Laboratorio de Virología, Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, Piso 4, 1428 Buenos Aires, Argentina.
Antiviral Res. 2010 Sep;87(3):329-37. doi: 10.1016/j.antiviral.2010.06.005. Epub 2010 Jun 25.
A selected group of aromatic disulfides, thiuram disulfides and thiosulfones, provided by the National Cancer Institute, were evaluated in vitro for their inhibitory activity against Junin virus (JUNV), the causative agent of Argentine hemorrhagic fever. The aromatic disulfides NSC4492 and NSC71033 and the thiuram disulfide NSC14560 were, respectively, the more potent virucidal and antiviral agents against JUNV, with inactivating concentration 50% (IC(50)) values of 0.2-0.5 microM for virucidal compounds and antiviral effective concentration 50% (EC(50)) of 8.5 microM for NSC14560. Both types of compounds exhibited inhibitory activity against three arenaviruses. Additionally, a comparable efficacy in the antiviral action of NSC14560 was observed in monkey, hamster or human cells with selectivity indices in the range 55.9-85.7. Time of addition experiments showed that the main antiviral activity of NSC14560 was situated before 5h of infection, but a significant inhibition was still observed when the compound was added up 9h p.i. This compound did not induce a refractory state to infection by cell pretreatment. Nor did it prevent viral entry, but the cytoplasmic and membrane expression of the main viral proteins was inhibited. The possible involvement of the RING finger motif of arenavirus Z protein as target for the thiuram disulfide is discussed.
一组精选的芳香族二硫化物、秋兰姆二硫化物和硫代磺酸盐由美国国家癌症研究所提供,在体外对其抑制胡宁病毒(JUNV)的活性进行了评估,JUNV 是阿根廷出血热的病原体。芳香族二硫化物 NSC4492 和 NSC71033 以及秋兰姆二硫化物 NSC14560 分别是针对 JUNV 更强的病毒灭活和抗病毒剂,其对 JUNV 的半最大病毒灭活浓度(IC(50))值为 0.2-0.5μM,抗病毒有效浓度(EC(50))为 8.5μM。这两种化合物都对三种沙粒病毒表现出抑制活性。此外,在猴子、仓鼠或人细胞中,NSC14560 的抗病毒作用效果相当,其选择性指数在 55.9-85.7 之间。添加时间实验表明,NSC14560 的主要抗病毒活性位于感染后 5 小时之前,但当在感染后 9 小时添加时仍观察到显著的抑制作用。该化合物不会诱导细胞预处理使其对感染产生抗性,也不会阻止病毒进入,但抑制了主要病毒蛋白的细胞质和膜表达。讨论了沙粒病毒 Z 蛋白的 RING 指模作为秋兰姆二硫化物的靶标的可能性。