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嘌呤核苷类似物的抗鼻病毒活性。

Antirhinovirus activity of purine nucleoside analogs.

作者信息

De Clercq E, Bernaerts R, Bergstrom D E, Robins M J, Montgomery J A, Holy A

出版信息

Antimicrob Agents Chemother. 1986 Mar;29(3):482-7. doi: 10.1128/AAC.29.3.482.

Abstract

A wide variety of purine nucleoside (mainly tubercidin and adenosine) analogs, which had previously been shown to inhibit the replication of a broad spectrum of RNA viruses, were evaluated for their antirhinovirus activity in human diploid (WI-38) fibroblasts. Tubercidin, 5-(1-hydroxyethyl)tubercidin, 5-(2-buten-1-yl)tubercidin, toyocamycin, and sangivamycin emerged as the most potent inhibitors. These compounds inhibited the replication of rhinovirus types 1A, 1B, and 9 at an MIC well below 1 microgram/ml. However, these compounds proved cytotoxic for the uninfected host cells at concentrations which were only slightly higher (3- to 10-fold, on the average) than those required for inhibition of rhinovirus replication. The most selective inhibitor of rhinovirus replication was 3-deazaguanine, with a selectivity index of 50. None of the carbocyclic and acyclic analogs of adenosine tested exhibited a potent or selective antirhinovirus activity.

摘要

此前已证明多种嘌呤核苷(主要是杀结核菌素和腺苷)类似物可抑制多种RNA病毒的复制,我们对其在人二倍体(WI-38)成纤维细胞中的抗鼻病毒活性进行了评估。杀结核菌素、5-(1-羟乙基)杀结核菌素、5-(2-丁烯-1-基)杀结核菌素、丰加霉素和放线菌素成为最有效的抑制剂。这些化合物在远低于1微克/毫升的最低抑菌浓度(MIC)下就能抑制1A、1B和9型鼻病毒的复制。然而,这些化合物在浓度仅略高于抑制鼻病毒复制所需浓度(平均高3至10倍)时,就被证明对未感染的宿主细胞具有细胞毒性。鼻病毒复制的最具选择性的抑制剂是3-脱氮鸟嘌呤,其选择性指数为50。所测试的腺苷的碳环和无环类似物均未表现出有效的或选择性抗鼻病毒活性。

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Antirhinovirus activity of purine nucleoside analogs.嘌呤核苷类似物的抗鼻病毒活性。
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