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EPR indication of oxidative stress by pharmaceutical agents.

机译：EPR指示药剂产生的氧化应激。

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摘要

Salbutamol (albuterol, (±)alpha-1-[(tert-butylamino)methyl]-4-hydroxy-m-xylene-alpha, alpha′-diol, C13H21NO3) and beclomethasone dipropionate are commonly prescribed pharmaceuticals for asthma. Salbutamol is a modern drug with three structural components engineered for delivery and activity. It is supplied in multiple dosage forms, most commonly in tablet or inhalar form. In the latter form, the drug is directly delivered to the respiratory tract. EPR spin-trapping studies have shown that mild heating and low levels of light exposure lead to the production of multiple reactive oxygen species. Radical production observed during salbutamol exposure to oxidative stressed conditions was found to involve interesting coordination chemistry that takes place between salbutamol and iron metal. The radical species are implicated in a variety of oxidative disorders and may account for the deleterious effects associated with salbutamol usage. The reactive oxygen radicals produced are sufficient to mutate DNA and inhibit the activity of Fhit, enzymatic product of the FHIT tumor suppressor gene.; Beclomethasone dipropionate, (9-chloro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21-dipropionate, C28H37ClO7) given generally for long-term asthma or rhinitis treatment, is structurally designed according to the steroid motif. A unique X-ray crystal structure of beclomethasone dipropionate was obtained which lacked the 11(O) to 21 water bridge observed in previously obtained crystal structures. Alterations in this structure could affect drug lipophilicity and overall activity. Light exposure and heating studies showed beclomethasone to be fairly stable, with minimal photo degradation proceeding via ester hydrolysis. Exposure to an in vitro oxidatively stressed environment revealed beclomethasone's antioxidant behavior. This work provided a chemical basis of why salbutamol and beclomethasone dipropionate function they way they do, why they contrast in their clinical activities, and how their redox behaviors relate to the progression, stabilization, and/or reduction of an oxidatively stressed state.
机译：沙丁胺醇（沙丁胺醇，（±）α-1-[[（叔丁基氨基）甲基] -4-羟基-间二甲苯-α，α'-二醇，C 13 H 21 NO 3 ）和倍氯米松二丙酸酯是哮喘的常用处方药。沙丁胺醇是一种现代药物，具有为传递和活性而设计的三个结构成分。它以多种剂型提供，最常见的是片剂或吸入形式。在后一种形式中，药物被直接递送到呼吸道。 EPR自旋捕集研究表明，温和的加热和低水平的曝光会导致产生多种活性氧。发现沙丁胺醇暴露于氧化应激条件下观察到的自由基产生涉及在沙丁胺醇和金属铁之间发生的有趣的配位化学。自由基物质与多种氧化紊乱有关，可能解释与沙丁胺醇使用相关的有害作用。产生的反应性氧自由基足以突变DNA并抑制FHIT抑癌基因酶促产物Fhit的活性。倍氯米松二丙酸酯，（9-氯-11β，17,21-三羟基-16β-甲基孕烯-1,4-二烯-3,20-二酮17,21-二丙酸酯，C 28 H 37 ClO 7 ）通常用于长期哮喘或鼻炎，是根据类固醇的母体结构设计的。获得了倍氯米松二丙酸酯的独特的X射线晶体结构，其缺乏在先前获得的晶体结构中观察到的11（O）至21的水桥。这种结构的改变可能会影响药物的亲脂性和整体活性。曝光和加热研究表明倍氯米松是相当稳定的，通过酯水解进行的光降解最小。暴露于体外氧化应激环境中，显示倍氯米松的抗氧化行为。这项工作提供了化学基础，说明了沙丁胺醇和倍氯米松双丙酸酯为何发挥功能，为什么它们在临床活动中形成对比，它们的氧化还原行为如何与氧化应激状态的进展，稳定和/或降低相关。

著录项

  • 作者

    Sykes, Kenneth Tremain.;

  • 作者单位

    Temple University.;

  • 授予单位 Temple University.;
  • 学科 Chemistry Analytical.; Chemistry Pharmaceutical.; Chemistry Radiation.
  • 学位 Ph.D.
  • 年度 2001
  • 页码 315 p.
  • 总页数 315
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;药物化学;化学;
  • 关键词

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