Shaw T, Amor P, Civitico G, Boyd M, Locarnini S
Macfarlane Burnet Centre for Medical Research, Fairfield Hospital, Victoria, Australia.
Antimicrob Agents Chemother. 1994 Apr;38(4):719-23. doi: 10.1128/AAC.38.4.719.
The in vitro antihepadnavirus activities of the purine nucleoside analogs ganciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine) and penciclovir [9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine; BRL 39123] were compared in primary duck hepatocyte cultures congenitally infected with the duck hepatitis B virus (DHBV). Both compounds inhibited DHBV DNA replication to a comparable extent during continuous short-term treatment of the cultures. However penciclovir was more active both during longer-term continuous treatment (50% inhibitory concentrations: penciclovir, 0.7 +/- 0.1 microM; ganciclovir, 4.0 +/- 0.2 microM) and in washout experiments (50% inhibitory concentrations: penciclovir, 3.0 +/- 0.4 microM; ganciclovir, 46 +/- 1.5 microM) designed to compare the persistence of inhibitory activity after removal of the extracellular compound. The effects on viral protein synthesis were similar to the effects on viral DNA replication. These data suggest that penciclovir or its oral form, famciclovir, may have clinical utility in the treatment of chronic hepatitis B virus infection.
在先天性感染鸭乙型肝炎病毒（DHBV）的原代鸭肝细胞培养物中，比较了嘌呤核苷类似物更昔洛韦（9-[2-羟基-1-(羟甲基)乙氧基甲基]鸟嘌呤）和喷昔洛韦[9-(4-羟基-3-羟甲基丁-1-基)鸟嘌呤；BRL 39123]的体外抗乙肝病毒活性。在对培养物进行连续短期处理期间，这两种化合物对DHBV DNA复制的抑制程度相当。然而，在长期连续处理期间（50%抑制浓度：喷昔洛韦，0.7±0.1微摩尔；更昔洛韦，4.0±0.2微摩尔）以及在洗脱实验（50%抑制浓度：喷昔洛韦，3.0±0.4微摩尔；更昔洛韦，46±1.5微摩尔）中，喷昔洛韦的活性更高，洗脱实验旨在比较去除细胞外化合物后抑制活性的持续性。对病毒蛋白合成的影响与对病毒DNA复制的影响相似。这些数据表明，喷昔洛韦或其口服形式泛昔洛韦可能在慢性乙型肝炎病毒感染的治疗中具有临床应用价值。
