通过原位杂交研究维拉帕米和S9788对多药耐药基因1（MDR-1）信使核糖核酸（mRNA）表达的影响。
Effects of verapamil and S9788 on MDR-1 mRNA expression studied by in situ hybridization.
作者信息
Joly P, Lallemand A, Oum'Hamed Z, Trentesaux C, Idoine O, Desplaces A
机构信息
Laboratoires de Physiologie ou de Biochimie, UFR de Pharmacie, Reims, France.
出版信息
Anticancer Res. 1996 Nov-Dec;16(6B):3609-14.
The effects of Verapamil and S9788 (triazineaminopiperidine), a new modulator of multidrug resistance, on mdr-1 mRNA expression were determined using in situ hybridization. S9788 appeared to be a better reversal drug by strongly decreasing drug efflux. However, Verapamil only decreased mdr-1 mRNA expression in Human erythroleukemic resistant cells (ADM/k562) and in Human lymphoblastic resistant cells (VLB/CEM). This effect occurred in all Verapamil-treated resistant cells with no difference between cell subpopulations. These results were confirmed by slot-blot experiments. In conclusion, S9788 and verapamil effects are comparable overall although the mechanisms responsible for this resistance modulation are not strictly identical.
使用原位杂交技术测定了维拉帕米和新型多药耐药调节剂S9788（三嗪氨基哌啶）对mdr-1 mRNA表达的影响。S9788似乎是一种更好的逆转药物，它能显著降低药物外排。然而，维拉帕米仅在人红白血病耐药细胞（ADM/k562）和人淋巴细胞耐药细胞（VLB/CEM）中降低mdr-1 mRNA表达。这种效应在所有经维拉帕米处理的耐药细胞中均有发生，细胞亚群之间无差异。这些结果通过狭缝印迹实验得到证实。总之，尽管导致这种耐药调节的机制并不完全相同，但S9788和维拉帕米的总体效果相当。
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