Histidine-rich Modification of a Scorpion-derived Peptide Improves Bioavailability and Inhibitory Activity against HSV-1

Zeng, Zhengyang; Zhang, Runhong; Hong, Wei; Cheng, Yuting; Wang, Huijuan; Lang, Yange; Ji, Zhenglin; Wu, Yingliang; Li, Wenxin; Xie, Youli; Cao, Zhijian

To assess whether Eval418 is suitable for further development as a candidate anti-HSV-1 agent, its cytotoxicity to Vero cells was determined by MTT assay (Figure 3a ). Vero cells were treated by Eval418 at a series of concentrations ranging from 0 to 200 μg/mL. After incubation for 48 h, the 50% cytotoxicity concentration (CC50) of Eval418 to Vero cells was 68.50 μg/mL. After treatment with Eval418 at 10 μg/mL, the cell viability of the peptide-treated Vero cells was greater than 95%. Hemolysis assay showed that the cell viability of erythrocytes was also more than 95% at concentrations of Eval418 of 10 μg/mL or less (Figure 3b ). These data indicated that 10 μg/mL or less, Eval418 was minimally cytotoxic to Vero cells and suitable for further anti-HSV-1 experiments. The hemolytic activity of Eval418 was evaluated in human erythrocytes by hemolytic assay. The concentrations also ranged from 0 to 200 μg/mL. The hemolysis rate of human erythrocytes was less than 50% when the concentration of Eval418 was as high as 200 μg/mL.