聚乙二醇化葛根素的药效学实验研究  

Study on Pharmacology of Pegylated Puerarin

作　　者：余美荣 蒋福升[2] 钱朝东[2] 丁滨[2] 高承贤[2] 陈铌铍[2] 丁志山[2] 

机构地区：[1]新昌县中医院,浙江新昌312500 [2]浙江中医药大学生命科学学院,浙江杭州310053

出　　处：《中华中医药学刊》2014年第3期567-569,共3页Chinese Archives of Traditional Chinese Medicine

基　　金：浙江省自然科学基金项目(Y206776)

摘　　要：目的:对聚乙二醇(PEG)化葛根素前药(mPEG5000-Pur)体内药效学进行初步评价,为开发新型无溶血不良反应的葛根素制剂奠定基础。方法:采用垂体后叶素诱导大鼠急性心肌缺血模型,观察mPEG5000-Pur对心肌的保护作用;采用氯仿诱导小鼠心律失常模型,观察mPEG5000-Pur抗心律失常的作用。结果:葛根素PEG化后增强了对大鼠缺血心肌的保护作用;并且PEG化也可增强葛根素的抗小鼠心律失常作用,但是药效不呈剂量依赖性。结论:葛根素经PEG化后仍然保持了抗心肌缺血和抗心律失常的作用,且药效均优于相应剂量葛根素注射液组,这可能与PEG化后对葛根素体内组织分布改善有关。Objective：The pharmeodynamics of mPEG5000-Pur was evaluated,which would pave the way for exploring a novel no -hemolytic Pur agent. Methods：The acute myocardial ischemia model was induced by intravenously injecting poste- rior pituitrin hormone to observe cardiovascular pharmacology of mPEG5000- Pur. Anti - arrhythmias effect of the prodrug mPEG5000-Pur was evaluated by the model of arrhythmias induced by CHCI3. Results ：Pur and mPEG5000-Put had protec- ted ischemie heart against myocardial damage. In addition, both Put and mPEG5000- Put showed significant protecting effect against ventricular arrhythmia in mice, which was not in a dose -dependent manner. However, comparing with Pur, mPEG^o0 - Pur was more effective against arrhythmia. Conclusion： Pegylated puerarin had stronger effects of anti - myocardi- al isehemia and anti - arrhythmia compared with Pur. This may be resulting from the changes of tissue distribution of Put by pegylation. Our work verified that mPEGs000 - Put would be a promising agent for cardiovascular disease treatment.

关 键 词：聚乙二醇化 葛根素 心肌缺血 心律失常 

分 类 号：R285.5[医药卫生—中药学]