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一氧化氮活性巯基化合物研究供体药物体外释放通路

The release of NO donor in vitro by sulflydryl compounds

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【作者】 李杨郑英

【Author】 LI Yang1,ZHENG Ying2(Department of Internal Medicine,The People’s Hospital of Jianggan,Zhejiang Hangzhou 310004,China;2.Department of Pharmacy,117th Hospital of PLA,Zhejiang Hangzhou 310013,China)

【机构】 杭州市江干人民医院内科中国人民解放军第117医院药剂科

【摘要】 目的:探索生理溶液中一氧化氮(NO)供体硝普钠(SNP)在含活性巯基化合物中释放NO的动力学特征,为在生理溶液中NO的释放通路及其规律特点提供科学依据。方法:在37℃恒温避光条件下,对NO特异氧化产物NO2-以Griess试剂还原显色,采用分光光度法,比较分别有巯基乙醇、二巯基丁二醇(DTT)、二巯基丙醇(BAL)、半胱氨酸(CYS)、谷胱甘肽(GSH)、青霉胺(PCA)、N-乙酰半胱氨酸(NAC)等7种巯基化合物存在的Krebs-Henseleit生理溶液中,SNP释放NO的情况(n=3)。结果:在含1,5,10,25mmol.L-1的7种巯基还原剂的Krebs-Henseleit生理溶液恒温测试系统中,其催化SNP释放NO的动力学特征分别符合一级、零级和多级动力学。结论:恒温避光Krebs-Henseleit生理溶液中,SNP通过巯基通路释放NO的动力学特征受到巯基化合物自身的化学结构及空间位置的影响,6h内SNP在含各巯基试剂的测试系统中释放NO量依次为CYS>BAL>GSH>DTT>巯基乙醇>PCA>NAC。

【Abstract】 OBJECTIVE To investigate the kinetic characteristics of nitric oxide(NO) released from sodium nitroprusside(SNP) in tyrode solution.METHODS Griess assay was used to measure NO releasing from SNP seven thio-containing compounds(mercapto ethanol,DTT,BAL,CYS,GSH,PCA and NAC) in Krebs-Henseleit solution were compared while protected from light at 37 ℃ by spectrophotometry.RESULTS For seven thio-containing compounds at 1,5,10,25 mmol·L-1 in Krebs-Henseleit solutions,NO was released in a first order rate、a zero order rate or multiple phase reactions respectively.CONCLUSION Under 37 ℃ and protected from light,the kinetics of NO released from SNP was significantly influenced by the construction and spatial structure of thiol-containing compound.The generation of NO from different thiol-containing compounds at 25 mmol·L-1 was successively.CYS>BAL >GSH>DTT> mercapto ethanol >PCA>NAC.

  • 【文献出处】 中国医院药学杂志 ,Chinese Journal of Hospital Pharmacy , 编辑部邮箱 ,2009年05期
  • 【分类号】R94
  • 【下载频次】164
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