Shipman C, Smith S H, Carlson R H, Drach J C
Antimicrob Agents Chemother. 1976 Jan;9(1):120-7. doi: 10.1128/AAC.9.1.120.
The drug 9-beta-d-arabinofuranosyladenine (ara-A) significantly suppressed the formation of herpes simplex virus type 1-induced syncytia in BHK-21/4 cells at concentrations as low as 0.1 mug/ml. Optimal activity was noted when the drug was added before initiation of viral deoxyribonucleic acid (DNA) synthesis (3.5 h postinfection). The deaminated derivative of ara-A, 9-beta-d-arabinofuranosylhypoxanthine (ara-H), was at least 10 times less effective in suppressing the development of herpes simplex virus-induced syncytia. The replication of herpes simplex virus was measured by assaying fluids and cells from infected drug-treated cultures by using a plaque production technique. Ara-A at drug levels of >10 < 32 mug/ml completely blocked the replication of infectious virus particles. Ara-H was less effective than ara-A in reducing the replication of virions. Rates of host and viral DNA synthesis were monitored by pulse labeling herpes simplex virus-infected synchronized KB cells with [(3)H]thymidine and subsequently separating viral from cellular DNA in CsCl density gradients. During synthetic (S) phase, ara-A or ara-H at concentrations ranging from 3.2 to 32 mug/ml selectively inhibited viral DNA synthesis. At 3.2 mug of ara-A per ml, viral DNA synthesis was reduced 74% although total cellular DNA synthesis was unaffected. Increasing concentrations of ara-A produced increasing temporal delays in the maximal rate of host DNA synthesis. This time shift was not observed in cells treated with ara-H.
药物9-β-D-阿拉伯呋喃糖基腺嘌呤(ara-A)在低至0.1微克/毫升的浓度下就能显著抑制单纯疱疹病毒1型在BHK-21/4细胞中诱导形成的多核巨细胞。在病毒脱氧核糖核酸(DNA)合成开始前(感染后3.5小时)添加该药物时,观察到最佳活性。ara-A的脱氨基衍生物9-β-D-阿拉伯呋喃糖基次黄嘌呤(ara-H)在抑制单纯疱疹病毒诱导的多核巨细胞形成方面的效果至少低10倍。通过使用噬斑形成技术检测感染药物处理培养物中的液体和细胞,来测量单纯疱疹病毒的复制情况。药物水平>10<32微克/毫升的ara-A完全阻断了感染性病毒颗粒的复制。ara-H在减少病毒粒子复制方面比ara-A效果差。通过用[³H]胸腺嘧啶脉冲标记单纯疱疹病毒感染的同步化KB细胞,随后在CsCl密度梯度中分离病毒DNA和细胞DNA,来监测宿主和病毒DNA的合成速率。在合成(S)期,浓度范围为3.2至32微克/毫升的ara-A或ara-H选择性地抑制病毒DNA合成。每毫升3.2微克的ara-A可使病毒DNA合成减少74%,而总细胞DNA合成不受影响。ara-A浓度增加会使宿主DNA合成最大速率出现越来越大的时间延迟。在用ara-H处理的细胞中未观察到这种时间变化。