Department of Molecular Microbiology and Immunology, Saint Louis University School of Medicine, 1100 S. Grand Blvd., St. Louis, Missouri, 63104, USA.
Antiviral Res. 2018 Aug;156:102-106. doi: 10.1016/j.antiviral.2018.06.010. Epub 2018 Jun 15.
Herpes simplex virus (HSV)-1 and HSV-2 cause painful blisters and shallow ulcers in exposed skin and mucosae during primary or recurrent infection. In addition, recurrent and potentially blinding HSV-1 infections of the eye afflict nearly half a million persons in the U.S. Current clinical therapies rely on nucleoside analog drugs such as acyclovir (ACV) or ganciclovir to ameliorate primary infections and reduce the frequency and duration of reactivations. However, these treatments do not fully suppress viral shedding and drug-resistant mutants develop in the eye and in vulnerable, immunosuppressed patients. Herpesvirus DNA replication requires several enzymes in the nucleotidyl transferase superfamily (NTS) that have recombinase and nuclease activities. We previously found that compounds which block NTS enzymes efficiently inhibit replication of HSV-1 and HSV-2 by up to 1 million-fold in Vero and human foreskin fibroblasts. Among the compounds with potent suppressive effects in culture is the anti-fungal drug ciclopirox. Here we report that topical application of ciclopirox olamine to the eyes of mice infected with HSV-1 reduced virus shed from the corneal epithelium compared with saline control, and reduced development of blepharitis to the level of mice treated with ACV. Results were dose-dependent. In addition, treatment with ciclopirox olamine significantly reduced acute and latent HSV-1 infection of the peripheral nervous system. These results support further development of ciclopirox olamine as a repurposed topical agent for HSV infections.
单纯疱疹病毒 (HSV)-1 和 HSV-2 在初次感染或复发感染时会导致暴露皮肤和黏膜出现疼痛性水疱和浅层溃疡。此外,美国近 50 万人患有反复发作且可能导致失明的 HSV-1 眼部感染。目前的临床治疗方法依赖于核苷类似物药物,如阿昔洛韦 (ACV) 或更昔洛韦,以改善初次感染并减少复发的频率和持续时间。然而,这些治疗方法并不能完全抑制病毒脱落,并且在眼部和易感染、免疫抑制的患者中会产生耐药突变体。疱疹病毒 DNA 复制需要核苷酸转移酶超家族 (NTS) 中的几种酶,这些酶具有重组酶和核酸酶活性。我们之前发现,阻断 NTS 酶的化合物可在 Vero 和人包皮成纤维细胞中使 HSV-1 和 HSV-2 的复制效率提高 100 万倍。在具有强效抑制作用的化合物中,有一种抗真菌药物环吡酮胺。在这里,我们报告将环吡酮胺局部应用于感染 HSV-1 的小鼠眼睛,与生理盐水对照组相比,可减少角膜上皮的病毒脱落,并使结膜炎的发展降低到用 ACV 治疗的小鼠的水平。结果呈剂量依赖性。此外,用环吡酮胺治疗可显著减少外周神经系统的急性和潜伏性 HSV-1 感染。这些结果支持进一步开发环吡酮胺作为一种用于治疗 HSV 感染的重新定位的局部药物。