Dipartimento di Farmacia, Università di Napoli Federico II, and DFM Scarl, Napoli, Italia.
Int J Nanomedicine. 2013;8:521-34. doi: 10.2147/IJN.S37739. Epub 2013 Feb 5.
This contribution reports the synthesis of a poly(amide)-based dendrimer functionalized at the termini with a membrane-interacting peptide derived from the herpes simplex virus (HSV) type 1 glycoprotein H, namely gH625-644. This peptide has been shown to interact with model membranes and to inhibit viral infectivity. The peptidodendrimer inhibits both HSV-1 and HSV-2 at a very early stage of the entry process, most likely through an interaction with the viral envelope glycoproteins; thus, preventing the virus from coming into close contact with cellular membranes, a prerequisite of viral internalization. The 50% inhibitory concentration was 100 and 300 nM against HSV-1 and HSV-2 respectively, with no evidence of cell toxicity at these concentrations. These results show that the functionalization of a dendrimer with the peptide sequence derived from an HSV glycoprotein shows promising inhibitory activity towards viruses of the Herpesviridae family.
本研究报告了一种基于聚酰胺的树枝状大分子的合成，其末端功能化了来自单纯疱疹病毒 (HSV) 1 型糖蛋白 H 的膜相互作用肽，即 gH625-644。该肽已被证明与模型膜相互作用，并抑制病毒感染性。该肽树状大分子在进入过程的非常早期阶段抑制 HSV-1 和 HSV-2，很可能通过与病毒包膜糖蛋白相互作用；从而阻止病毒与细胞膜近距离接触，这是病毒内化的前提。对 HSV-1 和 HSV-2 的 50%抑制浓度分别为 100 和 300 nM，在这些浓度下没有细胞毒性的证据。这些结果表明，用来自 HSV 糖蛋白的肽序列功能化树枝状大分子对疱疹病毒科的病毒显示出有希望的抑制活性。
