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Resorufin Enters the Photodynamic Therapy Arena: A Monoamine Oxidase Activatable Agent for Selective Cytotoxicity
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-11-23 , DOI: 10.1021/acsmedchemlett.0c00484 Toghrul Almammadov 1 , Gizem Atakan 2 , Ozen Leylek 3 , Gulnihal Ozcan 4 , Gorkem Gunbas 2 , Safacan Kolemen 1, 5, 6, 7
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-11-23 , DOI: 10.1021/acsmedchemlett.0c00484 Toghrul Almammadov 1 , Gizem Atakan 2 , Ozen Leylek 3 , Gulnihal Ozcan 4 , Gorkem Gunbas 2 , Safacan Kolemen 1, 5, 6, 7
Affiliation
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A red-absorbing, water-soluble, and iodinated resorufin derivative (R1) that can be selectively activated with a monoamine oxidase (MAO) enzyme was synthesized, and its potential as a photodynamic therapy (PDT) agent was evaluated. R1 showed high 1O2 generation yields in aqueous solutions upon addition of MAO isoforms, and it was further tested in cell culture studies. R1 induced photocytotoxicity after being triggered by endogenous MAO enzyme in cancer cells with a much higher efficiency in SH-SY5Y neuroblastoma cells with high MAO-A expression. Additionally, R1 displayed differential cytotoxicity between cancer and normal cells, without any considerable dark toxicity. To the best of our knowledge, R1 marks the first example of a resorufin-based photosensitizer (PS) as well as the first anticancer drug that is activated by a MAO enzyme. Remarkably, the target PDT agent was obtained only in three steps as a result of versatile resorufin chemistry.
中文翻译：
Resorufin 进入光动力治疗领域：一种用于选择性细胞毒性的单胺氧化酶激活剂
合成了一种可被单胺氧化酶 (MAO) 酶选择性激活的吸收红色、水溶性和碘化试卤灵衍生物 ( R1 )，并评估了其作为光动力疗法 (PDT) 药剂的潜力。R1在添加 MAO 同种型后在水溶液中显示出高1 O 2生成率，并在细胞培养研究中进行了进一步测试。R1在癌细胞中被内源性 MAO 酶触发后诱导光细胞毒性，在具有高 MAO-A 表达的 SH-SY5Y 神经母细胞瘤细胞中具有更高的效率。此外，R1在癌细胞和正常细胞之间显示出不同的细胞毒性，没有任何显着的暗毒性。据我们所知，R1标志着基于试卤灵的光敏剂 (PS) 的第一个例子，以及第一个被 MAO 酶激活的抗癌药物。值得注意的是，由于多功能试卤灵化学，目标 PDT 试剂仅通过三个步骤获得。
更新日期：2020-12-10
中文翻译：
Resorufin 进入光动力治疗领域：一种用于选择性细胞毒性的单胺氧化酶激活剂
合成了一种可被单胺氧化酶 (MAO) 酶选择性激活的吸收红色、水溶性和碘化试卤灵衍生物 ( R1 )，并评估了其作为光动力疗法 (PDT) 药剂的潜力。R1在添加 MAO 同种型后在水溶液中显示出高1 O 2生成率，并在细胞培养研究中进行了进一步测试。R1在癌细胞中被内源性 MAO 酶触发后诱导光细胞毒性，在具有高 MAO-A 表达的 SH-SY5Y 神经母细胞瘤细胞中具有更高的效率。此外，R1在癌细胞和正常细胞之间显示出不同的细胞毒性，没有任何显着的暗毒性。据我们所知，R1标志着基于试卤灵的光敏剂 (PS) 的第一个例子，以及第一个被 MAO 酶激活的抗癌药物。值得注意的是，由于多功能试卤灵化学，目标 PDT 试剂仅通过三个步骤获得。
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