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Antihypertensive Effect in Vivo of QAGLSPVR and Its Transepithelial Transport Through the Caco-2 Cell Monolayer

1
Yunnan Institute of Food Safety, Kunming University of Science and Technology, No. 727 South Jingming Road, Kunming 650500, China
2
Shandong Provincial Key Laboratory of Biochemical Engineering, College of Marine Science and Biological Engineering, Qingdao University of Science and Technology, Qingdao 266042, China
3
Food Science and Technology, Ocean University of China, No 5, Yushan Road, Qingdao 266005, China
*
Author to whom correspondence should be addressed.
Mar. Drugs 2019, 17(5), 288; https://doi.org/10.3390/md17050288
Received: 23 March 2019 / Revised: 17 April 2019 / Accepted: 25 April 2019 / Published: 13 May 2019
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Abstract

The peptide QAGLSPVR, which features high angiotensin-I-converting enzyme (ACE) inhibitory activity, was identified in our previous study. In this study, the in vivo antihypertensive effect of QAGLSPVR was evaluated. Results showed that QAGLSPVR exerts a clear antihypertensive effect on spontaneously hypertensive rats (SHRs), and the systolic and diastolic blood pressures of the rats remarkably decreased by 41.86 and 40.40 mm Hg, respectively, 3 h after peptide administration. The serum ACE activities of SHRs were determined at different times, and QAGLSPVR was found to decrease ACE activities in serum; specifically, minimal ACE activity was found 3 h after administration. QAGLSPVR could be completely absorbed by the Caco-2 cell monolayer, and its transport percentage was 3.5% after 2 h. The transport route results of QAGLSPVR showed that Gly-Sar and wortmannin exert minimal effects on the transport percentage of the peptide (p> 0.05), thus indicating that QAGLSPVR transport through the Caco-2 cell monolayer is not mediated by peptide transporter 1 or transcytosis. By contrast, cytochalasin D significantly increased QAGLSPVR transport (p< 0.05); thus, QAGLSPVR may be transported through the Caco-2 cell monolayer via the paracellular pathway. View Full-Text
Keywords: QAGLSPVR; antihypertensive effect; Caco-2 cell monolayer; transport routes QAGLSPVR; antihypertensive effect; Caco-2 cell monolayer; transport routes
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Sun, L.; Wu, B.; Yan, M.; Hou, H.; Zhuang, Y. Antihypertensive Effect in Vivo of QAGLSPVR and Its Transepithelial Transport Through the Caco-2 Cell Monolayer. Mar. Drugs 2019, 17, 288.

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