修饰的嘧啶核苷在体外对乙型肝炎病毒产生的强效抑制作用。
Potent inhibition of hepatitis B virus production in vitro by modified pyrimidine nucleosides.
作者信息
Matthes E, Langen P, von Janta-Lipinski M, Will H, Schröder H C, Merz H, Weiler B E, Müller W E
机构信息
Zentralinstitut für Molekularbiologie, Akademie der Wissenschaften der Deutschen Demokratischen Republik, Berlin-Buch, German Democratic Republic.
出版信息
Antimicrob Agents Chemother. 1990 Oct;34(10):1986-90. doi: 10.1128/AAC.34.10.1986.
2',3'-Dideoxy-3'-fluorothymidine (FddThd), 2',3'-didehydro-2',3'- dideoxythymidine (ddeThd), and 3'-fluoro-5-methyl-deoxycytidine (FddMeCyt) are, in their triphosphate forms, selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase. We report that 0.3 microM FddThd, FddMeCyt, or ddeThd as well as 3'-chloro-5-methyl-deoxycytidine (ClddMeCyt) or 3'-amino-5-methyl-deoxycytidine (AddMeCyt) almost completely blocked production of hepatitis B virus (HBV) particles by HBV DNA-transfected cell line 2.2.15 in vitro. Only at an at least 10-fold-higher concentration was a cytotoxic effect observed. These results indicate that FddThd, FddMeCyt, ClddMeCyt, AddMeCyt, and ddeThd are potent anti-HBV agents in vitro.
2',3'-二脱氧-3'-氟胸苷（FddThd）、2',3'-二脱氢-2',3'-二脱氧胸苷（ddeThd）和3'-氟-5-甲基脱氧胞苷（FddMeCyt），以其三磷酸酯形式，是1型人类免疫缺陷病毒逆转录酶的选择性抑制剂。我们报告，0.3微摩尔的FddThd、FddMeCyt或ddeThd，以及3'-氯-5-甲基脱氧胞苷（ClddMeCyt）或3'-氨基-5-甲基脱氧胞苷（AddMeCyt），几乎完全阻断了乙肝病毒（HBV）DNA转染的细胞系2.2.15在体外产生乙肝病毒颗粒。仅在至少高10倍的浓度下才观察到细胞毒性作用。这些结果表明，FddThd、FddMeCyt、ClddMeCyt、AddMeCyt和ddeThd在体外是有效的抗乙肝病毒药物。
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