<br>了解抗高血压肽 Asn-Cys-Trp 的跨上皮运输和跨双层扩散：来自 Caco-2 细胞单层和 DPPC 模型膜的见解,Journal of Agricultural and Food Chemistry

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了解抗高血压肽 Asn-Cys-Trp 的跨上皮运输和跨双层扩散：来自 Caco-2 细胞单层和 DPPC 模型膜的见解
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2024-04-19 , DOI: 10.1021/acs.jafc.4c00155
Sijia Wu ₁ , Ping Jiang ₂ , Xiaoliang Zhang ₁ , Chen Mao ₁ , Yaxi Dai ₁ , Hong Zhuang ₁ , Yong Pang ₁

Affiliation

了解肽 Asn-Cys-Trp (NCW) 的转运机制对于提高其肠道吸收和生物利用度至关重要。本研究研究了 Caco-2 细胞单层对 NCW 的吸收及其与 DPPC 双层的相互作用。结果显示，孵育3 h后，浓度为5 mmol/L的NCW的Papp （AP-BL）和Papp （BL-AP）值分别为（22.24±4.52）× ^10-7和（6.63±2.31） × 10 ^–7 cm/s，传输速率分别为 1.59 ± 0.32 和 0.62 ± 0.20%，表明其中等吸收。发现 NCW 通过 PepT1 和细胞旁转运途径转运，Gly-Pro 和细胞松弛素 D 对Papp值的显着影响证明了这一点。此外，NCW 上调 ZO-1 mRNA 表达。进一步研究 ZO-1 介导的 NCW 和紧密连接蛋白之间的相互作用将有助于更好地理解 NCW 的细胞旁转运机制。 NCW 和 DPPC 双层之间的相互作用主要由熵驱动。 NCW 通过静电、氢键和疏水相互作用渗透双层，导致双层的流动性、柔韧性和无序性以及相变和相分离增加。

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Understanding the Transepithelial Transport and Transbilayer Diffusion of the Antihypertensive Peptide Asn-Cys-Trp: Insights from Caco-2 Cell Monolayers and the DPPC Model Membrane

Understanding the transport mechanism of the peptide Asn-Cys-Trp (NCW) is crucial to improving its intestinal absorption and bioavailability. This study investigated the absorption of NCW through Caco-2 cell monolayers and its interaction with the DPPC bilayers. Results revealed that after a 3 h incubation, the Papp (AP-BL) and Papp (BL-AP) values of NCW at a concentration of 5 mmol/L were (22.24 ± 4.52) × 10^–7 and (6.63 ± 2.31) × 10^–7 cm/s, respectively, with the transport rates of 1.59 ± 0.32 and 0.62 ± 0.20%, indicating its moderate absorption. NCW was found to be transported via PepT1 and paracellular transport pathways, as evidenced by the significant impact of Gly-Pro and cytochalasin D on the Papp values. Moreover, NCW upregulated ZO-1 mRNA expression. Further investigation of the ZO-1-mediated interaction between NCW and tight junction proteins will contribute to a better understanding of the paracellular transport mechanism of NCW. The interaction between NCW and the DPPC bilayers was predominantly driven by entropy. NCW permeated the bilayers through electrostatic, hydrogen bonding, and hydrophobic interactions, resulting in increased fluidity, flexibility, and disorder as well as phase transition and phase separation of the bilayers.

更新日期：2024-04-19

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