Human MDR1 and MRP1 recognize berberine as their transport substrate

Human MDR1 and MRP1 recognize berberine as their transport substrate
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DOI:
10.1271/bbb.60441
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发表时间:
2007-01-01
影响因子:
1.6
通讯作者:
Yazaki, Kazufumi
Yazaki, Kazufumi
中科院分区:
工程技术4区
文献类型:
--
作者:
Shitan, Nobukazu;Tanaka, Miyako;Yazaki, Kazufumi

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为了检查人 ATP 结合盒 (ABC) 转运蛋白是否在植物生物碱小檗碱的解毒中发挥作用,我们使用多药耐药蛋白 1 (MDRI) 和多药耐药相关蛋白 1 (MRP1) 研究了小檗碱的转运。表达 MDR1 或 MRP1 的细胞积累较少的小檗碱。小檗碱的积累取决于细胞 ATP 水平,并被 MDR1 的典型抑制剂逆转,表明人类 MDR1 和 MRP1 直接流出小檗碱作为其底物。
To examine whether human ATP-binding cassette (ABC) transporters play a role in the detoxification of plant alkaloid berberine, we investigated berberine transport using multidrug resistance protein1 (MDRI) and multidrug resistance-associated proteinl (MRP1). Cells expressing MDR1 or MRP1 accumulated less berberine. Berberine accumulation depended on the cellular ATP level, and was reversed by typical inhibitors of MDR1, suggesting that human MDR1 and MRP1 directly efflux berberine as their substrate.