Effects of Elemene Injection on the kinetics of intracellular transport of Gefitinib in PC-9/GR cells
10.3969/j.issn.1001-1528.2018.02.007
- VernacularTitle: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
- Author:
Zhi CHEN
1
;
Jian-Dong YU
;
Chao-Yuan TANG
;
Li-Xin ZHU
;
En-Ying HU
;
Yang XIONG
Author Information
1. 浙江中医药大学药学院,浙江杭州310053
- Keywords:
Elemene (ELE);
Gefitinib (GEF);
the intracellular transport;
bioluminescence imaging;
oncological multidrug resistance
- From:
Chinese Traditional Patent Medicine
2018;40(2):284-290
- CountryChina
- Language:Chinese
-
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.
