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

Yunnan Institute of Food Safety, Kunming University of Science and Technology, No. 727 South Jingming Road, Kunming 650500, China
Shandong Provincial Key Laboratory of Biochemical Engineering, College of Marine Science and Biological Engineering, Qingdao University of Science and Technology, Qingdao 266042, China
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;
Received: 23 March 2019 / Revised: 17 April 2019 / Accepted: 25 April 2019 / Published: 13 May 2019
PDF [1080 KB, uploaded 13 May 2019]


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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