Parris D S, Harrington J E
Antimicrob Agents Chemother. 1982 Jul;22(1):71-7. doi: 10.1128/AAC.22.1.71.
Acyclovir (ACV) has been shown to inhibit the replication of herpes simplex virus (HSV) in vitro. We examined a wide variety of HSV clinical isolates for the presence of naturally occurring ACV-resistant (ACVr) variants. Although the ACV doses that inhibited 50% of these isolates were within the range of doses inhibiting 50% of the ACV-susceptible wild-type strains, we successfully isolated variants resistant to high ACV concentrations (25 to 75 microM) from each virion population even in the absence of prior drug exposure. Furthermore, we demonstrated, by fluctuation analysis of two encephalitis strains, that the ACVr variants were clonally distributed in the virus populations before exposure to ACV and did not result from rapid adaptation to ACV. All variants isolated after a single exposure to a high dose of ACV were true ACVr variants, as demonstrated by their plating efficiencies in the presence of ACV. We found that 36 and 50% of the ACVr variants of the two strains examined in detail displayed plating efficiencies in phosphonoacetic acid of greater than 0.1, possibly indicating that many of the ACVr variants contained alterations in the DNA polymerase gene locus. Because the distribution of ACVr variants in natural populations is relatively high (10(-4), these results suggest that selection of ACVr strains during ACV therapy is possible.
阿昔洛韦(ACV)已被证明在体外可抑制单纯疱疹病毒(HSV)的复制。我们检测了多种HSV临床分离株,以确定是否存在天然的阿昔洛韦耐药(ACVr)变异株。尽管抑制这些分离株中50%的ACV剂量在抑制50%的ACV敏感野生型菌株的剂量范围内,但即使在未预先接触药物的情况下,我们仍成功地从每个病毒粒子群体中分离出了对高浓度ACV(25至75 microM)耐药的变异株。此外,通过对两株脑炎病毒株的波动分析,我们证明ACVr变异株在接触ACV之前就在病毒群体中呈克隆分布,并非由对ACV的快速适应所致。单次接触高剂量ACV后分离出的所有变异株均为真正的ACVr变异株,这在其在ACV存在下的平板接种效率中得到了证明。我们发现,详细检测的两株病毒株中,分别有36%和50%的ACVr变异株在膦甲酸中的平板接种效率大于0.1,这可能表明许多ACVr变异株的DNA聚合酶基因位点发生了改变。由于ACVr变异株在自然群体中的分布相对较高(10^-4),这些结果表明在ACV治疗期间有可能选择出ACVr毒株。