Transport mechanism of flavanone aglycones across Caco-2 cell monolayers and artificial PAMPA membranes
Transport mechanism of flavanone aglycones across Caco-2 cell monolayers and artificial PAMPA membranes
复制标题
黄烷酮苷元跨 Caco-2 细胞单层和人工 PAMPA 膜的转运机制
DOI：
10.1111/j.2042-7158.2011.01374.x
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发表时间：
2012
影响因子：
3.3
通讯作者：
Ogihara T
中科院分区：
文献类型：
--
作者：
Kobayashi S;Nagai T;Konishi Y;Tanabe S;Morimoto K;Ogihara T
目的我们最近报道了黄酮苷元（橙皮素、柚皮素和圣草酚）在Caco-2细胞中除了通过跨细胞被动扩散外，还通过质子偶联主动转运被有效吸收。在这里，我们旨在详细评估这些黄烷酮的吸收机制，方法通过体外研究，在pH梯度和等pH条件下，在Caco-2细胞中平行进行人工膜渗透试验（PAMPA），评价上述化合物的吸收机制。2细胞和PAMPA在这些条件下，以及考虑的物理化学性质，表明橙皮素，柚皮素，圣草酚和homo圣草酚有效地运输被动扩散根据pH值分区假设，除了在樱花的情况下。然而，运输的所有黄烷酮显着的温度依赖性，并显着减少时，Caco-2细胞处理的氨基酸修饰reagents.ConclusionsOur数据证实，被动扩散和主动运输机制有助于黄烷酮吸收通过人肠上皮。
ObjectivesWe recently reported that flavanone aglycones (hesperetin, naringenin and eriodictyol) are efficiently absorbed via proton-coupled active transport, in addition to transcellular passive diffusion, in Caco-2 cells. Here, we aimed to evaluate in detail the absorption mechanisms of these flavanones, as well as homoeriodictyol and sakuranetin.MethodsWe evaluated the absorption mechanisms of the above compounds by means of in vitro studies in Caco-2 cells in parallel with an artificial membrane permeation assay (PAMPA) under pH-gradient and iso-pH conditions.Key findingsComparison of the permeability characteristics of flavanones in Caco-2 cells and in PAMPA under these conditions, as well as a consideration of the physicochemical properties, indicated that hesperetin, naringenin, eriodictyol and homoeriodictyol were efficiently transported by passive diffusion according to the pH-partition hypothesis, except in the case of sakuranetin. However, transport of all flavanones were remarkably temperature-dependent, and was significantly reduced when Caco-2 cells were treated with amino acid-modifying reagents.ConclusionsOur data confirm that both passive diffusion and an active transport mechanism contribute to flavanone absorption through human intestinal epithelium.