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一种水溶性金(III)卟啉的合成及其抗癌活性

Synthesis and anti-cancer activities of a water soluble gold(III) porphyrin.

作者信息

Lammer Aaron D, Cook Melissa E, Sessler Jonathan L

机构信息

Department of Chemistry, The University of Texas at Austin, 105 E. 24th Street-A5300, Austin, TX 78712-1224, USA.

出版信息

J Porphyr Phthalocyanines. 2015 Jan;19(1-03):398-403. doi: 10.1142/S1088424615500236.

Abstract

Gold(III) compounds continue to be explored for their potential utility as anticancer agents. A recognized limitation is the reactivity of gold(III), which is typically reduced to the more labile gold(I) state under physiological conditions. The use of porphyrins can overcome this problem. However, to date the stabilization provided by the use a strongly chelating porphyrin is offset by the poor solubility of the resulting complex in aqueous media. In this work, we describe the synthesis and anti-cancer activity of a gold(III)porphyrin complex with relatively good aqueous solubility. As judged from standard antiproliferation assays, this complex displays an IC of 9 μM for the A2780 human ovarian cancer cell line. This is a higher level of potency than displayed by two related control systems.

摘要

金(III)化合物因其作为抗癌剂的潜在效用而持续受到探索。一个公认的限制是金(III)的反应活性,在生理条件下它通常会还原为更不稳定的金(I)状态。卟啉的使用可以克服这个问题。然而,迄今为止,使用强螯合卟啉所提供的稳定性被所得配合物在水性介质中的低溶解度所抵消。在这项工作中,我们描述了一种具有相对良好水溶性的金(III)卟啉配合物的合成及其抗癌活性。根据标准的抗增殖测定判断,该配合物对A2780人卵巢癌细胞系的半数抑制浓度为9 μM。这一效力水平高于两个相关对照体系所显示的水平。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/039e/4407279/fe16395e0269/nihms680261f1.jpg

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