摘要
目的 :研究洛美利嗪 (lomerizine ,Lom)对人白血病细胞K5 6 2 ADM多药耐药逆转作用及机制。方法 :使用MTT法检测Lom对K5 6 2 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K5 6 2 ADM多药耐药细胞胞内P 糖蛋白 (P glycoprotein ,P gp)底物 罗丹明 12 3(rhodamine12 3,Rh12 3)的累积情况。结果 :Lom能明显提高DNR对K5 6 2 ADM多药耐药细胞的细胞毒作用 ,并可使胞内Rh12 3的浓度增加。K5 6 2敏感细胞株则不受影响。结论 :Lom能显著地抑制K5 6 2 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。
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.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2003年第4期393-395,共3页
Chinese Journal of Clinical Pharmacology and Therapeutics
