]（3）和[ru（l） Cl（CO）（沥青_（3））_（2）]（4），（HL = 2,5-DI（1 H-戊唑-1-基）-1,4-苯醌）被合成，结构表征通过元素分析，IR，电子，〜（1）H /〜（13）C NMR光谱研究及其生物活性（DNA /蛋白质相互作用，抗氧化剂和细胞毒性活性研究）并与适当的前体复合物进行了研究[RuHCl（CO）（PPH _（3））_（3）]（1），[RuHCl（CO）（Asph _（3））_（3）]（2）和配体LH。通过单晶X射线衍射研究确定新复合物3和4的晶体结构，其推出中央钌离子采用扭曲的八面体几何形状与L作为单母生双齿供体，观察到螯合剂经历C-H.在一个邻位的激活导致形成五元金属族的形成。通过光学学研究检查了复合物的DNA /蛋白质相互作用，其表现出与DNA的复合物的非平插性结合模式，并且复合物通过静电猝灭的机理强烈终止牛血清白蛋白（BSA）的荧光强度。新复合物与DNA /蛋白质表现出更好的结合亲和力。评价化合物的自由基清除能力，涉及DPPH基团，羟基自由基，一氧化氮基，超氧化物阴离子和过氧化氢。结果表明，新的配合物3和4具有显着的自由基清除能力，优于标准抗氧化剂维生素C和BHT。与B16F10，Hela，A549，MCF7和SKOV3细胞测试的复合物的体外细胞毒性的结果与标准药物顺铂进行比较，并且新的复合物3和4显示更好的活性抑制癌细胞的生长。在研究的所有生物活性中可以看到螯合的影响，并发现新的钌螯合物3和4优于前体复合物1,2和DNA /蛋白结合性能，自由基清除能力和细胞毒性的配体LH。

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