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Acta Pharmacologica Sinica 2006 April; 27 (4): 414-418; doi: 10.1111/j.1745-7254.2006.00294.x |
| Original Article | [ Full text ] |
| CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells1 |
Bian-sheng JI2, Ling HE3, Xiao-qu LI4, Guo-qing LIU3,5 2Institute of Pharmacy, Henan University, Kaifeng 475001, China; 3Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China; 4School of Life Sciences, Beijing Normal University, Beijing 100875, China |
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Aim: To investigate the modulatory effect of CJZ3, a lomerizine derivative, on P-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC). Methods: RBMEC were isolated and cultured in Dulbecco’s modified Eagle’s medium/F12 (1:1) medium, and the amount of intracellular rhodamine 123 (Rh123) was determined using a fluorescence spectrophotometer to evaluate the modulatory effect of CJZ3 on P-gp function. Results: The accumulation of Rh123 was potentiated in a concentration-dependent manner after incubation with CJZ3 for RBMEC, but not for human umbilical vein endothelial cells (HUVEC). CJZ3 caused the accumulation of intracellular Rh123 in a time-dependent manner and significantly decreased the efflux of Rh123 from the cells. The inhibitory effect of CJZ3 on P-gp function was reversible and remained for 120 min after CJZ3 (2.5 µmol/L) was removed from the medium. Conclusion: CJZ3 has a potent in vitro effect on the inhibition of P-gp function. |
Keywords: CJZ3; P-glycoprotein; blood-brain barrier |
| 1 Project supported by the High Technology Research and Development Program of China (No 2002AA2Z343E) and the Natural Science Foundation of Jiangsu Province, China (No BK 2004110). |
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