（S）-1-（3-羟基-2-膦酰甲氧基丙基）胞嘧啶（HPMPC）体外抗人巨细胞病毒活性的特殊特性。

Particular characteristics of the anti-human cytomegalovirus activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC) in vitro.

作者信息

Neyts J, Snoeck R, Balzarini J, De Clercq E

机构信息

Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.

出版信息

Antiviral Res. 1991 Jul;16(1):41-52. doi: 10.1016/0166-3542(91)90057-x.

DOI:10.1016/0166-3542(91)90057-x

PMID:1663729

Abstract

The acyclic nucleoside phosphonate analogue (S)-1-[3-hydroxy-2-phosphonylmethoxypropyl]cytosine (HPMPC) is a potent and selective inhibitor of human cytomegalovirus (HCMV) replication and DNA synthesis. Unlike 9-(1,3-dihydroxy-2-propoxymethyl)guanine (DHPG), HPMPC inhibits HCMV replication in cell cultures which have been treated with the compound before infection. Upon short-pulse treatment of HCMV-infected cells with HPMPC, a long-lasting antiviral response is obtained. The antiviral activity of HPMPC, unlike the antiviral activity of other cytosine derivatives (i.e. Ara-C, FIAC), is not readily reversed by 2'-deoxycytidine or cytidine. Neutral and alkaline sucrose gradient analysis of HCMV DNA isolated from HPMPC-treated HCMV-infected cell cultures revealed that HPMPC does not cause (detectable) single- or double-strand breakage of HCMV DNA.

摘要

无环核苷膦酸类似物（S）-1-[3-羟基-2-膦酰甲氧基丙基]胞嘧啶（HPMPC）是一种强效且具有选择性的人巨细胞病毒（HCMV）复制及DNA合成抑制剂。与9-(1,3-二羟基-2-丙氧甲基)鸟嘌呤（DHPG）不同，HPMPC可在感染前用该化合物处理过的细胞培养物中抑制HCMV复制。在用HPMPC对HCMV感染的细胞进行短脉冲处理后，可获得持久的抗病毒反应。与其他胞嘧啶衍生物（即阿糖胞苷、氟阿糖胞苷）的抗病毒活性不同，HPMPC的抗病毒活性不易被2'-脱氧胞苷或胞苷逆转。对从经HPMPC处理的HCMV感染细胞培养物中分离出的HCMV DNA进行中性和碱性蔗糖梯度分析表明，HPMPC不会导致（可检测到的）HCMV DNA单链或双链断裂。