Machida H, Sakata S, Morozumi M, Kiyanagi T, Kuninaka A, Yoshino H
Antiviral Res. 1982 Sep;2(4):217-26. doi: 10.1016/0166-3542(82)90044-4.
In vitro and in vivo anti-herpes activities of 1-beta-D-arabinofuranosylthymine 5'-monophosphate (ara-TMP) were compared with those of 1-beta-D-arabinofuranosylthymine (ara-T). On a molar basis ara-TMP was almost as active as ara-T against six strains of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) as monitored by a cytopathogenicity-inhibition and a plaque reduction assay in human embryonic lung fibroblast cells. When tested against experimental encephalitis in mice inoculated intracerebrally with HSV-1, intraperitoneal or intravenous treatment with 150 mg/kg/day of ara-TMP or 100 mg/kg/day of ara-T, for 5 days was effective in increasing in the mean survival time of mice. For a single dose of ara-TMP, intravenous administration was more effective than intraperitoneal or oral administration. However, oral administration of ara-T was the most effective of the treatment regimens used. Substantial plasma levels of ara-T were detected for a longer time after oral administration of ara-T than after intravenous administration of ara-TMP or ara-T, suggesting that the efficacy of oral administration of ara-T may be correlated with the maintenance of the substantial blood drug levels.
将1-β-D-阿拉伯呋喃糖基胸腺嘧啶5'-单磷酸酯（ara-TMP）的体外和体内抗疱疹活性与1-β-D-阿拉伯呋喃糖基胸腺嘧啶（ara-T）的进行了比较。在人胚肺成纤维细胞中，通过细胞病变抑制和蚀斑减少试验监测，在摩尔基础上，ara-TMP对6株1型单纯疱疹病毒（HSV-1）和2型单纯疱疹病毒（HSV-2）的活性几乎与ara-T相同。当用HSV-1脑内接种的小鼠进行实验性脑炎试验时，腹腔内或静脉内给予150mg/kg/天的ara-TMP或100mg/kg/天的ara-T，持续5天，可有效延长小鼠的平均存活时间。对于单剂量的ara-TMP，静脉内给药比腹腔内或口服给药更有效。然而，口服ara-T是所用治疗方案中最有效的。口服ara-T后比静脉内给予ara-TMP或ara-T后更长时间检测到相当高的血浆ara-T水平，这表明口服ara-T的疗效可能与维持相当高的血药水平有关。
