Sulfonic acid polymers are potent inhibitors of HIV-1 induced cytopathogenicity and the reverse transcriptases of both HIV-1 and HIV-2.
Sulfonic acid polymers are potent inhibitors of HIV-1 induced cytopathogenicity and the reverse transcriptases of both HIV-1 and HIV-2.
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磺酸聚合物是 HIV-1 诱导的细胞病变以及 HIV-1 和 HIV-2 逆转录酶的有效抑制剂。
DOI：
10.1016/0925-4439(93)90109-e
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发表时间：
1993
期刊：
影响因子：
--
通讯作者：
Mohan,P
中科院分区：
文献类型：
--
作者：
Tan,GT;Wickramasinghe,A;Verma,S;Hughes,SH;Pezzuto,JM;Baba,M;Mohan,P
评价了四种新型磺酸聚合物的体外HIV-1和HIV-2逆转录酶（RT）抑制活性，发现它们对两种RT具有等效性。芳香族聚合物显示出的IC 50值比脂肪族聚合物观察到的值低约103倍。在芳香族聚合物中，聚（4-苯乙烯磺酸）（PSS）（MW 8000; IC 50 = 0.02μg/ml）的效力是大约相同分子量范围的聚（茴香脑磺酸）（PAS）的3倍。PSS聚合物的活性与聚合物的尺寸成比例地增加，并且相对于苏拉明，活性可以增强超过200倍。这些聚合物还在对MT-4细胞无毒的浓度下抑制HIV-1的致细胞病变效应。这些稳定的磺酸聚合物的有效RT抑制特性表明，结构-活性研究是有必要的，以产生能够抑制病毒过程的多个阶段的药剂。
Four novel sulfonic acid polymers were evaluated for their in vitro HIV-1 and HIV-2 reverse transcriptase (RT) inhibitory activity and found to be equipotent against both RTs. The aromatic polymers demonstrated IC50values that were approximately 103-fold lower than those observed with the aliphatic polymers. Among the aromatic polymers, poly(4-styrenesulfonic acid) (PSS) (MW 8000; IC50= 0.02μg/ml) was 3-fold more potent than poly(anetholesulfonic acid) (PAS) of approximately the same molecular weight range. The activity of PSS polymers increased in proportion to the size of the polymers and, relative to suramin, activity could be enhanced over 200-fold. These polymers also inhibited the cytopathic effect of HIV-1 at concentrations that were non-toxic to MT-4 cells. The potent RT inhibitory properties of these stable sulfonic acid polymers suggest that structure-activity studies are warranted to yield agents capable of inhibiting multiple stages of the viral process.