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研究赛赓啶对ＫＢＶ２００细胞多药抗性的逆转作用及逆转机制。在ＫＢＶ２００细胞，采用ＭＴＴ法，测出赛赓啶对长春新碱、阿霉素和鬼臼乙叉甙耐药的逆转系数分别为５５，２０和１９，而对５氟尿嘧啶、美法仑的细胞毒性作用无明显影响，表明赛赓啶为多药抗性逆转剂。荧光分光光度法测定表明，赛赓啶可使ＫＢＶ２００细胞内阿霉素蓄积量增加。流式细胞荧光测定显示赛赓啶可增加罗丹明１２３的蓄积并减慢其外排。免疫细胞化学及狭缝杂交表明赛赓啶不影响ＫＢＶ２００细胞的Ｐ糖蛋白染色深度和ｍｄｒ１ＲＮＡ表达水平。以上结果提示赛赓啶的多药抗性逆转机制是抑制Ｐ糖蛋白泵的功能。
To investigate the reversal effect and mechanism of saimine on multidrug resistance in KBV200 cells. In KBV200 cells, MTT assay was used to determine the reversal coefficients of resistance to vincristine, doxorubicin and etoposide in racemectam were 55, 20 and 19 respectively, Fluorouracil, melphalan cytotoxicity had no significant effect, indicating that racenicidin multidrug resistance reversal agent. Fluorescence spectrophotometry showed that racemectin could increase the accumulation of doxorubicin in KBV200 cells. Flow cytometry revealed that stilbene increased the accumulation of rhodamine 123 and slowed its efflux. Immunocytochemistry and slit-hybridization showed that racemidine did not affect the P-glycoprotein staining depth and mdr1RNA expression in KBV200 cells. The above results suggest that racemectin multidrug resistance reversal mechanism is to inhibit the function of P glycoprotein pump.