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首页> 外文期刊>Parasitology >Anti-Trichomonas vaginalis activity of 1,10-phenanthroline-5,6-dione-based metallodrugs and synergistic effect with metronidazole
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Anti-Trichomonas vaginalis activity of 1,10-phenanthroline-5,6-dione-based metallodrugs and synergistic effect with metronidazole

机译：抗滴毛瘤阴道活性1,10菲咯啉-5,6-二酮的金属解压和与甲硝唑的协同作用

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摘要

Trichomonas vaginalis is responsible for the most common non-viral, sexually transmitted infection, human trichomoniasis, and is associated with an increased susceptibility to HIV. An escalation in resistance (2.5–10%) to the clinical drug, metronidazole (MTZ), has been detected and this compound also has adverse side-effects. Therefore, new treatment options are urgently required. Herein, we investigate the possible anti-T. vaginalis activity of 1,10-phenanthroline-5,6-dione (phendione) and its metal complexes, [Ag(phendione)2]ClO4 and [Cu(phendione)3](ClO4)2·4H2O. Minimum inhibitory concentration (MIC) against T. vaginalis ATCC 30236 and three fresh clinical isolates and mammalian cells were performed using serial dilution generating IC50 and CC50 values. Drugs combinations with MTZ were evaluated by chequerboard assay. A strong anti-T. vaginalis activity was found for all test compounds. IC50 values obtained for [Cu(phendione)3](ClO4)2·4H2O were similar or lower than those obtained for MTZ. In vitro assays with normal cells showed low cytotoxicity and [Cu(phendione)3](ClO4)2·4H2O presented a high selectivity index (SI) for fibroblasts (SI = 11.39) and erythrocytes (SI > 57.47). Chequerboard assay demonstrated that the combination of [Cu(phendione)3](ClO4)2·4H2O with MTZ leads to synergistic interaction, which suggests distinct mechanisms of action of the copper–phendione complex and avoiding the MTZ resistance pathways. Our results highlight the importance of phendione-based drugs as potential molecules of pharmaceutical interest.
机译：滴虫游戏阴道是最常见的非病毒，性传播感染，人毛癣病，并且与对艾滋病毒的易感性增加有关。已经检测到患有抗抵抗力（2.5-10％）的抵抗力（2.5-10％）甲硝唑（MTZ），并且该化合物也具有不良副作用。因此，迫切需要新的治疗选择。在此，我们研究了可能的抗T。阴道素活性为1,10-菲咯啉-5,6-二酮（Phendione）及其金属配合物，[Ag（Phendione）2] ClO4和[Cu（Phendione）3]（ClO 4）2·4H2O。使用串联稀释产生IC50和CC50值进行针对阴道抗阴炎ATCC 30236和三种新鲜临床分离株和哺乳动物细胞的最小抑制浓度（MIC）。用CHEQUERBERBORBORAL测定评估用MTZ的药物组合。强烈的反吨。对所有测试化合物发现了阴道活性。用于[Cu（Phendione）3]（CLO 4）2·4H2O的IC 50值相似或低于MTZ所获得的值。具有正常细胞的体外测定显示出低细胞毒性和[Cu（phendione）3]（CLO 4）2·4H2O给出了成纤维细胞（Si = 11.39）和红细胞（Si> 57.47）的高选择性指数（Si）。 Chequerboard测定证明[Cu（Phendione）3]（CLO 4）2·4H2O与MTZ的组合导致协同相互作用，这表明铜期综合体复合物和避免MTZ抗性途径的不同机制。我们的结果突出了Phendione的药物作为药物潜在分子的重要性。

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