摘要
比较轮环藤碱(Cyc)、海岛轮环藤碱(Insr)和海岛轮环藤酚碱(Insn)与维拉帕米(Ver)体外调节多药耐药性(MDR)的作用.方法:细胞毒试验采用MTT法,细胞内阿霉素(Dox)积累采用荧光分光光度法测定.结果:Cyc,Insr,Insn和Ver在MDR细胞系MCF7/Adr和KBv200能显著调节Dox和长春新碱的耐药性,且其作用呈剂量依赖性.Cyc,Insr,Insn和Ver均能增加MCF7/Adr细胞内Dox的积累.Cyc和Insr调节MDR作用明显优于Ver,而Insn的作用类似于Ver.结论:Cyc,Insr和Insn能通过增加MDR细胞内Dox的积累而调节MDR.
AIM: To compare cycleanine (Cyc), insularine (Insr), insulanoline (Insn) and verapamil (Ver) in modulation of multidrug resistance (MDR) in vitro . METHODS: The cytotoxic effect was determined by 3 [4,5 dimethylthiazol 2 yl], 5 diphenyl tetarzolium bromide (MTT) assay. The intracellular doxorubincin (Dox) accumulation was assayed by spectro fluorometer. RESULTS: Cyc, Insr, Insn, and Ver showed significant activities in modulating Dox and vincristine resistances in acquired resistant MCF 7/Adr and KB v200 cell lines in a dose dependent manner. Cyc, Insr, Insn, and Ver increased intracellular Dox accumulation in MCF 7/Adr cells. Cyc and Insr had greater activities than Ver in modulating MDR, while Insn had similar activity to that of Ver. CONCLUSION: MDR was modulated by Cyc, Insr, and Insn, due to the increase of intracellular Dox accumulation.
出处
《中国药理学报》
CSCD
1997年第5期455-458,共4页
Acta Pharmacologica Sinica
关键词
轮环藤碱
异喹啉
多种耐药性
cycleanine
insularine
insulanoline
isoquinolines
doxorubicin
vincristine
cultured tumor cells
multiple drug resistance