英语翻译Herein,we present a new Pt-Gd complex that caneffectivel

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.[

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.