• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

抗病毒无环核苷酸类似物9-(2-膦酰甲氧基乙基)腺嘌呤的匹伏酯前药对小鼠巨噬细胞一氧化氮合酶表达的抑制作用

Inhibition of murine macrophage nitric oxide synthase expression by a pivoxil prodrug of antiviral acyclic nucleotide analogue 9-(2-phosphonomethoxyethyl)adenine.

作者信息

Zídek Z, Franková D, Holý A, Boubelík M, Dráber P

机构信息

Institute of Pharmacology, Academy of Sciences of the Czech Republic, Prague.

出版信息

Biochem Pharmacol. 1997 Oct 15;54(8):855-61. doi: 10.1016/s0006-2952(97)00228-1.

DOI:10.1016/s0006-2952(97)00228-1
PMID:9354585
Abstract

The effect of the acyclic nucleotide analogue, 9-(2-phosphonomethoxyethyl)adenine (PMEA, Adefovir), and its (bis)pivaloyloxymethyl ester (bis-POM-PMEA, Adefovir Dipivoxil) on in vitro nitric oxide (NO) production by murine peritoneal macrophages was investigated. Bis-POM-PMEA inhibited in a concentration-dependent manner the formation of NO generated by interferon-gamma and lipopolysaccharide, the IC50 being 15 microM. Suppressed transcription of mRNA for inducible NO synthase (EC 1.14.13.39) resulting in decreased synthesis of NO synthase protein was found. Parent compound PMEA was virtually ineffective.

摘要

研究了无环核苷酸类似物9-(2-膦酰甲氧基乙基)腺嘌呤（PMEA，阿德福韦）及其（双）新戊酰氧甲基酯（双-POM-PMEA，阿德福韦酯）对小鼠腹腔巨噬细胞体外产生一氧化氮（NO）的影响。双-POM-PMEA以浓度依赖性方式抑制由γ-干扰素和脂多糖产生的NO的形成，IC50为15μM。发现诱导型一氧化氮合酶（EC 1.14.13.39）的mRNA转录受到抑制，导致一氧化氮合酶蛋白合成减少。母体化合物PMEA实际上无效。

相似文献

1
Inhibition of murine macrophage nitric oxide synthase expression by a pivoxil prodrug of antiviral acyclic nucleotide analogue 9-(2-phosphonomethoxyethyl)adenine.抗病毒无环核苷酸类似物9-(2-膦酰甲氧基乙基)腺嘌呤的匹伏酯前药对小鼠巨噬细胞一氧化氮合酶表达的抑制作用
Biochem Pharmacol. 1997 Oct 15;54(8):855-61. doi: 10.1016/s0006-2952(97)00228-1.
2
Cytotoxicity of pivoxil esters of antiviral acyclic nucleoside phosphonates: adefovir dipivoxil versus adefovir.抗病毒无环核苷膦酸酯的匹伏酯的细胞毒性：阿德福韦酯与阿德福韦的比较
Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2005 Dec;149(2):315-9. doi: 10.5507/bp.2005.049.
3
Chemokines, nitric oxide and antiarthritic effects of 9-(2-phosphonomethoxyethyl)adenine (Adefovir).趋化因子、一氧化氮与9-(2-膦酰甲氧基乙基)腺嘌呤（阿德福韦）的抗关节炎作用
Eur J Pharmacol. 1999 Jul 2;376(1-2):91-100. doi: 10.1016/s0014-2999(99)00343-x.
4
Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.口服双（新戊酰氧甲基）-9-（2-膦酰甲氧基乙基）腺嘌呤（9-（2-膦酰甲氧基乙基）腺嘌呤的双（新戊酰氧甲基）酯前药）在小鼠体内的抗逆转录病毒活性和药代动力学。
Antimicrob Agents Chemother. 1996 Jan;40(1):22-8. doi: 10.1128/AAC.40.1.22.
5
Macrophage activation by antiviral acyclic nucleoside phosphonates in dependence on priming immune stimuli.抗病毒无环核苷膦酸酯对巨噬细胞的激活作用依赖于启动免疫刺激。
Int J Immunopharmacol. 2000 Dec;22(12):1121-9. doi: 10.1016/s0192-0561(00)00068-0.
6
Design, synthesis and evaluation of novel oxazaphosphorine prodrugs of 9-(2-phosphonomethoxyethyl)adenine (PMEA, adefovir) as potent HBV inhibitors.新型氧杂磷杂环己烷磷酰胺前药的设计、合成与评价，其为 9-(2-磷酰甲氧基乙基)腺嘌呤（PMEA，阿德福韦）的强效 HBV 抑制剂。
Bioorg Med Chem Lett. 2009 Dec 15;19(24):6918-21. doi: 10.1016/j.bmcl.2009.10.072. Epub 2009 Oct 21.
7
Transport, uptake, and metabolism of the bis(pivaloyloxymethyl)-ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine in an in vitro cell culture system of the intestinal mucosa (Caco-2).9-(2-膦酰甲氧基乙基)腺嘌呤的双(新戊酰氧甲基)酯前药在肠黏膜体外细胞培养系统（Caco-2）中的转运、摄取及代谢
Pharm Res. 1997 Apr;14(4):492-6. doi: 10.1023/a:1012155717819.
8
Inhibition by 1'-acetoxychavicol acetate of lipopolysaccharide- and interferon-gamma-induced nitric oxide production through suppression of inducible nitric oxide synthase gene expression in RAW264 cells.
Carcinogenesis. 1998 Jun;19(6):1007-12. doi: 10.1093/carcin/19.6.1007.
9
Immunomodulatory properties of antiviral acyclic nucleotide analogues: cytokine stimulatory and nitric oxide costimulatory effects.抗病毒无环核苷酸类似物的免疫调节特性：细胞因子刺激和一氧化氮共刺激作用。
Int J Immunopharmacol. 1997 Sep-Oct;19(9-10):587-97. doi: 10.1016/s0192-0561(97)00047-7.
10
Synthesis and in vitro evaluation of a phosphonate prodrug: bis(pivaloyloxymethyl) 9-(2-phosphonylmethoxyethyl)adenine.一种膦酸酯前药的合成与体外评价：双（新戊酰氧甲基）9-（2-膦酰甲氧基乙基）腺嘌呤
Antiviral Res. 1992 Sep;19(3):267-73. doi: 10.1016/0166-3542(92)90084-i.

引用本文的文献

1
NUCLEOSIDE PRODRUGS OF A ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS.腺苷受体激动剂和拮抗剂的核苷前药。
Collect Czechoslov Chem Commun. 2006;71(6):912-928. doi: 10.1135/cccc20060912.
2
Screening of FDA-Approved Drug Library Identifies Adefovir Dipivoxil as Highly Potent Inhibitor of T Cell Proliferation.FDA 批准药物库筛选发现阿德福韦酯是一种强效的 T 细胞增殖抑制剂。
Front Immunol. 2021 Jan 8;11:616570. doi: 10.3389/fimmu.2020.616570. eCollection 2020.