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阿昔洛韦膦酸酯衍生物的细胞代谢及其与α2-干扰素联合使用时的抗疱疹病毒活性

Cell metabolism of acyclovir phosphonate derivatives and antiherpesvirus activity of their combinations with alpha2-interferon.

作者信息

Skoblov Yuri S, Karpenko Inna L, Jasko Maxim V, Kukhanova Marina K, Andronova Valery L, Galegov Georgy A, Sidorov Georgy V, Myasoedov Nicolai F

机构信息

Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 32 Vavilov str., Moscow 119991, Russian Federation.

出版信息

Chem Biol Drug Des. 2007 Jun;69(6):429-34. doi: 10.1111/j.1747-0285.2007.00517.x.

Abstract

The combinational use of acyclovir (ACV) phosphonate esters and alpha(2)-interferon was shown to produce a synergistic effect on inhibition of HSV-1 replication in Vero cell cultures. Unlike other acyclovir phosphonate derivatives studied earlier, ACV H-phosphonate is not an ACV prodrug. On penetrating into the cells, it may be directly converted into ACV monophosphate escaping dephosphonylation-phosphorylation steps.

摘要

阿昔洛韦(ACV)膦酸酯与α(2)-干扰素联合使用,在Vero细胞培养中对单纯疱疹病毒1型(HSV-1)复制的抑制产生协同效应。与之前研究的其他阿昔洛韦膦酸衍生物不同,阿昔洛韦氢膦酸酯不是阿昔洛韦前药。它进入细胞后,可能直接转化为阿昔洛韦单磷酸酯,从而避开去磷酸化-磷酸化步骤。

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