ABSTRACT
AIM: To study the effect of Lomerizine on the activity of P-glycorprotein (P-gp) in primary cultured rat brain microvessel endothelial cells (RBMECs). METHODS: Flow cytometry was used to study the efflux of rhodamine123 (Rh123) and expression of P-gp in RBMECs. RT-PCR was used to measure the expression in mRNA level of mdr1 gene in RBMECs. Transwell model was used to detect the influence of Lomerizine on the transport of Rh123 through RBMECs monolayer. RESULTS: Lomerizine inhibited the efflux of Rh123 in RBMECs. No changes of P-gp and mdr1 gene mRNA expression were detected in RBMECs after the treatment with 30 μmol·L-1 Lomerizine for 72 h. In the study of Transwell model, Lomerizine increased significantly the transport of Rh123 through RBMECs monolayer from upper compartments to lower compartments, and inhibited obviously the transport in reverse direction. CONCLUTION: The effect of Lomerizine on the activity of P-gp was mainly via its direct inhibitory effect on the function of P-gp in RBMECs and the transport of P-gp substrates in BBB may be affected by lomerizine.
ABSTRACT
Aim To study the reversal effect of CPUC1 on multidrug resistance in K562/A02 cells. Methods MTT assay was used to detect the cytotoxicity of vincristine. Intracellular accumulation of rhodamine123 was measured by flow cytometry to evaluate the function of P glycoprotein(Pgp). The apoptotic cells induced by vincristine were detected by flow cytometry using DNA content analysis and Annexin V/PI double staining. Results CPUC1 significantly reversed the resistance of K562/A02 cells to vincristine. CPUC1 increased intracellular accumulation of rhodamine123 in K562/A02 cells in a concentration dependent manner. CPUC1 increased the apoptosis induced by vincristine. Conclusion CPUC1 reversed multidrug resistance by inhibiting function of P gp in K562/A02 cells, suggesting that CPUC1 merits further study.
ABSTRACT
AIM: To study the effect of CPUE1 on the reversal of multidrug resistance (MDR) in K562/A02 cells and its mechanism. METHODS: MTT assay was used to determine the influence of CPUE1 on the cytotoxicity of vincrisine (VCR) in K562/A02 cells. The effect of CPUE1 on the apoptosis induced by VCR in K562/A02 cells was detected using DNA analysis and Annexin-Ⅴ/PI double stain assay. Flow cytometry was used to investigate the efflux of rhodamine123 (Rh123) by P-glycoprotein (P-gp) in K562/A02 cells. RESULTS: CPUE1 increased the cytotoxicity and apoptosis induced by VCR in K562/A02 cells. At the concentration of 10 ?mol?L -1 ,CPUE1 reduced the IC_ 50 value of VCR from 60.54 to 4.17 ?mol?L -1 . CPUE1 inhibited the efflux of Rh123 and resulted in the increase of intracellular accumulation of Rh123 in K562/A02 cells. CONCLUSION: CPUE1 has strong reversal effect on MDR in K562/A02 cells by inhibiting P-gp activity.
ABSTRACT
Objective To observe the effect of Naomaitai Capsule on the learning and memory abilities and cerebral lipid-peroxidation in rat with vascular dementia(VD).Methods Two VD models were(established).The first one was produced by occlusion of bilateral common carotid arteries in rats with the(following) steps: ischemia 20 min—reperfusion 10 min—ischemia 20 min.The learning and memory abilities were tested by Y type maze.Meanwhile,malondiadehyde(MDA) content and superoxide dismutase(SOD) activity in brain tissue of ischemia-reperfusion rats were measured.The second model was formed by injecting thrombin NS solution into internal carotid artery.The learning and memory abilities were studied by Y type Maze.The content of Evans blue in brain tissue was measured.Results In the model caused by cerebral ischemia-reperfusion,Naomaitai Capsule significantly improved the learning and memory abilities((P