双脱氧核苷类似物在静息和活化外周血单个核细胞中抗1型人类免疫缺陷病毒活性的比较分析
Comparative analysis of anti-human immunodeficiency virus type 1 activities of dideoxynucleoside analogs in resting and activated peripheral blood mononuclear cells.
作者信息
Shirasaka T, Chokekijchai S, Yamada A, Gosselin G, Imbach J L, Mitsuya H
机构信息
Experimental Retrovirology Section, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892, USA.
出版信息
Antimicrob Agents Chemother. 1995 Nov;39(11):2555-9. doi: 10.1128/AAC.39.11.2555.
Abstract
We determined the anti-human immunodeficiency virus type 1 (anti-HIV-1) activities of various dideoxy-nucleoside analogs by using phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMs) and resting PBMs (R-PBMs) as target cells. The comparative order of anti-HIV-1 activity in PHA-PBMs was azidothymidine (AZT) > dideoxycytidine (ddC) > dideoxythymidinene (d4T) > dideoxyinosine (ddI) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) > 2'-beta-fluoro-dideoxyadenosine (F-ara-ddA), while that in R-PBMs was ddC > ddI, PMEA, and F-ara-ddA, >> AZT and d4T. A pronucleotide, bis-(S-acetylthioethanol)phosphotriester-ddAMP, which bypasses the anabolic monophosphorylation step for the intracellular delivery of ddAMP, was highly active both in PHA-PBMs and R-PBMs. These data may have basic and clinical relevance in the design of anti-HIV chemotherapy, particularly combination chemotherapy with dideoxynucleosides, and in the development of active pronucleotides.
摘要
我们以植物血凝素激活的外周血单个核细胞（PHA - PBMs）和静息外周血单个核细胞（R - PBMs）作为靶细胞，测定了各种双脱氧核苷类似物的抗1型人类免疫缺陷病毒（抗HIV - 1）活性。PHA - PBMs中抗HIV - 1活性的比较顺序为：叠氮胸苷（AZT）>双脱氧胞苷（ddC）>双脱氧胸苷（d4T）>双脱氧肌苷（ddI）以及9 - （2 - 膦酰甲氧基乙基）腺嘌呤（PMEA）> 2'-β - 氟双脱氧腺苷（F - ara - ddA），而在R - PBMs中为ddC > ddI、PMEA和F - ara - ddA >> AZT和d4T。一种前体药物，双 - （S - 乙酰硫代乙醇）磷酸三酯 - ddAMP，它绕过了ddAMP细胞内递送的合成代谢单磷酸化步骤，在PHA - PBMs和R - PBMs中均具有高活性。这些数据在抗HIV化疗设计，特别是与双脱氧核苷的联合化疗设计以及活性前体药物的研发中可能具有基础和临床相关性。
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