Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, Institute of Biomedicine of Seville (IBiS), University Hospital Virgen del Rocío/CSIC/University of Seville, 41013, Seville, Spain.
Department of Medicine, University of Seville, 41009, Seville, Spain.
Sci Rep. 2019 Jan 9;9(1):17. doi: 10.1038/s41598-018-37290-3.
The repositioning of drugs already approved by regulatory agencies for other indications is an emerging alternative for the development of new antimicrobial therapies. The repositioning process involves lower risks and costs than the de novo development of novel antimicrobial drugs. Currently, infections by adenovirus show a steady increment with a high clinical impact in immunosuppressed and immunocompetent patients. The lack of a safe and efficacious drug to treat these infections supports the search for new antiviral drugs. Here we evaluated the anti-adenovirus activity of niclosanide, oxyclozanide, and rafoxanide, three salicylanilide anthelmintic drugs. Also, we carried out the cytotoxicity evaluation and partial characterization of the mechanism of action of these drugs. The salicylanilide anthelmintic drugs showed significant anti-adenovirus activity at low micromolar concentrations with little cytotoxicity. Moreover, our mechanistic assays suggest differences in the way the drugs exert anti-adenovirus activity. Niclosamide and rafoxanide target transport of the HAdV particle from the endosome to the nuclear envelope, whilst oxyclozanide specifically targets adenovirus immediately early gene E1A transcription. Data suggests that the studied salicylanilide anthelmintic drugs could be suitable for further clinical evaluation for the development of new antiviral drugs to treat infections by adenovirus in immunosuppressed patients and in immunocompetent individuals with community-acquired pneumonia.
重新定位已获监管机构批准用于其他适应症的药物是开发新抗菌疗法的一种新兴替代方法。重新定位过程的风险和成本低于新型抗菌药物的从头开发。目前,腺病毒感染在免疫抑制和免疫功能正常的患者中呈稳步增长趋势,具有很高的临床影响。缺乏安全有效的药物来治疗这些感染,这支持了寻找新的抗病毒药物的研究。在这里,我们评估了尼氯柳胺、奥昔氯柳胺和三氯苯达唑这三种水杨酰苯胺类驱虫药对腺病毒的抗活性。此外,我们还进行了这些药物的细胞毒性评估和作用机制的部分特征分析。水杨酰苯胺类驱虫药在低微摩尔浓度下表现出显著的抗腺病毒活性,同时细胞毒性很小。此外,我们的机制研究表明,这些药物发挥抗腺病毒活性的方式存在差异。尼氯柳胺和三氯苯达唑靶向 HAdV 颗粒从内体到核膜的转运,而奥昔氯柳胺则特异性靶向腺病毒早期基因 E1A 转录。数据表明,研究中的水杨酰苯胺类驱虫药可能适合进一步的临床评估,以开发新的抗病毒药物,用于治疗免疫抑制患者的腺病毒感染以及免疫功能正常的社区获得性肺炎患者。