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有机化学 ›› 2009, Vol. 29 ›› Issue (06): 936-941. 上一篇    下一篇

研究论文

四(4-磺酸基苯基)卟啉锰钠盐-NO配合物的合成及NO释放效能和 生物学活性研究

肖丽波a ; 鲁燕妮b ; 刘凌鹏a; 吴鹏飞a; 冯 清*,a   

  1. (a华中科技大学化学与化工系 生物无机化学与药物湖北省重点实验室 武汉 430030)
    (b海南省疾病预防控制中心 物理化学检验所 海口 570203)
  • 收稿日期:2007-12-31 修回日期:2008-07-28 发布日期:2009-06-20
  • 通讯作者: 冯 清

Synthesis, NO Release Efficiency and Its Bioactivities of Nitrosyl meso-Tetrakis-[4-(sodium sulfonato)phenyl]porphyrin Manganese Complex

Xiao, Liboa ; Lu, Yannib ; Liu, Lingpenga; Wu, Pengfeia; Feng, Qing*,a   

  1. (a Hubei Key Laboratory of Bioinorganic Chemistry & Materia Medica, Department of Chemistry, Huazhong University of Science and Technology, Wuhan 430030)
    (b Hainan Center for Disease Control and Prevention, Institute of Physics and Chemistry, Haikou 570203)
  • Received:2007-12-31 Revised:2008-07-28 Published:2009-06-20
  • Contact: Feng, Qing

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合成、表征了一种新型的NO供体化合物meso-5,10,15,20-四(4-磺酸基苯基)卟啉锰钠盐—NO配合物(TPPSNa-Mn-NO), 并初步研究其药理学作用. 采用重氮化偶合反应检测TPPSNa-Mn-NO体外NO的释放效果. 观察TPPSNa-Mn-NO对家兔离体胸主动脉环的舒张作用和对于大鼠收缩压、舒张压及心率的影响. TPPSNa-Mn-NO的体外NO释放效率约为70.86%, 该化合物可以使30 mmol•L－1甲氧胺引起家兔离体胸主动脉收缩的量效关系曲线非平行右移, 最大反应(Emax)压降低约30.2%, 静脉给药后实验组大鼠血压第5 min时开始下降, 并持续缓慢降低, 给药后30 min下降幅度达最大, 而后缓慢回升, 给药后120 min时接近用药前水平且仍低于用药前水平. 药物对大鼠心率无显著影响. TPPSNa-Mn-NO具有缓慢持久降压的药理作用, 且不影响其他重要的生命指标, 有望成为长效降压药理想的候选化合物.

关键词: 一氧化氮供体, 离体血管环, 降压, TPPSNa-Mn-NO

A nitrosyl meso-tetrakis[4-(sodium sulfonato)phenyl]porphyrin manganese complex (TPPSNa- Mn-NO) was synthesized as a NO donor and its pharmacological effects were investigated. The NO-relea- sing property of TPPSNa-Mn-NO in aqueous was studied by diazotization at room temperature. The relaxation of TPPSNa-Mn-NO was investigated on isolated rabbit aorta pectoralis circle. The systolic blood pressure, diastolic blood pressure and heart rates of rats were investigated before and after drug administration. The NO-releasing ratio of TPPSNa-Mn-NO was 70.86%. TPPSNa-Mn-NO shifted methoxamine cumulative dose-response curves rightward im-paralleling a group reduced the Max, and the reduced percentage was 30.2%. For the blood pressure of rats began to decrease at the time of 5 min after the administration, the blood pressure of rats reached the minimum at the time of 30 min, then increased slowly, and finally, ap-proached the normal blood pressure at 120 min, but was still lower than that before the administration. For the control group, the blood pressure of the rats was not changed after employing the normal salined. For the treatment TPPSNa-Mn-NO could decrease the blood pressure slowly and lastingly, but had no effect on heart rates, anapnea and electrocardiography. Perhaps it would be used as an ideal prolonged hypotensive drug.

Key words: NO donor, isolated vascular circle, depressurizati, TAPPSNa-Mn-NO