鉴定具有逆转癌症多药耐药性的潜在特性的含硒化合物。
Identification of selenocompounds with promising properties to reverse cancer multidrug resistance.
作者信息
Domínguez-Álvarez Enrique, Gajdács Márió, Spengler Gabriella, Palop Juan Antonio, Marć Małgorzata Anna, Kieć-Kononowicz Katarzyna, Amaral Leonard, Molnár Joseph, Jacob Claus, Handzlik Jadwiga, Sanmartín Carmen
机构信息
Department of Organic and Pharmaceutical Chemistry, School of Pharmacy, University of Navarra, Irunlarrea 1, 31010 Pamplona, Spain; Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, Hungary.
出版信息
Bioorg Med Chem Lett. 2016 Jun 15;26(12):2821-2824. doi: 10.1016/j.bmcl.2016.04.064. Epub 2016 Apr 22.
In previous studies, 56 novel selenoesters and one cyclic selenoanhydride with chemopreventive, antiproliferative and cytotoxic activity were described. Herein, the selenoanhydride and selected selenoesters were evaluated for their ability to reverse the cancer multidrug resistance (MDR) using the ABCB1 efflux pump inhibition assay in mouse MDR T-lymphoma cells. Results showed that the selenoanhydride (1) and the selenoesters with ketone terminal fragments (9-11) exerted (1.7-3.6)-fold stronger efflux pump inhibitory action than the reference verapamil. In addition, those four derivatives triggered apoptotic events in more than 80% of the examined MDR mouse cells.
在先前的研究中，描述了56种具有化学预防、抗增殖和细胞毒性活性的新型硒酯和一种环状硒酸酐。在此，使用ABCB1外排泵抑制试验在小鼠多药耐药T淋巴瘤细胞中评估了硒酸酐和选定的硒酯逆转癌症多药耐药（MDR）的能力。结果表明，硒酸酐（1）和具有酮末端片段的硒酯（9-11）的外排泵抑制作用比参考药物维拉帕米强（1.7-3.6）倍。此外，这四种衍生物在超过80%的检测多药耐药小鼠细胞中引发了凋亡事件。
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