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首页> 外文期刊>International Journal of Environmental Research and Public Health >Genistein and Glyceollin Effects on ABCC2 (MRP2) and ABCG2 (BCRP) in Caco-2 Cells
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Genistein and Glyceollin Effects on ABCC2 (MRP2) and ABCG2 (BCRP) in Caco-2 Cells

机译：Genistein和Glyceollin在Caco-2细胞中对ABCC2（MRP2）和ABCG2（BCRP）的影响

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摘要

The goal of the present study was to determine the effects of glyceollins on intestinal ABCC2 (ATP Binding Cassette C2, multidrug resistance protein 2, MRP2) and ABCG2 (ATP Binding Cassette G2, breast cancer resistance protein, BCRP) function using the Caco-2 cell intestinal epithelial cell model. Glyceollins are soy-derived phytoestrogens that demonstrate anti-proliferative activity in several sources of cancer cells. 5 (and 6)-carboxy-2′,7′-dichloroflourescein (CDF) was used as a prototypical MRP2 substrate; whereas BODIPY-prazosin provided an indication of BCRP function. Comparison studies were conducted with genistein. Glyceollins were shown to inhibit MRP2-mediated CDF transport, with activity similar to the MRP2 inhibitor, MK-571. They also demonstrated concentration-dependent inhibition BCRP-mediated efflux of BODIPY-prazosin, with a potency similar to that of the recognized BCRP inhibitor, Ko143. In contrast, genistein did not appear to alter MRP2 activity and even provided a modest increase in BCRP efflux of BODIPY-prazosin. In particular, glyceollin inhibition of these two important intestinal efflux transporters suggests the potential for glyceollin to alter the absorption of other phytochemicals with which it might be co-administered as a dietary supplement, as well as alteration of the absorption of pharmaceuticals that may be administered concomitantly.
机译：本研究的目的是使用Caco-2确定Glyceollins对肠道ABCC2（ATP结合盒C2，多药抗性蛋白2，MRP2，乳腺癌抗性蛋白，BCRP）功能的影响细胞肠上皮细胞模型。 Glyceollins是大豆衍生的植物雌激素，其在几种癌细胞中显示抗增殖活性。 5（和6）-Carboxy-2'，7'-二氯氟乙烯（CDF）用作原型MRP2基材;虽然Bodipy-prazosin提供了BCRP功能的指示。将比较研究用核酸丁进行。显示Glyceollins以抑制MRP2介导的CDF转运，其活性类似于MRP2抑制剂MK-571。它们还证明了浓度依赖性抑制BCRP介导的Bodipy-Prazosin的介导，具有与公认的BCRP抑制剂KO143类似的效力。相比之下，Genistein没有似乎改变MRP2活性，甚至提供了Bodipy-Prazosin的BCRP Efflux的适度增加。特别地，对于这两个重要的肠道流出转运蛋白的Glyceollin抑制表明Glyceollin的可能性改变其它植物化学物质的吸收，其中可以将其作为膳食补充剂共同施用，以及可以施用的药物的吸收的变化同时。

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