药学学报, 2014, 49(10): 1413-1417
引用本文:
夏春芳, 叶祖光, 周湘宁, 唐甜甜, 文令军, 刘新义. PEG化葛根素在急性心肌缺血模型大鼠上的组织分布[J]. 药学学报, 2014, 49(10): 1413-1417.
XIA Chun-fang, YE Zu-guang, ZHOU Xiang-ning, TANG Tian-tian, WEN Ling-jun, LIU Xin-yi. Tissue distribution of PEGylated puerarin in acute myocardial ischemia mode rats[J]. Acta Pharmaceutica Sinica, 2014, 49(10): 1413-1417.

PEG化葛根素在急性心肌缺血模型大鼠上的组织分布
夏春芳1, 叶祖光4, 周湘宁1, 唐甜甜2, 文令军3, 刘新义2
1. 中南大学湘雅二医院肿瘤科, 湖南 长沙 410011;
2. 中南大学湘雅二医院临床药学研究所, 湖南 长沙 410011;
3. 中南大学湘雅二医院检验科, 湖南 长沙 410011;
4. 中国中医科学院, 北京 100700
摘要:
为了探索PEG化葛根素在急性心肌缺血模型大鼠上的组织分布特点,采用健康雄性SD大鼠60只,随机分成两组,每组30只,均静脉注射给予PEG化葛根素,剂量为488 mg·kg-1,给药5 min后,一组设为正常大鼠,另一组大鼠腹腔注射给予异丙肾上腺素(剂量为50 mg·kg-1),造成急性心肌缺血模型。分别于给药后30、60、90、120、150和180 min处死部分动物,取心、肝、脾、肺、肾、脑组织脏器,利用HPLC测定各组大鼠组织脏器中葛根素的浓度。结果显示,PEG化葛根素在正常大鼠脏器中AUC大小顺序为肝 > 肾 > 心 ≈ 脾 > 肺 > 脑,而在急性心肌缺血模型大鼠中AUC大小顺序为肝 ≈ 心 > 肾 > 肺 ≈ 脾 > 脑,其中,在模型大鼠心脏中AUC为正常大鼠心脏中的1.7倍,且存在显著性差异(P<0.05)。结果表明,PEG化葛根素在心肌梗死早期区域具有较好的心脏靶向性,可以将药物蓄积于缺血心肌,为该药的进一步研究开发和临床应用提供重要的参考依据。
关键词:    PEG化葛根素      组织分布      急性心肌缺血      心脏靶向     
Tissue distribution of PEGylated puerarin in acute myocardial ischemia mode rats
XIA Chun-fang1, YE Zu-guang4, ZHOU Xiang-ning1, TANG Tian-tian2, WEN Ling-jun3, LIU Xin-yi2
1. Department of Oncology, The Second Xiangya Hospital of Central South University, Changsha 410011, China;
2. Institute of Clinical Pharmacy, The Second Xiangya Hospital of Central South University, Changsha 410011, China;
3. Clinical Laboratory, The Second Xiangya Hospital of Central South University, Changsha 410011, China;
4. China Academy of Traditional Chinese Medicine, Beijing 100700, China
Abstract:
The aim of this study is to explore the tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats. Healthy male SD rats were randomly divided into two groups (30 each). Both were given PEGylated puerarin at a dose of 488 mg·kg-1. After 5 min of medication, one group was normal rats, another group with acute myocardial ischemia was established by peritoneal injection of 50 mg·kg-1 isoprenaline. After administration, the animals were executed at 30, 60, 90, 120, 150 and 180 min, then heart, liver, spleen, lung, kidney were extracted. The content of puerarin in organ tissue was determined by HPLC. The results showed that the AUC of tissue distribution of PEGylated puerarin in normal rats was liver > kidney > heart ≈ spleen > lung > brain. While the AUC of tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats was liver ≈ heart > kidney > lung ≈ spleen > brain. AUCheart of PEGylated puerarin in acute myocardial ischemia model rats was 1.7 times than that of the normal rats, and there was significant difference (P<0.05). Thus, PEGylated puerarin had a good heart-targeting property in early myocardial infarction area, drugs could accumulate in the ischemic myocardium. It provided important information for further study and clinic use of PEGylated puerarin.
Key words:    PEGylated puerarin    tissue distribution    acute myocardial ischemia    heart-targeting   
收稿日期: 2014-05-06
基金项目: 湖南省自然科学基金资助项目(14JJ3038)
通讯作者: 文令军,Tel:86-731-85292093,E-mail:13723878082@139.com;刘新义,Fax:86-731-82235227,E-mail:liuxinyi128@126.com
Email: 13723878082@139.com;liuxinyi128@126.com
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