一种水溶性、构型稳定的衍生化C60富勒烯的合成及杀病毒活性
Synthesis and virucidal activity of a water-soluble, configurationally stable, derivatized C60 fullerene.
作者信息
Schinazi R F, Sijbesma R, Srdanov G, Hill C L, Wudl F
机构信息
Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322.
出版信息
Antimicrob Agents Chemother. 1993 Aug;37(8):1707-10. doi: 10.1128/AAC.37.8.1707.
Abstract
The bis(monosuccinimide) derivative of p,p'-bis(2-aminoethyl)diphenyl-C60 (compound 1), prepared by the fulleroid route, is active against human immunodeficiency virus type 1 (HIV-1) and HIV-2 (50% effective concentration [EC50] averaging approximately 6 microM) in acutely or chronically infected human lymphocytes and is active in vitro against 3'-azido-3'-deoxythymidine-resistant HIV-1 (EC50, approximately 3 microM). The virucidal properties of compound 1 were confirmed by virus inactivation assays. Compound 1 was noncytotoxic up to 100 microM in peripheral blood mononuclear cells and H9, Vero, and CEM cells. In cell-free assays, whereas the fullerene showed comparable activity against HIV-1 reverse transcriptase and DNA polymerase alpha (50% inhibitory concentration of approximately 5 microM), it demonstrated selective activity against HIV-1 protease.
摘要
通过富勒烯途径制备的对，对'-双（2-氨基乙基）二苯基-C60的双（单琥珀酰亚胺）衍生物（化合物1），在急性或慢性感染的人淋巴细胞中对1型人类免疫缺陷病毒（HIV-1）和HIV-2具有活性（50%有效浓度[EC50]平均约为6 microM），并且在体外对3'-叠氮-3'-脱氧胸苷耐药的HIV-1具有活性（EC50，约为3 microM）。通过病毒灭活试验证实了化合物1的杀病毒特性。化合物1在高达100 microM的浓度下对外周血单核细胞以及H9、Vero和CEM细胞无细胞毒性。在无细胞试验中，虽然富勒烯对HIV-1逆转录酶和DNA聚合酶α表现出相当的活性（50%抑制浓度约为5 microM），但它对HIV-1蛋白酶表现出选择性活性。
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