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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
【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.
【Key words】 sodium nitro prusside; nitricoxide; thiols; pharmacokinetics;
- 【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