MOE Joint International Research Laboratory of Animal Health and Food Safety, College of veterinary medicine, Nanjing Agricultural University, Jiangsu, PR China.
College of veterinary medicine, Gansu Agricultural University, Gansu, PR China.
PLoS One. 2019 Apr 11;14(4):e0215227. doi: 10.1371/journal.pone.0215227. eCollection 2019.
Surfactin has antiviral activity against various enveloped viruses by inhibiting viral membrane fusion. However, the potential utility of surfactin as an antiviral drug is limited by its cytotoxicity. In this study, 10 surfactin analogues were obtained by chemical synthesis and evaluated to determine their anti-PEDV activities, hemolytic activities, and critical micelle concentrations. The main goal of our study was to develop a safer drug; a surfactin analogue with high anti-PEDV activity and low hemolytic activity. Compared with surfactin, one of the analogues we developed, SLP5, has lower hemolytic activity, with the same antiviral activity. The selectivity index of SLP5 is 52, while the SI for surfactin is 4, in other words, the safe and effective concentration range of SLP5 is 12 times greater than that of surfactin. Like surfactin, SLP5 has a direct antiviral effect on PEDV. Structurally, SLP5 is a linear lipopeptide with three carboxyl groups. Surfactin derivatives similar to SLP5 could be obtained by lactone bond hydrolyzation of surfactin, as well as total synthesis.
表面活性剂通过抑制病毒膜融合具有针对各种包膜病毒的抗病毒活性。然而，表面活性剂作为抗病毒药物的潜在用途受到其细胞毒性的限制。在这项研究中，通过化学合成获得了 10 种表面活性剂类似物，并对其抗 PEDV 活性、溶血活性和临界胶束浓度进行了评估。我们研究的主要目的是开发一种更安全的药物；一种具有高抗 PEDV 活性和低溶血活性的表面活性剂类似物。与表面活性剂相比，我们开发的类似物之一 SLP5 的溶血活性较低，而抗病毒活性相同。SLP5 的选择性指数为 52，而表面活性剂的 SI 为 4，换句话说，SLP5 的安全有效浓度范围是表面活性剂的 12 倍。与表面活性剂一样，SLP5 对 PEDV 具有直接的抗病毒作用。结构上，SLP5 是一种带有三个羧基的线性脂肽。通过表面活性剂的内酯键水解以及全合成，可以得到类似于 SLP5 的表面活性剂衍生物。
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