Novel Virostatic Agents against Bluetongue Virus

• DOI: 10.1371/journal.pone.0043341
• Publication Date: 2012-08-15T21:04:00Z
• Authors: Linlin Gu; Volodymyr Musiienko; Zhijun Bai; Aijian Qin; Stewart W. Schneller; Qianjun Li
• Keywords: Viral life cycle; EC50; Viral protein; IC50

Bluetongue virus (BTV), a member in the family Reoviridae, is re-emerging animal disease infecting cattle and sheep. With its recent outbreaks Europe, there pressing need for efficacious antivirals. We presented here identification characterization of novel virostatic molecule against BTV, an aminothiophenecarboxylic acid derivative named compound 003 (C003). The efficacy C003 could be improved via chemical modification, leading to de novo synthesized 052 (C052). 50% effective concentrations (EC50) C052 were determined at 1.76±0.73 µM 0.27±0.12 µM, respectively. cytotoxicity concentration (CC50) was over 100 CC50 82.69 µM. Accordingly, selective index (SI50) BTV 57 306, inhibitory effect C003/C052 on BTV-induced apoptosis also confirmed inhibition caspase-3/-7 activation post infection. inhibit induced CPE even when added as late 24 h.p.i., indicating that they might act stage viral life-cycle. reduce two-logs both progeny production number genomic RNA copies. Interestingly, host autophagy protein expression inhibited infection cells treated with C052, suggesting agents inhibiting activation. Although further investigations needed pin down exact mechanism C003/C052, our finding suggested these compounds potent lead potential action BTV.