中成药2018，Vol.40Issue(2)：284-290,7.DOI:10.3969/j.issn.1001-1528.2018.02.007
榄香烯注射液对吉非替尼在PC-9/GR细胞内转运动力学影响
Effects of Elemene Injection on the kinetics of intracellular transport of Gefitinib in PC-9/GR cells
摘要
Abstract
AIM To study the effects of Elemene Injection (ELE) on the kinetics of intracellular transport of Gefitinib (GEF) in PC-9/GR cells and to probe the role of ELE in reversing oncological multidrug resistance.METHODS The intracellular pharmacokinetic behavior of D-luciferin potassium salt,a substrate of an ATP-binding cassette (ABC) protein,was investigated in PC-9/GRFluc cells using real-time bioluminescence imaging.The resistance of PC-9/GR cells to GEF was determined by MTT assay.Compusyn software was used to analyze the synergistic effect of GEF and ELE,and HPLC to detect the uptake of GEF in PC-9/GR cells.RESULTS The respective GEF IC50 values of 0.01 μg/mL in PC-9 cells and 1.50 μg/mL in PC-9/GR cells revealed the 150 times drug resistance of PC-9/GR to PC-9 cells.The significantly enhanced intracellular fluorescence intensity of D-fluorescein potassium salt by the intervention of ELE also indicated remarkable GEF uptake increase in PC-9/GR cell line (P ＜ 0.05) due to the synergistic result.CONCLUSION Partly as the mechanism in reversing oncological multidrug resistance,ELE,a booster for the fluorescence intensity of D-luciferin potassium salt,promotes cellular uptake of GEF by inhibiting efflux function of ABC proteins.关键词
榄香烯/吉非替尼/胞内转运动力学/活体生物发光技术/肿瘤多药耐药Key words
Elemene (ELE)/Gefitinib (GEF)/the intracellular transport/bioluminescence imaging/oncological multidrug resistance分类
医药卫生引用本文复制引用
陈芝,俞建东,唐超园,祝丽欣,胡恩莹,熊阳..榄香烯注射液对吉非替尼在PC-9/GR细胞内转运动力学影响[J].中成药,2018,40(2):284-290,7.基金项目
国家自然科学基金面上项目(81473434,81673607,81774011) （81473434,81673607,81774011）
