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目的:探讨榄香烯乳(elemene,ELE)逆转人肺腺癌A549/DDP细胞株耐药性及其机制。方法:采用MTT法检测榄香烯乳单用的细胞毒作用及与顺铂(cisplatin,DDP)合用时耐药逆转作用;采用流式细胞术检测榄香烯乳对A549/DDP细胞内罗丹明-123(rhodamine-123,Rh123)蓄积的影响;采用Western blot检测榄香烯乳对耐药细胞A549/DDP细胞膜上P-gp蛋白表达的影响。结果:不同浓度榄香烯对A549/DDP细胞均有一定的抑制作用,呈时间-剂量依赖性效应。单用DDP的IC50为15.46μg/ml,合用20μg/ml榄香烯24h,IC50为4.15μg/ml,逆转耐药倍数为3.63。同时,榄香烯增加A549/DDP细胞内Rh123的蓄集,降低细胞膜上Pgp的表达,且呈剂量依赖性,表明榄香烯能减少A5 4 9/DDP细胞对药物的外排和抑制P-gp蛋白的表达。结论:榄香烯在体外逆转肿瘤细胞耐药性可能与其抑制P-gp的功能和表达有关。
Objective: To investigate the drug resistance and its mechanism of elemene (ELE) in reversing human lung adenocarcinoma A549 / DDP cell line. Methods: MTT assay was used to detect the cytotoxicity of elemene alone and the reversal of drug resistance in combination with cisplatin (DDP). Flow cytometry was used to detect the inhibitory effect of elemene on A549 / DDP intracellular rhodamine -123 (rhodamine-123, Rh123). Western blot was used to detect the effect of elemene on the expression of P-gp protein in the cell membrane of A549 / DDP cell line. Results: Different concentrations of elemene had certain inhibitory effect on A549 / DDP cells in a time-and dose-dependent manner. IC50 of single DDP was 15.46μg / ml, combined with 20μg / ml elemene 24h, IC50 was 4.15μg / ml, the reversal of resistance multiple was 3.63. At the same time, elemene increased the accumulation of Rh123 in A549 / DDP cells and decreased the expression of Pgp on the cell membrane in a dose-dependent manner, indicating that elemene can reduce drug efflux and inhibit P- gp protein expression. CONCLUSION: Elemene can reverse the drug resistance of tumor cells in vitro possibly by inhibiting the function and expression of P-gp.