甲苯咪唑是一种抗寄生虫药物，在胃腹膜癌转移的临床前模型中可抑制药物转运蛋白的表达。
Mebendazole, an antiparasitic drug, inhibits drug transporters expression in preclinical model of gastric peritoneal carcinomatosis.
作者信息
Celestino Pinto Laine, de Fátima Aquino Moreira-Nunes Caroline, Soares Bruno Moreira, Burbano Rommel Mário Rodriguez, de Lemos José Alexandre Rodrigues, Montenegro Raquel Carvalho
机构信息
Biological Science Institute, Federal University of Para, Belem, Pará, Brazil.
Laboratory of Pharmacogenomics, Nucleus of Research and Development of Medicines (NPDM), Federal University of Ceara, Fortaleza, Ceará, Brazil.
出版信息
Toxicol In Vitro. 2017 Sep;43:87-91. doi: 10.1016/j.tiv.2017.06.007. Epub 2017 Jun 9.
The present study aimed to investigate whether MBZ down-regulates drug transporter expression (ABCB1, ABCC1, SLC47A1). mRNA expression level of ABCB1, ABCC1 and SLC47A1 was evaluated by qPCR and protein expression levels MDR-1 was performed by western blotting in malignant ascites cells (AGP-01) treated with MBZ for 24h. The mRNA expression level of ABCB1 and ABCC1 significantly decreased at a 1.0μM of MBZ compared to negative control, while SLC47A1 extremely decreased at all tested concentrations of MBZ. Protein expression levels MDR-1 significantly decreased at a 1.0μM of MBZ compared to negative control. Therefore, our results showed MBZ may play an important role in inhibiting MDR gene expression in malignant ascites cells.
本研究旨在探讨硝唑尼特（MBZ）是否下调药物转运蛋白表达（ABCB1、ABCC1、SLC47A1）。通过qPCR评估ABCB1、ABCC1和SLC47A1的mRNA表达水平，并通过蛋白质印迹法检测用MBZ处理24小时的恶性腹水细胞（AGP-01）中多药耐药蛋白1（MDR-1）的蛋白质表达水平。与阴性对照相比，在1.0μM的MBZ作用下，ABCB1和ABCC1的mRNA表达水平显著降低，而在所有测试浓度的MBZ作用下，SLC47A1极度降低。与阴性对照相比，在1.0μM的MBZ作用下，MDR-1的蛋白质表达水平显著降低。因此，我们的结果表明MBZ可能在抑制恶性腹水细胞中的多药耐药（MDR）基因表达方面发挥重要作用。
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