| 洛美利嗪对人白血病细胞K562/ADM多药耐药的逆转作用 |
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| 引用本文： | 吴玉林,祝浩杰,刘国卿.洛美利嗪对人白血病细胞K562/ADM多药耐药的逆转作用[J].中国临床药理学与治疗学,2003,8(4):393-395. |
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| 作者姓名： | 吴玉林 祝浩杰 刘国卿 |
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| 作者单位： | 1. 中国药科大学生理教研室,南京,210009,江苏
2. 中国药科大学药理教研室,南京,210009,江苏 |
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| 摘 要： | 目的：研究洛美利嗪(lomerizine，Lom)对人白血病细胞K562／ADM多药耐药逆转作用及机制。方法：使用MTT法检测Lom对K562／ADM多药耐药细胞柔红霉素(DNR)细胞毒性的影响，使用荧光分光光度计和流式细胞术分析Lom对K562／ADM多药耐药细胞胞内P—糖蛋白(P—glycoprotein，P—gp)底物—罗丹明123(rhodamine 123，Rh123)的累积情况。结果：Lom能明显提高DNR对K562／ADM多药耐药细胞的细胞毒作用，并可使胞内Rh123的浓度增加。K562敏感细胞株则不受影响。结论：Lom能显地抑制：K562／ADM多药耐药细胞上P—gp的活性，提高P—gp底物的胞内浓度，并增强其他抗癌药的细胞毒作用。
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| 关 键 词： | 药理学 洛美利嗪 P—糖蛋白 P—糖蛋白抑制剂 多药耐药性 |
| 文章编号： | 1009-2501(2003)04-0393-03 |
| 修稿时间： | 2003年3月20日 |
Reversal of lomerizine on multidrug resistance in human leukemia cell line K562/ADM |
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| WU Yu-Ling,ZHU Hao-Jie ,LIU Guo-Qing.Reversal of lomerizine on multidrug resistance in human leukemia cell line K562/ADM[J].Chinese Journal of Clinical Pharmacology and Therapeutics,2003,8(4):393-395. |
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| Authors: | WU Yu-Ling ZHU Hao-Jie LIU Guo-Qing |
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| Institution: | WU Yu-Ling,ZHU Hao-Jie 1,LIU Guo-Qing 1 Department of Physiology,China Pharmaceutical University,Nanjing 210009,Jiangsu,China, 1 Department of Pharmacology,China Pharmaceutical University,Nanjing 210009,Jiangsu,China |
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| Abstract: | AIM: To investigate the efficacy of lomerizine on multidrug resistance (MDR) reversal and its mechanism. METHODS: Cytotoxicity of daunomycin (DNR) on K562/ADM was assessed by MTT assay in the presence of lomerizine. Fluorescence of P-glycoprotein (P-gp) substrate rhodamine123 (Rh123) in K562/ADM was measured by fluorescence spectrophotometry and flow cytometry. RESULTS: Lomerizine could significantly increase the chemosensitivity of K562/ADM to DNR and intracellular content of Rh123. No effect was found in K562 cells. CONCLUSION: Lomerizine shows significant inhibition on the activity of P-gp in K562/ADM, increases intracellular accumulation of P-gp substrates, and enhances cytotoxicity of other anticancer drugs. |
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| Keywords: | pharmacology lomerizine P-glycoprotein P-glycoprotein inhibitor multidrug resistance |
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