Bioavailability of antihypertensive lactoferricin B-derived peptides: Transepithelial transport and resistance to intestinal and plasma peptidases

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• 作者：Ricardo Fern¨¢ndez-Musoles ; Juan B. Salom ; Mar¨ªa Castell¨®-Ruiz ; Mar¨ªa del Mar Contreras ; Isidra Recio ; Paloma Manzanares
• 刊名：International Dairy Journal
• 出版年：2013
• 出版时间：October, 2013
• 年：2013
• 卷：32
• 期：2
• 页码：169-174
• 全文大小：305 K

文摘

The transepithelial transport of the angiotensin I-converting enzyme (ACE)-inhibitory and antihypertensive lactoferricin B (LfcinB)-derived hexapeptide LfcinB_20-25 (RRWQWR) and of its two main fragments RWQ and WQ were investigated using a human intestinal cell (Caco-2) monolayer. The three peptides were susceptible to the action of brush-border peptidases. Intact LfcinB_20-25 was not transported across Caco-2 whereas RWQ and WQ were both absorbed through the cell monolayer. Apparent permeability (P_app) values for absorptive transport across the monolayer were 0.7?¡Á?10^?8?cm?s^?1 (RWQ) and 3.9?¡Á?10^?8?cm?s^?1 (WQ). The effect of pathway-selective inhibitors on peptide absorption suggested paracellular diffusion as the main mechanism for the transport of intact RWQ and WQ. In?vitro incubation in human plasma showed half-life values of 1.9?min (RWQ) and 2.3?h (WQ). These results highlight the possibility of transport of antihypertensive lactoferricin B-derived peptides across human intestinal mucosa.