用正交设计观察了6种中草药有效成分和三氟啦嗪(TFP)对钙调素依赖环核苷酸磷酸二酯酶(CaM-PDE)激活活性的影响,结果表明：a)两面针碱(Nit)、槲皮素(Que)和TFP对CaM－PDE激活活性具有明显抑制作用(P＜0.01),其抑制强度：Qne＞TFP＞Nit小檗碱(Ber)、麻黄碱(Eph)和鱼腥草素(Hou)对CaM－PDE无明显作用(P＞0.05),青藤碱(Sin)对酶的作用可疑c)Qne与TFP、Nit与TFP之间有协同作用.结果提示Nit和Que可能是CaM拮抗剂,两者的作用位点似乎不同于TFP.

Effects of nitidine(Nit),berberine(Ber),sinomenine(Sin),ephedrine(Eph),ho-uttuynin(Hou),quercetin(Que)and trifluoprazine(TFP)on calmodulin一dependent c-Yclic nucleotide phosphodiesterase(CaM一PDE)were investigated by orthdgonal design.Our observation came out that, Nit,Que and TFP significantly inhibited the CaM-activa-ted PDE activity(P<0.01)in .th: order of Que>TFP>Nit.Ber, Eph,and Hou had no e-ffects on the enzyme activity(P>0.05).T ie effect of Sin on CaM一PDE was uncertain,It was also shown that there were coopetativity between Nit and TFP and synergism between Que and TFP.These results suggested that Nit and Que may act as calmodulin an- tagonists and might have different sites on calmodulin in comparison with those for TFP.

美国中华医学会(CMB)基金