英语翻译Herein,we present a new Pt-Gd complex that caneffectively target the nuclei of tumor cells by means of afunctionalized dtpa ligand linked to two {PtII(terpy)} (terpy=2,2’:6’,2’’-terpyridine) units that have the capacity to bindDNA

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英语翻译Herein,wepresentanewPt-Gdcomplexthatcaneffectivelytargetthenucleioftumorcellsbymeansofafunctiona

英语翻译Herein,we present a new Pt-Gd complex that caneffectively target the nuclei of tumor cells by means of afunctionalized dtpa ligand linked to two {PtII(terpy)} (terpy=2,2’:6’,2’’-terpyridine) units that have the capacity to bindDNA
英语翻译
Herein,we present a new Pt-Gd complex that can
effectively target the nuclei of tumor cells by means of a
functionalized dtpa ligand linked to two {PtII(terpy)} (terpy=
2,2’:6’,2’’-terpyridine) units that have the capacity to bind
DNA in an intercalative manner.[22–24] Based on prior work
with analogous Pt–Ln complexes (Ln=La,Nd,Eu),which
were designed to act as luminescent probes for DNA
recognition,[24] we reasoned that the related Pt-Gd species 1
would have the capacity to deliver gadolinium to this
important biomolecule.In this work,we report the first
unequivocal example of gadolinium delivery to a tumor-cell
nucleus by a platinum complex.
Complex 1 was prepared in good yield by a similar manner
to that described for the analogous Pt-Ln species (Ln=La,
Nd,Eu; Scheme 1).[24] The convenient one-pot synthesis of 1
demonstrates the high affinity of the soft PtII and hard GdIII
cations for the soft and hard Lewis bases (S and N/O,
respectively) that are present in the functionalized DTPA
ligand.The purple Pt-Gd complex has excellent solubility and
stability in aqueous solution,and no evidence was found for
the loss of PtII or GdIII ions from 1,even after 24 h of standing
in a buffered pH 7.4 solution at room temperature.
Preliminary DNA thermal denaturation (DNA melting)
experiments involving calf-thymus DNAwere performed on 1
at pH 7.4 (Supporting Information,Figure S1).There exists a
significant difference in the melting temperatures between
the free- and drug-treated DNA samples (DTm=4.5\20.5 8C),and the DNA-binding propensity of the complex follows that
seen for the related Pt-Nd species[24] and other dinuclear
{PtII(terpy)} species.[

英语翻译Herein,we present a new Pt-Gd complex that caneffectively target the nuclei of tumor cells by means of afunctionalized dtpa ligand linked to two {PtII(terpy)} (terpy=2,2’:6’,2’’-terpyridine) units that have the capacity to bindDNA
这里我们介绍一种新的Pt－Gd络合物,它可以用一种官能化的DTPA配体有效地瞄准肿瘤细胞的核,此配体连结到两个有能力以嵌插方式结合DNA｛PtII(terpy)｝(terpy=2,2:6’,2”-三联吡啶)的单元上[22-24].根据以前对类似的Pt－Ln络合物（Ln＝La、Nd、Eu）的研究（这些络合物是设计用来起识别DNA的发光探测剂作用的）[24],我们推论,有关的Pt－Gd种类1将有能力向这一重要的生物分子提供Gd.在本文中,我们报道了用Pt络合物将Gd提供到肿瘤细胞核的第一个毫不含糊的例子.
络合物1用一种与类似的Pt－Ln种类（Ln＝La、Nd、Eu；方案1）所描述的相似的方式,以良好的产率制备[24].1的方便的一锅法合成证明了软的PtII和硬的GdIII阳离子对于存在于官能化的DTPS配体中软的和硬的Lewis碱（分别为S和N/O）的高的亲和力.紫色的Pt－Gd络合物在含水溶液中具有优异的可溶性,而且没有发现PtII或GdIII离子从1中损失的证据,即使停放在室温下缓冲的pH7.4溶液中24h也是如此.
对1在pH7.4下进行了初步的、涉及小牛胸腺DNA的DNA热变性作用（DNA熔融）实验（支持信息,图S1）.无药物和有药物处理的DNA样本之间在熔融温度上存在明显的差别（ΔTm=4.5±0.5℃）,而络合物的DNA结合倾向遵循有关的Pt－Nd种类[24]和其他双核的｛PtII(terpy)｝种类[25-27]所看到的情况.

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我们提出一种可以有效地定位于肿瘤细胞核内的新型铂-钆复合物。这是借助于与两个PtII-terpy单元（terpy为2,2',6',2''-三联吡啶）相连的dtpa配体达成的，该配体可以以嵌入式（intercalative）与DNA结合[22-24]。基于先前有关类似的Pt-Ln复合物（Ln为La、Nd或Eu）的工作——此复合物是被设计来作为DNA的发光探针的[24]——我们有理由认为相关的Pt-Ga种类1号复合物可能会具有将钆呈递于重要生物分子中的能力。在本研究中，我们报告了证明钆通过铂复合物呈递于肿瘤细胞核的第一个清晰例证。
1号复合物合成方式类似于此前描述的同类Pt-Ln类种类复合物 (Ln=La,Nd,Eu; Scheme 1)[24]，产率较高。其传统单罐式合成证明，较强的三价钆离子和较弱的二价铂离子对功能化DTPA配体中存在的强弱路易斯碱（分别为N/O和S）有相当高的亲和力。此种紫色的铂-钆复合物有优秀的水溶性，在水溶液中稳定，即使在室温下于pH7.4的缓冲溶液中保留24h，也未发现二价铂离子或三价钆离子流失。
在pH7.4条件下用小牛胸腺DNA进行了关于1号复合物作用的初步DNA热失活（DNA熔解）实验（补充信息，图S1）。自由DNA样品与药物处理的DNA样品的熔解之间，存在显著差异（DTm=4.5+-0.5度）。此复合物的DNA结合特性类似于此前在相关的Pt-Nd种类[24]和其它双核[PtII(terpy)]中所见到的情况

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在此，我们提出一个新的铂钆复杂目标的手段，可以有效地DTPA的一个功能化的肿瘤细胞的细胞核配体与两个（PtII（terpy））（terpy = 2,2'：6'，2'' -三联吡啶）单位，有能力的插入方式与DNA结合在一个。探针进行DNA荧光[22-24]根据以前的工作相类似铂配合物的淋巴结（78 =镧，钕，铕），其中担任设计承认，[24]我们的理由是，有关铂钆物种1将有能力提供这项重要的生物大分子钆。在这项工作中，我们提供的报告首次明确钆例子，一个肿瘤细胞细胞核由铂复杂。复杂1产量良好编写由一个类似的方式是拉描述了类似的铂LN的物种（78 =，钕，铕，计划1）。[24]便捷的一锅合成1显示了S和高亲和力的软PtII和（硬GdIII阳离子的软，硬刘易斯基地ñ /输出，分别）是目前在官能DTPA的配体。紫色的铂钆复合具有优良的溶解度和溶液稳定性在水溶液中，没有发现证据，一从损失PtII或GdIII离子，即使在24热Ĥ初步站在一个缓冲溶液在pH 7.4室温。脱氧核糖核酸变性（DNA的熔点）的实验涉及小牛胸腺DNAwere 1上执行，在pH 7.4（支持信息，图中一）。温度之间存在着显着性差异熔化的自由和药物治疗的DNA样本（数字地面模型= 4.5 0.5 8C条），以及倾向的复杂的DNA结合如下物种见到有关铂钕[24]其他双核（PtII（terpy））品种。[

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