US Army Medical Research Institute of Infectious Diseases, Fort Detrick, Frederick, Maryland, USA.
Antimicrob Agents Chemother. 2010 May;54(5):2152-9. doi: 10.1128/AAC.01315-09. Epub 2010 Mar 8.
There exists an urgent need to develop licensed drugs and vaccines for the treatment or prevention of filovirus infections. FGI-103 is a low-molecular-weight compound that was discovered through an in vitro screening assay utilizing a variant of Zaire ebolavirus (ZEBOV) that expresses green fluorescent protein. In vitro analyses demonstrated that FGI-103 also exhibits antiviral activity against wild-type ZEBOV and Sudan ebolavirus, as well as Marburgvirus (MARV) strains Ci67 and Ravn. In vivo administration of FGI-103 as a single intraperitoneal dose of 10 mg/kg delivered 24 h after infection is sufficient to completely protect mice against a lethal challenge with a mouse-adapted strain of either ZEBOV or MARV-Ravn. In a murine model of ZEBOV infection, delivery of FGI-103 reduces viremia and the viral burden in kidney, liver, and spleen tissues and is associated with subdued and delayed proinflammatory cytokine responses and tissue pathology. Taken together, these results identify a promising antiviral therapeutic candidate for the treatment of filovirus infections.
目前迫切需要开发用于治疗或预防丝状病毒感染的许可药物和疫苗。FGI-103 是一种低分子量化合物,是通过利用表达绿色荧光蛋白的扎伊尔埃博拉病毒(ZEBOV)变体进行体外筛选试验发现的。体外分析表明,FGI-103 还对野生型 ZEBOV 和苏丹埃博拉病毒以及马尔堡病毒(MARV)株 Ci67 和 Ravn 具有抗病毒活性。在感染后 24 小时内给予 FGI-103 单次腹腔内剂量 10mg/kg,足以完全保护小鼠免受经小鼠适应的 ZEBOV 或 MARV-Ravn 株的致死性挑战。在 ZEBOV 感染的小鼠模型中,FGI-103 的递送可降低病毒血症和肾脏、肝脏和脾脏组织中的病毒负担,并与减弱和延迟的促炎细胞因子反应和组织病理学相关。总之,这些结果确定了一种有前途的丝状病毒感染治疗药物候选物。