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目的 用血管紧张素Ⅰ转化酶 (ACE)抑制药雷米普利 (Ram)建立一种新的大鼠在体ACE生物活性检测方法。方法 比较不同剂量 (0 0 5、0 1mg·kg- 1 ,iv)Ram在给药后1、2 4、48h对血管紧张素Ⅰ (AngⅠ )升压和缓激肽 (BK)降压效应的影响 ,以AngⅠ的升压百分率 (% )或BK的降压百分率 (% )间接反映ACE活性变化。结果 大鼠给予Ram后1、2 4h ,静脉注射AngⅠ和心肌匀浆上清液 (含AngⅠ )的升压作用均降低 (P <0 0 5) ,且呈剂量依赖性 ,但在 48h后Ram对AngⅠ和心肌匀浆上清液 (含AngⅠ )的升压作用无影响。比较给予Ram后 1hAngⅠ的升压作用和缓激肽(BK)的降压作用 ,发现BK的降压作用比AngⅠ升压作用更明显 (P <0 0 5)。结论 大鼠静脉注射Ram后 2 4h内心肌和血浆中ACE活性显著被抑制 ,48h后ACE活性基本恢复 ;AngⅠ升压、BK降压效应的变化可作为ACE生物活性的在体检测指标 ,后者更为敏感
Objective To establish a new method for detecting in vivo ACE biological activity of angiotensin Ⅰ converting enzyme (ACE) inhibitor Ramipril (Ram). Methods The effects of different doses of Ram (0 0, 5, 1 mg · kg-1, iv) on the antihypertensive effect of angiotensin Ⅰ (Ang Ⅰ) and bradykinin (BK) , Which indirectly reflects the change of ACE activity with the percentage of increase of Ang I (%) or the percentage of decrease of BK (%). RESULTS: In the first and second hour after Ram administration, Ang I and the supernatant of myocardial homogenate (including AngⅠ) were decreased (P <0 05) in a dose-dependent manner. However, after 48 h Ram Ang I and myocardial homogenate supernatant (including Ang Ⅰ) no effect on the role of the pressure. Compared with the hypotensive effect of Ang I at 1 h and the antihypertensive effect of bradykinin (BK), we found that the antihypertensive effect of BK is more obvious than that of Ang Ⅰ (P <0.05). CONCLUSIONS: ACE activity in myocardium and plasma was significantly inhibited at 24 h after intravenous injection of Ram, and ACE activity recovered at 48 h. The changes of ACE inhibitory effect of Ang I and BK could be used as in-vivo indexes of ACE activity. More sensitive