Xia Chun-Fang, Ye Zu-Guang, Zhou Xiang-Ning, Tang Tian-Tian, Wen Ling-Jun, Liu Xin-Yi
Department of Oncology, The Second Xiangya Hospital of Central South University, Changsha, China.
Yao Xue Xue Bao. 2014 Oct;49(10):1413-7.
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 x 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 x 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. AUC(heart) 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.
本研究旨在探讨聚乙二醇化葛根素在急性心肌缺血模型大鼠体内的组织分布。将健康雄性SD大鼠随机分为两组（每组30只）。两组均给予488 mg·kg⁻¹剂量的聚乙二醇化葛根素。给药5分钟后，一组为正常大鼠，另一组通过腹腔注射50 mg·kg⁻¹异丙肾上腺素建立急性心肌缺血模型。给药后，分别于30、60、90、120、150和180分钟处死动物，然后取出心脏、肝脏、脾脏、肺脏、肾脏。采用高效液相色谱法测定各器官组织中葛根素的含量。结果表明，聚乙二醇化葛根素在正常大鼠体内的组织分布AUC为肝脏＞肾脏＞心脏≈脾脏＞肺脏＞脑。而聚乙二醇化葛根素在急性心肌缺血模型大鼠体内的组织分布AUC为肝脏≈心脏＞肾脏＞肺脏≈脾脏＞脑。聚乙二醇化葛根素在急性心肌缺血模型大鼠体内的AUC(心脏)是正常大鼠的1.7倍，差异有统计学意义（P＜0.05）。因此，聚乙二醇化葛根素在早期心肌梗死区域具有良好的心脏靶向性，药物可在缺血心肌中蓄积。这为聚乙二醇化葛根素的进一步研究和临床应用提供了重要信息。
