血管紧张素转化酶中药抑制剂的筛选模型研究

Establishment of three screening models of angiotensin converting enzyme inhibitors

目的:研究比较不同的血管紧张素转化酶抑制剂(ACEI)筛选模型,提供从中草药中快速筛选ACEI药物的方法。方法:以卡托普利为阳性药,分别以大鼠血清、血管紧张素转化酶(ACE)纯酶、兔肺ACE粗提物作为酶源,采用不同的检测方法,建立3种ACEI筛选模型,考察多种中药有效成分ACEI活性。结果:大鼠血清粗提酶液模型检测卡托普利IC50值为2.30 nmol.L-1;ACE纯酶模型检测卡托普利IC50值为1.04 nmol.L-1;兔肺ACE粗提物模型检测卡托普利IC50值为1.40nmol.L-1,3种ACE筛选模型线性关系均良好,模型建立成功。结论:3种模型均可用于中草药的体外活性筛选,但各有利弊,可根据中草药组分和筛选模型的特点选择快速有效的模型。

Objective： To establish and compare three in vitro screening models of angiotensin converting enzyme inhibitors（ACEI）,and provide methodological basis for screening ACEI drugs from Chinese herbal medicine.Method： Three screening models were established using rat serum,pure angiotensin converting enzyme（ACE） and crude extract enzyme from rabbit lung as enzyme sources,respectively,with corresponding testing methods,and captopril as the positive drug.Result： The IC50 of captopril was 2.30 nmol·L-1 using rat serum as the enzyme;and 1.04 nmol·L-1 for ACE pure enzyme;and 1.40 nmol·L-1 for crude extract enzyme from rabbit lung.Conclusion： Results from the three screening models were all in accordance with literature reports.These models can be applied to in vitro pharmaceutical screening.The selection of suitable screening model depend on the experimental situation and the inherent characters of models.