09-08-2009, 07:38 PM
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Senior Member
Join Date: Feb 2008
Location: South East Wisconsin
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Reversal effect and mechanism of lobeline on the multidrug-resistance of human breast
- 1: Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2009 Aug;34(8):738-43.
- [Reversal effect and mechanism of lobeline on the multidrug-resistance of human breast cancer cells MCF-7/ADM.]
[Article in Chinese]
Chen J, Shen L, Zhou R, Yao W, Zhong M, Zhu ZH, Zeng S.
Department of Oncology, Xiangya Hospital, Central South University, Changsha 410008, China.
Objective To explore the reversal effect and mechanism of lobeline on the multidrug-resistance (MDR) of human breast cancer cells MCF-7/ADM. Methods In human breast cancer cell line MCF-7/ADM, MTT assay was used to determine the cell growth inhibiting ratio of MCF-7/ADM by ADM and Fu.Fluorospectorphotometer was employed to investigate the intracellular concentration of rhodamine123 to reflect the effect of lobeline on the activity of MDR-related protein P-glycoprotein (P-gp).Taking untreated MCF-7/ADM cells as controls,flow cytometry was applied to detect the intracellular concentration of rhodamine123 in MCF-7/ADM cell intervened with lobeline of 20 mumol/L.Results The sensitivity of MCF-7/ADM to ADM and Fu was significantly increased by lobeline in a dose-dependent manner. The inhibitive concentration 50 (IC(50)) of ADM declined from (44.81+/-0.43) mg/L to (16.72+/-0.75) mg/L with a reversion index of 2.68. The IC(50) of Fu declined from (53.12+/-1.60) mg/L to (38.90+/-1.43) mg/L with a reversion index of 1.37. The fluorescence intensity of lobeline-treated cells was significantly higher than that of the controls, when the concentration of lobeline was more than 10 mumol/L. With fewer side effects, the reversal efficacy of 20 mumol/L lobeline was 71.6% of the classical MDR reversal agent of verapamil at the same concentration. Conclusion Lobeline can reverse the MDR of MCF-7/ADM cells by inhibiting the activity of P-glycoprotein.
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