氧杂环丁烷霉素G对豚鼠巨细胞病毒体内外感染的抗病毒作用。

Antiviral effect of oxetanocin G against guinea pig cytomegalovirus infection in vitro and in vivo.

作者信息

Yamamoto N, Yamada Y, Daikoku T, Nishiyama Y, Tsutsui Y, Shimada N, Takahashi K

机构信息

Laboratory of Virology, Research Institute for Disease Mechanism and Control, Nagoya University School of Medicine, Japan.

出版信息

J Antibiot (Tokyo). 1990 Dec;43(12):1573-8. doi: 10.7164/antibiotics.43.1573.

DOI:10.7164/antibiotics.43.1573

PMID:2177463

Abstract

The antiviral activity of a new guanosine analog, 9-(2-deoxy-2-hydroxymethyl-beta-D-erythrooxetanosyl)guanine (OXT-G), against guinea pig cytomegalovirus (GPCMV) was evaluated both in vitro and in vivo. In the plaque reduction assay, the median effective concentration (EC50) of OXT-G, ganciclovir (DHPG) and acyclovir (ACV) against GPCMV was 0.03, 6.4 and 52 micrograms/ml, respectively. The selectivity index, based on the ratio of the median inhibitory concentration for cell growth of guinea pig embryo fibroblasts to the median effective concentration for GPCMV plaque formation, was about 100-fold higher than that of DHPG. In an in vivo study, Hartley guinea pigs infected with GPCMV were treated with OXT-G or DHPG (20 mg/kg/day) for 2 weeks, and it was found that virus titers in the salivary gland were 70-fold lower in OXT-G-treated guinea pigs than in DHPG-treated animals. The results indicate that OXT-G was more potent and selective against GPCMV infection than DHPG.

摘要

一种新型鸟苷类似物9-(2-脱氧-2-羟甲基-β-D-赤藓糖氧杂环丁烷基)鸟嘌呤（OXT-G）对豚鼠巨细胞病毒（GPCMV）的抗病毒活性在体外和体内均进行了评估。在蚀斑减少试验中，OXT-G、更昔洛韦（DHPG）和阿昔洛韦（ACV）对GPCMV的半数有效浓度（EC50）分别为0.03、6.4和52微克/毫升。基于豚鼠胚胎成纤维细胞生长的半数抑制浓度与GPCMV蚀斑形成的半数有效浓度之比的选择性指数比DHPG高约100倍。在一项体内研究中，用OXT-G或DHPG（20毫克/千克/天）对感染GPCMV的哈特利豚鼠进行2周治疗，发现OXT-G治疗的豚鼠唾液腺中的病毒滴度比DHPG治疗的动物低70倍。结果表明，OXT-G对GPCMV感染比DHPG更有效且更具选择性。