A new acyclic heterodinucleotide active against Human Immunodeficiency Virus and Herpes Simplex Virus
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- 作者：Franchetti ; Palmarisa ; Abu Sheikha ; Ghassan ; Cappellacci ; Loredana ; Marchetti ; Stefano ; Grifantini ; Mario ; et. al.
- 关键词：Acyclovir (ACV) ; Anti-HIV activity ; Anti-HSV activity ; Human macrophages ; (R)PMPA
- 刊名：Antiviral Research
- 出版年：2000
- 出版时间：September, 2000
- 年：2000
- 卷：47
- 期：3
- 页码：149-158
- 全文大小：140 K
文摘
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.