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首页> 外文期刊>New Journal of Chemistry >Encapsulation of oxime acetylcholinesterase reactivators: influence of physiological conditions on the stability of oxime-cucurbit[7]uril complexes
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Encapsulation of oxime acetylcholinesterase reactivators: influence of physiological conditions on the stability of oxime-cucurbit[7]uril complexes

机译：肟乙酰胆碱酯酶酶反应器的封装：生理条件对肟 - 葫芦[7]尿道复合物的稳定性影响

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摘要

Oxime-based acetylcholinesterase reactivators are a specific group of drugs used for the treatment of organophosphate intoxication. However, high hydrophilicity and poor blood-brain barrier penetration limit their physiological potential. Cucurbit[7]urile (CB[7]) was used in this work as a potential carrier of oxime molecules to increase their treatment effectiveness. The host-guest chemistry of CB[7] with five clinically used oximes (trimedoxime, asoxime, obidoxime, pralidoxim and methoxime) and two new pre-clinical oximes (K027 and K048) was characterized under simulated physiological conditions using titration experiments with UV-vis detection. CB[7] forms stable complexes of 1 : 1 stoichiometry with all tested oximes. The decrease of complex stability was observed at a pH above the pK(a)of oxime, which limits the applicability of the complexation for oximes with pK(a)below the physiological pH. The combination of physiological ionic strength and pH causes partial decrease of the complex stability. The effect of organic solvent used in the sample pretreatment step before spectral analysis of oxime-CB[7] complexes in biological samples was demonstrated. Methanol is a more suitable solvent with low effect on complex stability. Finally, the ability of mass spectrometry with electrospray ionization was demonstrated for the analysis of oxime-CB[7] complexes.
机译：肟基乙酰胆碱酯酶反应器是用于治疗有机磷酸盐的特定药物组。然而，高亲水性和血脑障碍差的渗透率限制了它们的生理潜力。葫芦[7]尿布（Cb [7]）在这项工作中使用作为肟分子的潜在载体，以提高其治疗效果。 CB [7]的宿主化学化学与五种临床用过的肟（粉末肟，沥青，虫草，Pralidoxim和甲氧肟）和两个新的临床前肟（K027和K048）在模拟的生理条件下，使用滴定实验与UV- VIS检测。 CB [7]形成稳定的复合物，其具有所有测试的肟的1：1个化学计量。在高于肟的pK（a）的pH下观察到复杂稳定性的降低，这限制了络合对肟的适用性与低于生理pH的pk（a）。生理离子强度和pH的组合导致复杂稳定性的部分降低。证明了在生物样品中肟-CB [7]复合物的肟-CB [7]复合物的光谱分析前的样品预处理步骤的有机溶剂的影响。甲醇是一种更合适的溶剂，对复杂稳定性低。最后，对电喷雾电离的质谱能力进行了证明用于肟-CB [7]络合物的分析。

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  • 来源
    《New Journal of Chemistry》 |2020年第34期|共6页
  • 作者

    Andrys Rudolf; Klusonova Aneta; Lisa Miroslav; Karasova Jana Zdarova;

  • 作者单位

    Univ Hradec Kralove Fac Sci Dept Chem Rokitanskeho 62 Hradec Kralove 50003 Czech Republic;

    Univ Hradec Kralove Fac Sci Dept Chem Rokitanskeho 62 Hradec Kralove 50003 Czech Republic;

    Univ Hradec Kralove Fac Sci Dept Chem Rokitanskeho 62 Hradec Kralove 50003 Czech Republic;

    Univ Def Fac Mil Hlth Sci Hradec Kralove Dept Toxicol &

    Mil Pharm Tychonova 1 Prague Czech Republic;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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