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首页> 外文期刊>Chemistry: A European journal >Photoinduced Reduction of Pt~(IV) within an Anti-Proliferative Pt~(IV)- Texaphyrin Conjugate
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Photoinduced Reduction of Pt~(IV) within an Anti-Proliferative Pt~(IV)- Texaphyrin Conjugate

机译：抗增殖的Pt〜（IV）-得沙弗林缀合物内Pt〜（IV）的光诱导还原

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摘要

In an effort to increase the stability and control the platinum reactivity of platinum-texaphyrin conjugates, two Pt~(IV) conjugates were designed, synthesized, and studied for their ability to form DNA adducts. They were also tested for their anti-proliferative effects using wild-type and platinum-resistant human ovarian cancer cell lines (A2780 and 2780CP, respectively). In comparison to an analogous firstgeneration Pt~(II) chimera, one of the new conjugates provided increased stability in aqueous environments. Using a combination of ~1H NMR spectroscopy and FAAS (flameless atomicabsorption spectrometry), it was found that the Pt~(IV) center within this conjugate undergoes photoinduced reduction to Pt~(II) upon exposure to glass-filtered daylight, resulting in an entity that binds DNA in a controlled manner. Under conditions in which the Pt~(IV) complex is reduced to the corresponding Pt~(II) species, these new conjugates demonstrated potent anti-proliferative activity in both test ovarian cancer cell lines.
机译：为了提高稳定性并控制铂-邻菲菊酯缀合物的铂反应性，设计，合成并研究了两种Pt〜（IV）缀合物形成DNA加合物的能力。还使用野生型和抗铂类人卵巢癌细胞系（分别为A2780和2780CP）测试了它们的抗增殖作用。与类似的第一代Pt〜（II）嵌合体相比，一种新的结合物在水性环境中具有更高的稳定性。使用〜1H NMR光谱和FAAS（无焰原子吸收光谱法）的组合，发现该共轭物中的Pt〜（IV）中心在暴露于玻璃滤光的日光下会发生光诱导还原为Pt〜（II），从而导致以受控方式结合DNA的实体。在其中Pt〜（IV）络合物还原为相应的Pt〜（II）物种的条件下，这些新的结合物在两种测试卵巢癌细胞系中均显示出强大的抗增殖活性。

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