Institute for Specific Prophylaxis and Tropical Medicine Center for Pathophysiology, Infectiology, and Immunology, Medical University of Vienna, Kinderspitalgasse 15, A-1090 Vienna, Austria.
Institute for Specific Prophylaxis and Tropical Medicine Center for Pathophysiology, Infectiology, and Immunology, Medical University of Vienna, Kinderspitalgasse 15, A-1090 Vienna, Austria.
Int J Parasitol Drugs Drug Resist. 2021 Aug;16:38-44. doi: 10.1016/j.ijpddr.2021.04.004. Epub 2021 Apr 30.
Trichomonads are an order of parasitic protists which infect a wide range of hosts. The human parasite Trichomonas vaginalis and the bovine parasite Tritrichomonas foetus which also infects cats and swine are of considerable medical and veterinary importance, respectively. Since trichomonads are microaerophiles/anaerobes they are susceptible to 5-nitroimidazoles such as metronidazole. 5-nitroimidazoles are exclusively toxic to microaerophilic/anaerobic organisms because reduction, i.e. activation, of the drug can only occur in a highly reductive environment. 5-nitroimidazoles have remained a reliable treatment option throughout the last decades but drug resistance can be a problem. Clinical resistance to 5-nitroimidazoles has been studied in more detail in T. vaginalis and has been ascribed to defective oxygen scavenging mechanisms which lead to higher intracellular oxygen concentrations and, consequently, to less drug being reduced. Two enzymes, flavin reductase (FR) and NADH oxidase have been suggested to be the major oxygen scavenging enzymes in T. vaginalis. The loss, or at least an impairment of FR which reduces oxygen to hydrogen peroxide, has been proposed as the central mechanism that enables the emergence of 5-nitroimidazole resistance. In this study we explored if T. foetus also encodes a homolog of FR and if it is, likewise, involved in resistance. T. foetus was indeed found to express a FR but it was only weakly active as compared to the T. vaginalis homolog. Further, activity of FR in T. foetus was unchanged in metronidazole-resistant cell lines, ruling out that it has a role in metronidazole resistance. Finally, we measured oxygen scavenging rates in metronidazole-sensitive and -resistant cell lines and found that NADH oxidase and FR are not the major oxygen scavenging enzymes in trichomonads and that oxygen scavenging is possibly a consequence, rather than a cause of metronidazole resistance.
滴虫是一种寄生原生动物目,感染范围广泛的宿主。人类寄生虫阴道毛滴虫和牛寄生虫胎儿滴虫也感染猫和猪,分别具有相当大的医学和兽医重要性。由于滴虫是微需氧/厌氧菌,它们易受 5-硝基咪唑类药物如甲硝唑的影响。5-硝基咪唑类药物仅对微需氧/厌氧菌有毒,因为药物的还原,即激活,只能在高度还原性环境中发生。5-硝基咪唑类药物在过去几十年中一直是可靠的治疗选择,但药物耐药性可能是一个问题。在阴道毛滴虫中更详细地研究了对 5-硝基咪唑类药物的临床耐药性,并归因于缺陷的氧清除机制,导致细胞内氧浓度更高,因此减少的药物更少。两种酶,黄素还原酶(FR)和 NADH 氧化酶被认为是阴道毛滴虫中主要的氧清除酶。FR 的丧失,或至少其功能受损,将氧还原为过氧化氢,被认为是导致 5-硝基咪唑类药物耐药性出现的核心机制。在这项研究中,我们探讨了胎儿滴虫是否也编码 FR 的同源物,如果是,它是否同样参与耐药性。事实上,发现胎儿滴虫表达 FR,但与阴道毛滴虫同源物相比,其活性较弱。此外,在甲硝唑耐药细胞系中,FR 的活性在甲硝唑耐药细胞系中没有改变,排除了它在甲硝唑耐药性中的作用。最后,我们测量了甲硝唑敏感和耐药细胞系中的氧清除率,发现 NADH 氧化酶和 FR 不是滴虫中的主要氧清除酶,氧清除可能是甲硝唑耐药性的结果,而不是原因。