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微调钌(II)芳基配合物的细胞毒性，以提高对乳腺癌的选择性。

Fine-tuning the cytotoxicity of ruthenium(II) arene compounds to enhance selectivity against breast cancers.

机构信息

LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, no 228, 4050-313 Porto, Portugal.

Institut des Sciences et Ingénierie Chimiques, École Polytechnique Fédérale de Lausanne (EPFL), 1015 Lausanne, Switzerland.

出版信息

Dalton Trans. 2023 Aug 22;52(33):11679-11690. doi: 10.1039/d3dt02037a.

DOI:10.1039/d3dt02037a
PMID:37552495
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10442743/
Abstract

Ruthenium-based complexes have been suggested as promising anticancer drugs exhibiting reduced general toxicity compared to platinum-based drugs. In particular, Ru(η-arene)(PTA)Cl (PTA = 1,3,5-triaza-7-phosphaadamantane), or RAPTA, complexes have demonstrated efficacy against breast cancer by suppressing metastasis, tumorigenicity, and inhibiting the replication of the human tumor suppressor gene BRCA1. However, RAPTA compounds have limited cytotoxicity, and therefore comparatively high doses are required. This study explores the activity of a series of RAPTA-like ruthenium(II) arene compounds against MCF-7 and MDA-MB-231 breast cancer cell lines and [Ru(η-toluene)(PPh)Cl] was identified as a promising candidate. Notably, [Ru(η-toluene)(PPh)Cl]Cl was found to be remarkably stable and highly cytotoxic, and selective to breast cancer cells. The minor groove of DNA was identified as a relevant target.

摘要

钌基配合物被认为是很有前途的抗癌药物，与铂类药物相比，其一般毒性较低。特别是 Ru(η-芳烃)(PTA)Cl（PTA=1,3,5-三氮杂-7-磷杂金刚烷）或 RAPTA 配合物通过抑制转移、肿瘤发生和抑制人肿瘤抑制基因 BRCA1 的复制，已被证明对乳腺癌有效。然而，RAPTA 化合物的细胞毒性有限，因此需要比较高的剂量。本研究探讨了一系列 RAPTA 类似的钌（II）芳基化合物对 MCF-7 和 MDA-MB-231 乳腺癌细胞系的活性，发现[Ru(η-甲苯)(PPh)Cl]是一种很有前途的候选药物。值得注意的是，[Ru(η-甲苯)(PPh)Cl]Cl 被发现非常稳定且具有高细胞毒性，对乳腺癌细胞具有选择性。DNA 的小沟被确定为一个相关的靶标。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/9c084674a2ce/d3dt02037a-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/8489133bcb03/d3dt02037a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/4e308a7522ca/d3dt02037a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/17e5d16655a5/d3dt02037a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/e91dbbe61fc2/d3dt02037a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/a4d7bec3ce07/d3dt02037a-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/9c084674a2ce/d3dt02037a-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/8489133bcb03/d3dt02037a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/4e308a7522ca/d3dt02037a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/17e5d16655a5/d3dt02037a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/e91dbbe61fc2/d3dt02037a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/a4d7bec3ce07/d3dt02037a-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1190/10442743/9c084674a2ce/d3dt02037a-f6.jpg

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