Current Medicinal Chemistry, 2016.

Modulation of Expression and Activity of ABC Transporters by the Phytoestrogen Genistein. Impact on Drug Disposition

Juan Pablo Rigalli, Nadia Ciriaci, Aldo Domingo Mottino, et al

Institute of Experimental Physiology, Faculty of Biochemical and Pharmaceutical Science, Rosario National University, Suipacha 570, 2000 Rosario, Argentina.

ATP binding cassette (ABC) transporters are involved in drug absorption, distribution and elimination. They also mediate multidrug resistance in cancer cells. Isoflavones, such as genistein (GNT), belong to a class of naturally-occurring compounds found at high concentrations in commonly consumed soya based-foods and dietary supplements. GNT and its metabolites interact with ABC transporters as substrates, inhibitors and/or modulators of their expression. This review compiles information about regulation of ABC transporters by GNT with special emphasis on the three major groups of ABC transporters involved in excretion of endo- and xenobiotics as follows: Pglycoprotein (MDR1, ABCB1), a group of multidrug resistance associated proteins (MRPs, ABCC subfamily) and ABCG2 (BCRP), an ABC half-transporter. The impact of these regulations on potential GNT-drug interactions is further considered.

荷兰《当代药物化学》, 2016.

由植物性雌激素金雀异黄素调节ABC转运蛋白的表达及活性：对药物分布的影响
胡安 巴勃罗 芮盖丽, 纳迪亚 科瑞埃克, 等
实验生理学研究所、 生物化学与制药科学、 罗萨里奥国立大学、 Suipacha 570，系 2000年罗萨里奥，阿根廷

ATP 结合盒 (ABC) 转运蛋白参与了药物的吸收、 分布和消除。它们还介导癌细胞中的多药耐药性。异黄酮，例如染料木素（GNT），属于一类天然存在的化合物，其以高浓度存在于常用的大豆食物和膳食补充剂中。GNT及其代谢物与作为表达的底物抑制剂或调节ABC转运蛋白。本文综述了GNT调节ABC转运蛋白的信息，特别强调涉及内源和外源物排泄的三个主要ABC转运蛋白组：糖蛋白（MDR1，ABCB1），一组多药耐药性相关蛋白（MRPs， ABCC亚家族）和ABCG2（BCRP），ABC半转运蛋白。 进一步考虑这些规定对潜在的GNT-药物相互作用的影响。