期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 67, 期 19, 页码 5544-5551出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.9b00397
关键词
ACE-inhibitory peptide; Caco-2 cells; intestinal transport; liposome; bioavailability
资金
- Natural Science Funding of China [31571852]
- 333 Project Foundation of Jiangsu Province [BRA2017450]
- Jiangsu Agricultural Science and Technology Innovation Fund [CX(18)3036]
- Jiangsu Science and Technology Department [BE 2018397]
The purpose of the study was to investigate the transepithelial transport route of Arg-Leu-Ser-Phe-Asn-Pro (RLSFNP), a milk-derived angiotensin-converting enzyme (ACE) inhibitory peptide, and to encapsulate RLSFNP in a liposome to improve its intestinal bioavailability. The transport route was investigated using transport inhibitors in a human intestinal Caco-2 cell monolayer model. Sodium azide and wortmannin significantly reduced the permeability of RLSFNP (P < 0.01), indicating that energy-dependent transcytosis is involved in the transport of RLSFNP across Caco-2 cells. The hexapeptide RLSFNP was then embedded in liposomes, and the RLSFNP liposome was characterized. Afterward, the cellular uptake and transepithelial transport ability of the RLSFNP liposome across Caco-2 cell monolayers was observed. The results demonstrated that the RLSFNP liposome was successfully prepared, having a significant sustained release and storage capability. The RLSFNP liposome can be absorbed by Caco-2 cells, with an increased intestinal absorption of RLSFNP compared to RLSFNP alone. The results showed a new way to improve RLSFNP intestinal bioavailability.
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