Nifedipine induced reversal of multidrug resistance can be deteriorated by S9 mix prepared from the transgenic cell line CHL-3A4
- VernacularTitle:转基因细胞系CHL-3A4可使硝苯吡啶的多药耐药逆转作用丧失
- Author:
Yuli QIAN
;
Gejian ZHU
;
Yingnian YU
- Publication Type:Journal Article
- Keywords:
Cytochrome P - 450;
Nifedipine;
Doxorubicin
- From:
Chinese Journal of Pathophysiology
1989;0(05):-
- CountryChina
- Language:Chinese
-
Abstract:
AIM:To demonstate the expression of human cytochrome P450 3A4 isozyme in the transgenic cell line CHL - 3A4 established in this laboratory. METHODS:Nifedipine (NIF) can induce the reversal of the brug resistance for adriamycin of multidrug resistant(MDR) cell K562r. The NIF is the specific substlate for CYP3A4. To determine the NIF oxidase activity of the transgenic CHL - 3A4 cells by comparing the biological effect of NIF, which preinculbated with or without CHL - 3A4 S9 mix. RESULTS: When the multidrug resistance cell K562r was cultured in medium with NIF (12. 5 ?g? L- 1 ), a calcium channel blocker and specific substrate for CYP3A, it's IC50 for adri- amycin declined from(6.47?0.60) mg ? L- 1 to (0. 89?0. 15) mg? L-1. When cells were cultured in NIF(exactly the same concentration ) pretreated with CHL - 3A4 S9 mix,no reversal of MDR was observed [IC50 for adriamycin is (6.10?0.50) mg? L-1 ] while if NIF was pretreated with CHL S9 or inactivated CHL - 3A4 S9 mix, its biological effect was not deteriorated [IC50 for adriamycin is (0. 32?0.90) and (0.32?0.04) mg?L-1, P
