Effects of hydrophobicity and molecular weight on the transport permeability of oligopeptides across Caco-2 cell monolayers
Effects of hydrophobicity and molecular weight on the transport permeability of oligopeptides across Caco-2 cell monolayers
复制标题
疏水性和分子量对寡肽跨 Caco™2 细胞单层转运渗透性的影响
DOI：
10.1111/jfbc.13188
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发表时间：
2020
影响因子：
4
通讯作者：
Liu Jingbo
中科院分区：
文献类型：
--
作者：
Wang Liying;Ding Long;Du Zhiyang;Liu Jingbo
本文的目的是研究疏水性和分子量（MW）对寡肽跨Caco-2细胞单层的跨上皮转运渗透性的影响。结果表明，不同N端氨基酸的寡肽具有较宽的渗透性值范围，并可根据其与log D和MW的相关性分为三个级别。在良好的渗透性水平下，渗透性与log D正相关，但与MW负相关（p < .001）;在中等渗透性水平下，渗透性与log D和MW负相关（p < .001）;在低渗透性水平下，渗透性与log D和MW正相关（p < .01）。这些结果表明，第一次跨Caco-2细胞单层的寡肽的运输可能是密切相关的log D和MW的分子特性。实际应用大量食源性生物活性肽具有促进健康的作用，并显示出作为功能食品中生物活性成分的潜力。然而，肠道吸收差限制了食品活性肽的应用，特别是含有三个以上氨基酸的寡肽。虽然食源性寡肽在肠上皮中的跨上皮转运已被广泛报道，但其转运机制仍不清楚。我们的研究表明，在Caco-2细胞单层的运输渗透性和log D和MW的寡肽之间的三个层次的关系，并提供了一个新的证据，跨细胞和细胞旁途径的寡肽通过肠道运输的共存。这一结果将有助于了解寡肽在肠道中的转运机制。
The objective of this paper was to investigate the effects of hydrophobicity and molecular weight (MW) on the transepithelial transport permeability of oligopeptides across Caco-2 cell monolayers. Results showed that oligopeptides with different N-terminal amino acids had a wide range of permeability values and could be divided into three levels according to their correlations with log D and MW. At a good level of permeability, the permeability was positively correlated with log D, but negatively correlated with MW (p < .001); at an intermediate level of permeability, the permeability was negatively correlated with log D and MW (p < .001); and at a low level of permeability, the permeability was positively correlated with log D and MW (p < .01). These results suggest for the first time that the transport of oligopeptides across Caco-2 cell monolayers might be closely related to their molecular properties of log D and MW. Practical applications A great number of food-derived bioactive peptides display health-promoting effects and show potential as bioactive ingredients in functional foods. However, the poor absorption in the intestine limits the application of food bioactive peptides, especially for the oligopeptides containing more than three amino acids. Although the transepithelial transport of food-derived oligopeptides in the intestinal epithelium has been widely reported, its transport mechanism is still obscure. Our study shows a three-level relationship between the transport permeability and log D and MW of oligopeptides across Caco-2 cell monolayers and provides a novel evidence for the coexistence of transcellular and paracellular pathways for the transport of oligopeptides through the intestine. This result will contribute to the understanding of the transport mechanisms of oligopeptides in the intestine.