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The purpose of this article is to elucidate the transport permeability and route of ACE\u2010inhibitory peptide Arg\u2010Leu\u2010Ser\u2010Phe\u2010Asn\u2010Pro (RLSFNP) across the intestinal epithelium using Caco\u20102 cell monolayers.<\/jats:p><\/jats:sec><jats:sec><jats:title>RESULTS<\/jats:title><jats:p>Intact RLSFNP and RLSFNP breakdown fragments F, FNP, SFNP and RLSF were found in RLSFNP transport solution across Caco\u20102 cell monolayers using ultra\u2010performance liquid chromatography\u2013tandem mass spectrometry. RLSFNP fragments FNP, SFNP and RLSF also contributed to ACE inhibitory effects. Protease inhibitors (bacitracin and leupeptin) and absorption enhancers (sodium glycocholate hydrate, sodium deoxycholate and Na<jats:sub>2<\/jats:sub>EDTA) improved the transport flux of RLSFNP. A transport inhibitor experiment showed that intact RLSFNP may be transported via the paracellular route.<\/jats:p><\/jats:sec><jats:sec><jats:title>CONCLUSION<\/jats:title><jats:p>Intact RLSFNP can be transported across the Caco\u20102 cell monolayers via the paracellular route. Extensive hydrolysis was the chief reason for the low permeability of RLSFNP. \u00a9 2017 Society of Chemical Industry<\/jats:p><\/jats:sec>","DOI":"10.1002\/jsfa.8545","type":"journal-article","created":{"date-parts":[[2017,7,17]],"date-time":"2017-07-17T01:12:41Z","timestamp":1500253961000},"page":"976-983","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":31,"title":["Transepithelial transport of milk\u2010derived angiotensin I\u2010converting enzyme inhibitory peptide with the RLSFNP sequence"],"prefix":"10.1002","volume":"98","author":[{"given":"Yuxing","family":"Guo","sequence":"first","affiliation":[{"name":"Department of Food Science and Technology, Ginling College Nanjing Normal University  Nanjing China"},{"name":"Foods for Health Institute, Department of Food Science and Technology University of California  Davis CA 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