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首页> 外文期刊>Drug discovery today >Calmangafodipir [Ca4Mn(DPDP)(5)], mangafodipir (MnDPDP) and MnPLED with special reference to their SOD mimetic and therapeutic properties
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Calmangafodipir [Ca4Mn(DPDP)(5)], mangafodipir (MnDPDP) and MnPLED with special reference to their SOD mimetic and therapeutic properties

机译：Calmangafodipir [Ca4Mn（DPDP）（5）]，mangafodipir（MnDPDP）和MnPLED特别要考虑它们的SOD模拟和治疗特性

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摘要

Reactive oxygen species (ROS) and reactive nitrogen species (RNS) participate in pathological tissue damage. Mitochondrial manganese superoxide dismutase (MnSOD) normally keeps ROS and RNS in check. During development of mangafodipir (MnDPDP) as a magnetic resonance imaging (MRI) contrast agent, it was discovered that MnDPDP and its metabolite manganese pyridoxyl ethyldiamine (MnPLED) possessed SOD mimetic activity. MnDPDP has been tested as a chemotherapy adjunct in cancer patients and as an adjunct to percutaneous coronary intervention in patients with myocardial infarctions, with promising results. Whereas Mill contrast depends on release of Mn2+, the SOD mimetic activity depends on Mn2+ that remains bound to DPDP or PLED. Calmangafodipir [Ca4Mn(DPDP)(5)] is stabilized with respect to Mn2+ and has superior therapeutic activity. Ca4Mn(DPDP)(5) is presently being explored as a chemotherapy adjunct in a clinical multicenter Phase II study in patients with metastatic colorectal cancer.
机译：活性氧（ROS）和活性氮（RNS）参与病理组织损伤。线粒体锰超氧化物歧化酶（MnSOD）通常可以控制ROS和RNS。在将锰福地吡（MnDPDP）用作磁共振成像（MRI）造影剂的过程中，发现MnDPDP及其代谢产物锰吡啶氧基乙二胺锰（MnPLED）具有SOD模拟活性。 MnDPDP已作为癌症患者的化疗辅助剂和心肌梗死患者的经皮冠状动脉介入治疗的辅助剂进行了测试，并获得了可喜的结果。密尔对比度取决于Mn2 +的释放，而SOD模拟活性取决于仍与DPDP或PLED结合的Mn2 +。 Calmangafodipir [Ca4Mn（DPDP）（5）]对Mn2 +具有稳定作用，并具有出色的治疗活性。 Ca4Mn（DPDP）（5）目前正在临床多中心II期临床研究中作为转移性结直肠癌患者的化疗辅助药物进行研究。

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