Franchetti P, Abu Sheikha G, Cappellacci L, Marchetti S, Grifantini M, Balestra E, Perno C, Benatti U, Brandi G, Rossi L, Magnani M
Dipartimento di Scienze Chimiche, Università di Camerino, 62032, Camerino, Italy.
Antiviral Res. 2000 Sep;47(3):149-58. doi: 10.1016/s0166-3542(00)00101-7.
The most common therapies against human herpes virus (HSV-1) and human immunodeficiency virus (HIV-1) infectivity are based on the administration of nucleoside analogues. Acyclovir (ACV) is the drug of choice against HSV-1 infection, while the acyclic nucleoside phosphonate analogue PMPA has shown marked anti-HIV activity in a phase I and II clinical studies. As monocyte-derived macrophages are assumed to be important as reservoirs of both HSV-1 and HIV-1 infection, new approaches able to inhibit replication of both viruses in macrophages should be welcome. ACVpPMPA, a new heterodinucleotide consisting of both an antiherpetic and an antiretroviral drug bound by a phosphate bridge, was synthesized and encapsulated into autologous erythrocytes modified to increase their phagocytosis by human macrophages. ACVpPMPA-loaded erythrocytes provided an effective in vitro protection against both HSV-1 and HIV-1 replication in human macrophages.
针对人类疱疹病毒（HSV-1）和人类免疫缺陷病毒（HIV-1）感染性的最常见治疗方法是基于核苷类似物的给药。阿昔洛韦（ACV）是对抗HSV-1感染的首选药物，而无环核苷膦酸类似物PMPA在I期和II期临床研究中已显示出显著的抗HIV活性。由于单核细胞衍生的巨噬细胞被认为是HSV-1和HIV-1感染的重要储存库，因此能够抑制两种病毒在巨噬细胞中复制的新方法应该会受到欢迎。ACVpPMPA是一种新的杂二核苷酸，由通过磷酸桥连接的抗疱疹病毒药物和抗逆转录病毒药物组成，它被合成并封装到经过修饰的自体红细胞中，以增加人类巨噬细胞对其的吞噬作用。负载ACVpPMPA的红细胞在体外为人类巨噬细胞提供了针对HSV-1和HIV-1复制的有效保护。
