State Key Laboratory of Synthetic Chemistry, Institute of Molecular Functional Materials, Chemical Biology Centre and Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong, China.
Chem Soc Rev. 2015 Dec 21;44(24):8786-801. doi: 10.1039/c5cs00132c. Epub 2015 Apr 14.
Gold complexes have recently gained increasing attention in the design of new metal-based anticancer therapeutics. Gold(III) complexes are generally reactive/unstable under physiological conditions via intracellular redox reactions, and the intracellular Au(III) to Au(I) reduction reaction has recently been "traced" by the introduction of appropriate fluorescent ligands. Similar to most Au(I) complexes, Au(III) complexes can inhibit the activities of thiol-containing enzymes, including thioredoxin reductase, via ligand exchange reactions to form Au-S(Se) bonds. Nonetheless, there are examples of physiologically stable Au(III) and Au(I) complexes, such as [Au(TPP)]Cl (H2TPP = 5,10,15,20-tetraphenylporphyrin) and [Au(dppe)2]Cl (dppe = 1,2-bis(diphenylphosphanyl)ethane), which are known to display highly potent in vitro and in vivo anticancer activities. In this review, we summarize our current understanding of anticancer gold complexes, including their mechanisms of action and the approaches adopted to improve their anticancer efficiency. Some recent examples of gold anticancer chemotherapeutics are highlighted.
金配合物在新型金属基抗癌治疗药物的设计中最近受到了越来越多的关注。金(III)配合物在生理条件下通常通过细胞内氧化还原反应表现出反应性/不稳定性，并且最近通过引入适当的荧光配体“追踪”了细胞内的 Au(III)到 Au(I)还原反应。与大多数 Au(I)配合物类似，金(III)配合物可以通过配体交换反应抑制含巯基酶的活性，包括硫氧还蛋白还原酶，从而形成 Au-S(Se)键。尽管如此，也有一些生理稳定的 Au(III)和 Au(I)配合物的例子，例如 [Au(TPP)]Cl（H2TPP = 5,10,15,20-四苯基卟啉）和 [Au(dppe)2]Cl（dppe = 1,2-双（二苯基膦基）乙烷），已知它们具有很强的体外和体内抗癌活性。在这篇综述中，我们总结了我们对抗癌金配合物的理解，包括它们的作用机制和提高抗癌效率的方法。强调了一些最近的金抗癌化疗药物的例子。
