无环核苷膦酸酯对组织培养中人类乙型肝炎病毒和鸭乙型肝炎病毒感染的抑制作用。
Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture.
作者信息
Heijtink R A, Kruining J, de Wilde G A, Balzarini J, de Clercq E, Schalm S W
机构信息
Department of Virology, Erasmus University Rotterdam, The Netherlands.
出版信息
Antimicrob Agents Chemother. 1994 Sep;38(9):2180-2. doi: 10.1128/AAC.38.9.2180.
Abstract
The inhibitory effects of the 9-(2-phosphonylmethoxyethyl)adenine-related compounds (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-adenine, (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine, and (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine on human hepatitis B virus replication in the human hepatoma cell line HepG2 2.2.15 and duck hepatitis B virus infection in primary duck hepatocytes were investigated. (R)-9-(2-phosphonylmethoxypropyl-2,6-diaminopurine had the lowest 50% inhibitory concentrations against hepatitis B virus and duck hepatitis B virus, 0.22 and 0.06 microM, respectively, i.e., two- to fivefold lower concentrations than required for (R)-9-(2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxyethyl)adenine. All compounds were not toxic in vitro at a concentration of 100 microM.
摘要
研究了9-(2-膦酰甲氧基乙基)腺嘌呤相关化合物(S)-9-(3-羟基-2-膦酰甲氧基丙基)腺嘌呤、(S)-9-(3-氟-2-膦酰甲氧基丙基)腺嘌呤、(R)-9-(2-膦酰甲氧基丙基)腺嘌呤、(R)-9-(2-膦酰甲氧基丙基)-2,6-二氨基嘌呤和(S)-1-(3-羟基-2-膦酰甲氧基丙基)胞嘧啶对人肝癌细胞系HepG2 2.2.15中乙型肝炎病毒复制及原代鸭肝细胞中鸭乙型肝炎病毒感染的抑制作用。(R)-9-(2-膦酰甲氧基丙基)-2,6-二氨基嘌呤对乙型肝炎病毒和鸭乙型肝炎病毒的50%抑制浓度最低，分别为0.22和0.06微摩尔，即比(R)-9-(2-膦酰甲氧基丙基)腺嘌呤和9-(2-膦酰甲氧基乙基)腺嘌呤所需浓度低两到五倍。所有化合物在100微摩尔浓度下体外均无毒性。
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