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抗癌之路铺满了黄金吗？具有多种迷人生物学特性的金属卡宾配合物。

Is the Way to Fight Cancer Paved with Gold? Metal-Based Carbene Complexes with Multiple and Fascinating Biological Features.

作者信息

Iacopetta Domenico, Rosano Camillo, Sirignano Marco, Mariconda Annaluisa, Ceramella Jessica, Ponassi Marco, Saturnino Carmela, Sinicropi Maria Stefania, Longo Pasquale

机构信息

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, Italy.

Biopolymers and Proteomics IRCCS, Ospedale Policlinico San Martino-IST, Largo R. Benzi 10, 16132 Genova, Italy.

出版信息

Pharmaceuticals (Basel). 2020 May 11;13(5):91. doi: 10.3390/ph13050091.

DOI:10.3390/ph13050091
PMID:32403274
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7281280/
Abstract

Herein, we report the synthesis and the multiple anti-tumor properties of new gold and silver carbene complexes. The chemical modifications, grounded on our previous studies, led us to identify a good lead complex, gold-based, whose biological features are very exciting and promising in the anti-cancer research and could be further developed. Indeed, the bis-[4,5-dichloro-(-methyl-'(2-hydroxy-2-phenyl)ethyl-imidazole-2-ylidene)gold(I)][dichloro-gold] () complex possesses the ability to interfere with at least three important and different intracellular targets, namely the human topoisomerases I and II and tubulin, which are able to modulate metabolic processes not directly correlated each other. We proved that the modifications of the ligands structure in , with respect to another already published complex, i.e., bis-[4,5-dichloro-(-methyl-'(cyclopentane-2ol)-imidazole-2-ylidine)gold(I)][dichloro-gold] (), produce a different behavior toward tubulin-polymerization process, since a tubulin-polymerization inhibitor and a stabilizer, with the final same result of hampering the tumor growth. Taken together, our outcomes designate as a promising compound for the development of multi-targeted anti-cancer therapies.

摘要

在此，我们报告新型金和银卡宾配合物的合成及其多种抗肿瘤特性。基于我们之前的研究进行的化学修饰，使我们确定了一种良好的先导配合物，即基于金的配合物，其生物学特性在抗癌研究中非常令人兴奋且前景广阔，有望进一步开发。实际上，双-[4,5-二氯-(-甲基-'(2-羟基-2-苯基)乙基-咪唑-2-亚基)金(I)]二氯金配合物具有干扰至少三个重要且不同的细胞内靶点的能力，即人类拓扑异构酶I和II以及微管蛋白，它们能够调节彼此不直接相关的代谢过程。我们证明，与另一种已发表的配合物，即双-[4,5-二氯-(-甲基-'(环戊烷-2-醇)-咪唑-2-亚基)金(I)]二氯金相比，中配体结构的修饰对微管蛋白聚合过程产生了不同的影响，因为是微管蛋白聚合抑制剂，是稳定剂，最终都产生了阻碍肿瘤生长的相同结果。综上所述，我们的研究结果表明是开发多靶点抗癌疗法的一种有前景的化合物。

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