黄芩苷PC12细胞跨膜转运的实验研究  

Transport behavior of baicalin in PC12 cells

作　　者：赵爽[1] 雷帆[1] 李慧颖[1] 王玉刚[1] 柴玉爽[1] 杜力军[1] 

机构地区：[1]清华大学蛋白质科学教育部重点实验室,生命科学学院医学院药物药理学研究室,北京100084

出　　处：《中国药理学通报》2012年第6期839-842,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 30973896,30801523,81073092);“重大新药创制”国家科技重大专项资助项目(No 2012ZX09102201-008,2012ZX09103201-041)

摘　　要：目的研究黄芩苷神经元跨膜转运的特点,部分阐释黄芩苷发挥神经系统保护作用的物质性基础。方法以PC12细胞为研究对象,使用高效液相色谱(HPLC)、质谱(MS)法检测黄芩苷孵育细胞内的物质含量及相关代谢产物。结果 100 mg.L-1黄芩苷给药30 min后,胞内黄芩苷浓度达峰值,8 h后胞内已测不出黄芩苷;在50～400 mg.L-1的给药浓度下,胞内黄芩苷含量与给药剂量呈正相关;抑制剂Verapamil与Nimodipine对黄芩苷转运有明显影响;同时胞内检测出黄芩素、6-甲氧基-黄芩苷两种结构类似物。结论黄芩苷能够浓度依赖性的跨膜入胞,此过程受相关抑制剂影响,并产生代谢产物。Aim To investigate the transport behavior of baicalin in PC12 cells and to explain the material basement of nervous system protection activity of baicalin.Methods PC12 cells were used as for research,and HPLC and MS were applied to detect the transport behavior of baicalin.Results When cells were treated by baicalin of 0.1 mg·L-1,the concentration of baicalin in cells reached a peak when incubating for 30 min and there was no baicalin left after 8 h;when the dosage of baicalin from 0.05 mg·L-1 to 0.4 mg·L-1 was in administration,intracellular baicalin concentration and administration dosage showed linear positive correlation;verapamil and nimodipine had effect on transport;in addition,baicalein and 6-methoxy-baicalin could be detected in the cells.Conclusion Baicalin can transport into PC12 cells and can be affected by some inhibitors,producing compounds.

关 键 词：黄芩苷 跨膜转运 PC12细胞 黄芩素 6-甲氧基-黄芩苷 P-糖蛋白 

分 类 号：R284.1[医药卫生—中药学] R287[医药卫生—中医学]