Umemura Masanari, Kim Jeong-Hwan, Aoyama Haruki, Hoshino Yujiro, Fukumura Hidenobu, Nakakaji Rina, Sato Itaru, Ohtake Makoto, Akimoto Taisuke, Narikawa Masatoshi, Tanaka Ryo, Fujita Takayuki, Yokoyama Utako, Taguri Masataka, Okumura Satoshi, Sato Motohiko, Eguchi Haruki, Ishikawa Yoshihiro
Cardiovascular Research Institute, Yokohama City University, Graduate School of Medicine, 3-9 Fukuura, Kanazawa-ku, Yokohama 236-0004, Japan.
Department of Environment and Natural Sciences, Graduate School of Environment and Information Sciences, Yokohama National University, 79-7, Tokiwada, Hodogaya, Yokohama 240-8501, Japan.
J Pharmacol Sci. 2017 Aug;134(4):203-210. doi: 10.1016/j.jphs.2017.07.002. Epub 2017 Jul 25.
Iron-salen, i.e., μ-oxo-N,N'-bis(salicylidene)ethylenediamine iron (Fe(Salen)) was a recently identified as a new anti-cancer compound with intrinsic magnetic properties. Chelation therapy has been widely used in management of metallic poisoning, because an administration of agents that bind metals can prevent potential lethal effects of particular metal. In this study, we confirmed the therapeutic effect of deferoxamine mesylate (DFO) chelation against Fe(Salen) as part of the chelator antidote efficacy. DFO administration resulted in reduced cytotoxicity and ROS generation by Fe(Salen) in cancer cells. DFO (25 mg/kg) reduced the onset of Fe(Salen) (25 mg/kg)-induced acute liver and renal dysfunction. DFO (300 mg/kg) improves survival rate after systematic injection of a fatal dose of Fe(Salen) (200 mg/kg) in mice. DFO enables the use of higher Fe(Salen) doses to treat progressive states of cancer, and it also appears to decrease the acute side effects of Fe(Salen). This makes DFO a potential antidote candidate for Fe(Salen)-based cancer treatments, and this novel strategy could be widely used in minimally-invasive clinical settings.
铁-萨伦,即μ-氧代-N,N'-双(水杨醛)乙二胺铁(Fe(Salen)),最近被鉴定为一种具有内在磁性的新型抗癌化合物。螯合疗法已广泛应用于金属中毒的治疗,因为给予能结合金属的药物可以预防特定金属的潜在致命影响。在本研究中,我们证实了去铁胺甲磺酸盐(DFO)螯合对Fe(Salen)的治疗效果,作为螯合剂解毒剂疗效的一部分。给予DFO可降低癌细胞中Fe(Salen)诱导的细胞毒性和活性氧生成。DFO(25mg/kg)减轻了Fe(Salen)(25mg/kg)诱导的急性肝肾功能障碍的发生。DFO(300mg/kg)提高了在小鼠中系统性注射致死剂量的Fe(Salen)(200mg/kg)后的存活率。DFO能够使用更高剂量的Fe(Salen)来治疗进展期癌症,并且它似乎还能降低Fe(Salen)的急性副作用。这使得DFO成为基于Fe(Salen)的癌症治疗的潜在解毒剂候选物,并且这种新策略可广泛应用于微创临床环境。