中药提取物及活性部位抑制血管紧张素转化酶活性的研究
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摘要：目的筛选抑制血管紧张素转化酶(angiotensin converting enzyme, ACE)活性的中药及活性部位。方法采用体外模型比较8味中药提取物对ACE的抑制作用，并提取纯化抑制ACE作用最大的中药提取物的活性部位。结果8味中药提取物均能抑制ACE活性。金银花提取物70 %甲醇洗脱部位对ACE抑制率为87.3 %，主要成分为绿原酸，重结晶纯度80.4 %。结论金银花提取物对ACE具有较强的抑制效果，活性部位主要成分为绿原酸。
关键词：高效液相色谱法；血管紧张素转化酶；中药提取物；活性部位；绿原酸
中图分类号：R285.5文献标识码：A文章编号：1672-979X(2009)-01-0020-04
Research on Inhibition of Traditional Chinese Medicine Extracts and Active Fraction on Angiotensin Converting Enzyme
CAO Xiao-Gang1, YU Gang1, YE Xiao-Li2, WANG Li-Jun1, LI Xue-Gang1*
(1. College of Pharmacy, Southwest University, Chongqing 400716, China; 2. College of Life Science, Southwest University, Chongqing 400715, China)
Abstract：Objective To screen the traditional Chinese medicine extracts and active fraction with inhibition on angiotensin converting enzyme (ACE). Methods An in vitro model was employed to compare the inhibiting activities of eight species of traditional Chinese medicine extracts on ACE, and the active fraction of the extract with the maximum inhibition was extracted and purified. Results The eight species of traditional Chinese medicine extracts all could inhibit the ACE activity. The inhibition ratio of the fraction from Lonicera japonica eluted with 70 % methanol was 87.3 %, and the main ingredient was chlorogenic acid with the purity of 80.4 % after recrystallization.Conclusion The extract from Lonicera japonica has a stronger inhibition on ACE and the main ingredient of active fraction is chlorogenic acid.
Key words：HPLC; angiotensin converting enzyme; traditional Chinese medicine extract; active fraction; chlorogenic acid
血管紧张素转化酶(angiotensin converting enzyme，ACE)是哺乳动物体内调节血压的关键酶之一，主要催化血管紧张素Ⅰ转化为具有较强升压作用的血管紧张素Ⅱ。卡托普利(captopril)，西拉普利(cilazapril)，依那普利(enalapril)，赖诺普利(lisinopri)等药物的临床应用表明，抑制ACE活性能有效的降低血压，但长期使用，耐受性差，常见不良反应，限制了临床使用[1,2]。中药来源于天然动植物，资源丰富[3]，筛选能有效抑制ACE活性的中药具有重要的现实意义。本实验采用体外模型[4]，以马尿酰-组氨酰-亮氨酸(Hip-His-Leu，HHL)为ACE反应底物，产物马尿酸为测定指标，卡托普利为阳性对照，研究中药提取物及活性部位抑制ACE的效果，旨在为开发降血压中药提供科学依据 ......
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