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体内低毒性但体外高活性的抗癌有机铑和铱配合物：DNA 损伤、活性氧形成和溶血活性。

Anticancer organorhodium and -iridium complexes with low toxicity in vivo but high potency in vitro: DNA damage, reactive oxygen species formation, and haemolytic activity.

机构信息

School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.

Auckland Cancer Society Research Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.

出版信息

Chem Commun (Camb). 2019 Oct 3;55(80):12016-12019. doi: 10.1039/c9cc03822a.

DOI:10.1039/c9cc03822a
PMID:31498360
Abstract

Redox-modulating anticancer drugs allow the exploitation of altered redox biology observed in many cancer cells. We discovered dinuclear RhIII(Cp*) and IrIII(Cp*) complexes that have in vitro anticancer activity superior to cisplatin and the investigational drug IT-139, while being less toxic in haemolysis and in vivo zebrafish models. The mode of action appears to be related to DNA damage and ROS-mediated stress pathways.

摘要

氧化还原调节抗癌药物允许利用许多癌细胞中观察到的改变的氧化还原生物学。我们发现了双核 RhIII(Cp*)和 IrIII(Cp*)配合物，它们具有比顺铂和研究药物 IT-139更好的体外抗癌活性，而在溶血和体内斑马鱼模型中毒性较低。作用模式似乎与 DNA 损伤和 ROS 介导的应激途径有关。

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