Nakamura K, Eizuru Y, Kumura K, Minamishima Y
Department of Microbiology, Miyazaki Medical College, Japan.
J Med Virol. 1990 Jun;31(2):141-7. doi: 10.1002/jmv.1890310212.
The antiviral activities of antileukemic drugs 1-beta-D-arabinofuranosylcytosine (Cytarabine; Ara-C), 2,2'-anhydro-1-beta-D-arabinofuranosylcytosine (Ancitabine; Cyclo-C), and N4-behenoyl-1-beta-D-arabinofuranosylcytosine (Enocitabine; BH-AC) were evaluated in vitro against human cytomegalovirus (HCMV) in comparison with those of five other antiviral drugs. Both Ara-C and Cyclo-C showed the strongest inhibitory effect to HCMV. BH-AC inhibited the replication of HCMV and depicted almost as the same dose-response curve as Ganciclovir (DHPG). In the presence of Ara-C, Cyclo-C, or BH-AC, triphosphate forms of the nucleoside analogs were detected in the HCMV-infected cells, and synthesis of HCMV DNA was strongly suppressed. Thus, Ara-C, Cyclo-C, and BH-AC were not only antileukemic, but also antiviral in vitro. However, Ara-C and Cyclo-C may not be suitable as anti-HCMV agents, because they are cytotoxic or excreted rapidly in the urine in vivo [Van Voris, 1984; Hirayama et al., 1974]. Because of lower toxicity and longer retention in vivo, BH-AC may be expected as an anti-HCMV agent in patients with leukemia, in addition to serving as an antileukemic drug.
将抗白血病药物1-β-D-阿拉伯呋喃糖基胞嘧啶（阿糖胞苷；Ara-C）、2,2'-脱水-1-β-D-阿拉伯呋喃糖基胞嘧啶（安西他滨；环胞苷）和N4-山嵛酰-1-β-D-阿拉伯呋喃糖基胞嘧啶（依诺他滨；BH-AC）的抗病毒活性与其他五种抗病毒药物进行了体外抗人巨细胞病毒（HCMV）活性评估。Ara-C和环胞苷对HCMV均显示出最强的抑制作用。BH-AC抑制了HCMV的复制，其剂量-反应曲线与更昔洛韦（DHPG）几乎相同。在存在Ara-C、环胞苷或BH-AC的情况下，在HCMV感染的细胞中检测到了核苷类似物的三磷酸形式，并且HCMV DNA的合成受到强烈抑制。因此，Ara-C、环胞苷和BH-AC不仅具有抗白血病作用，在体外也具有抗病毒作用。然而，Ara-C和环胞苷可能不适合作为抗HCMV药物，因为它们具有细胞毒性或在体内经尿液快速排泄[Van Voris，1984；Hirayama等人，1974]。由于毒性较低且在体内保留时间较长，BH-AC除了作为抗白血病药物外，有望成为白血病患者的抗HCMV药物。
