葛根素衍生物抗心肌缺血再灌注损伤的活性筛选

Optimization of Activities of Puerarin Derivatives Against Myocardial Ischemia/Reperfusion Injury

目的:对5个葛根素衍生物(PDs)进行抗心肌缺血再灌注损伤的活性筛选。方法:建立离体大鼠心肌缺血再灌注损伤模型,以缺血30min再灌注60min过程中冠脉流量(CF)和心率(HR)的变化及再灌注结束后左心室梗死范围(IS)为指标,对5个葛根素衍生物进行活性筛选。结果:与模型组比较,5个葛根素衍生物均能显著降低IS;葛根素衍生物13号(G13)、14号(G14)、20号(G20)和25号(G25)能显著增加CF;G20和G25能减慢并稳定HR;G20降低IS和增加CF的作用强于葛根素(Pue),故筛选出G20进行进一步研究。结论:所试5个PDs均有显著降低缺血再灌注致心肌损伤的作用,并可缩小左心室梗死范围,其中以G20作用为最好。

OBJECTIVE： To optimize the pharmacological activities of 5 puerarin derivatives（PDs） against myocardial ischemia/reperfusion injury. METHODS： An ex vivo myocardial ischemia/reperfusion injury model was established on rats, and the pharmacological activities of 5 PDs was optimized with coronary flow（CF） and heart rate（HR） during the ischemia （30 min） /reperfusion （60 min） and the infarct size of left ventricle（IS） after the termination of reperfusion as indexes. RESULTS： As compared with model group, all the 5 PDs could significantly reduce the IS; G13, G14, G20 and G25 could increase CF; G20 and G25 could slow down and stabilize HR. The activities of G20 in reducing IS and increasing CF were more potent than those of puerarin, thus G20 was selected for further study. CONCLUSION： All the 5 PDs showed remarkable protective effects on myocardial damage and IS caused by myocardial ischemia/ reperfusion injury and minimize the infarct size of left ventricle （IS）, among the 5 PDs, G20 is the best in efficacy.