（-）-顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶（524W91）可抑制原代人肝细胞中的乙型肝炎病毒复制。
(-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (524W91) inhibits hepatitis B virus replication in primary human hepatocytes.
作者信息
Condreay L D, Condreay J P, Jansen R W, Paff M T, Averett D R
机构信息
Division of Experimental Therapy, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709, USA.
出版信息
Antimicrob Agents Chemother. 1996 Feb;40(2):520-3. doi: 10.1128/AAC.40.2.520.
Abstract
The anti-hepatitis B virus (HBV) activity of (-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (524W91) in cultures of primary human hepatocytes was examined. 524W91 was anabolized to the active 5'-triphosphate in these cells. HBV replication was equally inhibited in cultures incubated with 524W91 when the drug was added 24 h preinfection, at infection, or 24 h postinfection. 524W91 inhibited HBV replication by 50% at less than 20 nM in human hepatocytes.
摘要
检测了（-）-顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶（524W91）在原代人肝细胞培养物中的抗乙型肝炎病毒（HBV）活性。524W91在这些细胞中被代谢为活性5'-三磷酸。当在感染前24小时、感染时或感染后24小时添加该药物时，524W91在培养物中对HBV复制的抑制作用相同。在人肝细胞中，524W91在低于20 nM时对HBV复制的抑制率达50%。
相似文献
1
(-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine (524W91) inhibits hepatitis B virus replication in primary human hepatocytes.（-）-顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶（524W91）可抑制原代人肝细胞中的乙型肝炎病毒复制。
Antimicrob Agents Chemother. 1996 Feb;40(2):520-3. doi: 10.1128/AAC.40.2.520.
2
Pharmacokinetics, oral bioavailability, and metabolism in mice and cynomolgus monkeys of (2'R,5'S-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine, an agent active against human immunodeficiency virus and human hepatitis B virus.(2'R,5'S)-顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶在小鼠和食蟹猴体内的药代动力学、口服生物利用度及代谢，该药物对人类免疫缺陷病毒和乙型肝炎病毒具有活性。
Antimicrob Agents Chemother. 1994 Dec;38(12):2722-9. doi: 10.1128/AAC.38.12.2722.
3
The anti-hepatitis B virus activities, cytotoxicities, and anabolic profiles of the (-) and (+) enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine.顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶的(-)和(+)对映体的抗乙型肝炎病毒活性、细胞毒性及合成代谢特征
Antimicrob Agents Chemother. 1992 Dec;36(12):2686-92. doi: 10.1128/AAC.36.12.2686.
4
Evaluation of the potent anti-hepatitis B virus agent (-) cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine in a novel in vivo model.在一种新型体内模型中对强效抗乙肝病毒药物（-）顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的评估。
Antimicrob Agents Chemother. 1994 Mar;38(3):616-9. doi: 10.1128/AAC.38.3.616.
5
In vivo antiviral activity and pharmacokinetics of (-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine in woodchuck hepatitis virus-infected woodchucks.(-)-顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶在土拨鼠肝炎病毒感染的土拨鼠体内的抗病毒活性及药代动力学
Antimicrob Agents Chemother. 1997 Oct;41(10):2076-82. doi: 10.1128/AAC.41.10.2076.
6
Pharmacokinetics, oral bioavailability, and metabolic disposition in rats of (-)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine, a nucleoside analog active against human immunodeficiency virus and hepatitis B virus.（-）-顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶在大鼠体内的药代动力学、口服生物利用度及代谢情况，该核苷类似物对人类免疫缺陷病毒和乙型肝炎病毒具有活性。
Antimicrob Agents Chemother. 1993 Nov;37(11):2285-92. doi: 10.1128/AAC.37.11.2285.
7
Efficacy of lamivudine on replication of hepatitis B virus in HIV-infected patients.拉米夫定对HIV感染患者体内乙型肝炎病毒复制的疗效。
Lancet. 1995 Feb 11;345(8946):396-7. doi: 10.1016/s0140-6736(95)90388-7.
8
Intracellular metabolism of (-)- and (+)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine in HepG2 derivative 2.2.15 (subclone P5A) cells.（-）-和（+）-顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶在HepG2衍生物2.2.15（亚克隆P5A）细胞中的细胞内代谢
Antimicrob Agents Chemother. 1994 Jun;38(6):1230-8. doi: 10.1128/AAC.38.6.1230.
9
Use of the hepatitis B virus recombinant baculovirus-HepG2 system to study the effects of (-)-beta-2',3'-dideoxy-3'-thiacytidine on replication of hepatitis B virus and accumulation of covalently closed circular DNA.利用乙肝病毒重组杆状病毒-HepG2系统研究（-）-β-2'，3'-二脱氧-3'-硫代胞苷对乙肝病毒复制及共价闭合环状DNA积累的影响。
Antimicrob Agents Chemother. 1999 Aug;43(8):2017-26. doi: 10.1128/AAC.43.8.2017.
10
Synthesis, in vitro anti-HIV and anti-hepatitis B activities and pharmacokinetic properties of amphiphilic heterodinucleoside phosphates containing ddC and AZT.含双脱氧胞苷（ddC）和叠氮胸苷（AZT）的两亲性杂二核苷磷酸酯的合成、体外抗HIV和抗乙肝病毒活性及药代动力学性质
Nucleosides Nucleotides. 1999 Apr-May;18(4-5):949-50. doi: 10.1080/15257779908041609.
引用本文的文献
1
Putative Repurposing of Lamivudine, a Nucleoside/Nucleotide Analogue and Antiretroviral to Improve the Outcome of Cancer and COVID-19 Patients.核苷/核苷酸类似物及抗逆转录病毒药物拉米夫定的潜在新用途：改善癌症和新冠肺炎患者的治疗效果
Front Oncol. 2021 Jul 21;11:664794. doi: 10.3389/fonc.2021.664794. eCollection 2021.
2
Clinical potential of emerging new agents in hepatitis B.新型乙肝治疗药物的临床潜力
Drugs. 2000 Oct;60(4):701-10. doi: 10.2165/00003495-200060040-00001.
3
Treatment of chronic hepatitis B: new antiviral therapies.慢性乙型肝炎的治疗：新的抗病毒疗法
Curr Gastroenterol Rep. 1999 Feb-Mar;1(1):20-6. doi: 10.1007/s11894-999-0082-7.
4
Pharmacokinetics of beta-L-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys.β-L-2',3'-二脱氧-5-氟胞苷在恒河猴体内的药代动力学
Antimicrob Agents Chemother. 1999 Apr;43(4):920-4. doi: 10.1128/AAC.43.4.920.
本文引用的文献
1
Reproducible high level infection of cultured adult human hepatocytes by hepatitis B virus: effect of polyethylene glycol on adsorption and penetration.乙型肝炎病毒对培养的成人人类肝细胞进行可重复的高水平感染：聚乙二醇对吸附和穿透的影响。
Virology. 1993 Feb;192(2):534-40. doi: 10.1006/viro.1993.1069.
2
High-capacity in vitro assessment of anti-hepatitis B virus compound selectivity by a virion-specific polymerase chain reaction assay.通过病毒粒子特异性聚合酶链反应测定法对抗乙型肝炎病毒化合物选择性进行高容量体外评估。
Antimicrob Agents Chemother. 1993 Mar;37(3):441-7. doi: 10.1128/AAC.37.3.441.
3
Evaluation of the potent anti-hepatitis B virus agent (-) cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine in a novel in vivo model.在一种新型体内模型中对强效抗乙肝病毒药物（-）顺式-5-氟-1-[2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的评估。
Antimicrob Agents Chemother. 1994 Mar;38(3):616-9. doi: 10.1128/AAC.38.3.616.
4
Isolation, culture, and transplantation of human hepatocytes.人肝细胞的分离、培养和移植。
J Natl Cancer Inst. 1982 May;68(5):771-8.
5
Production of hepatitis B virus particles in Hep G2 cells transfected with cloned hepatitis B virus DNA.用克隆的乙型肝炎病毒DNA转染Hep G2细胞后乙型肝炎病毒颗粒的产生。
Proc Natl Acad Sci U S A. 1987 Feb;84(4):1005-9. doi: 10.1073/pnas.84.4.1005.
6
Stable expression and replication of hepatitis B virus genome in an integrated state in a human hepatoma cell line transfected with the cloned viral DNA.乙型肝炎病毒基因组在转染了克隆病毒DNA的人肝癌细胞系中以整合状态稳定表达和复制。
Proc Natl Acad Sci U S A. 1987 Jan;84(2):444-8. doi: 10.1073/pnas.84.2.444.
7
Analysis of plasma protein and lipoprotein synthesis in long-term primary cultures of baboon hepatocytes maintained in serum-free medium.
In Vitro Cell Dev Biol. 1989 Feb;25(2):174-82. doi: 10.1007/BF02626175.
8
Use of a low-speed, iso-density percoll centrifugation method to increase the viability of isolated rat hepatocyte preparations.使用低速等密度 Percoll 离心法提高分离的大鼠肝细胞制剂的活力。
In Vitro Cell Dev Biol. 1986 Apr;22(4):201-11. doi: 10.1007/BF02623304.
9
Replicative intermediates of hepatitis B virus in HepG2 cells that produce infectious virions.在产生传染性病毒粒子的HepG2细胞中乙型肝炎病毒的复制中间体。
J Virol. 1988 Aug;62(8):2836-44. doi: 10.1128/JVI.62.8.2836-2844.1988.
10
Cellular pharmacology of 2',3'-dideoxy-2',3'-didehydrothymidine, a nucleoside analog active against human immunodeficiency virus.2',3'-二脱氧-2',3'-二脱氢胸苷的细胞药理学，一种对人类免疫缺陷病毒有活性的核苷类似物。
Antimicrob Agents Chemother. 1989 Jun;33(6):844-9. doi: 10.1128/AAC.33.6.844.
Zotero 插件