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Mar. Drugs 2018, 16(9), 299; https://doi.org/10.3390/md16090299

Antihypertensive Effects of Two Novel Angiotensin I-Converting Enzyme (ACE) Inhibitory Peptides from Gracilariopsis lemaneiformis (Rhodophyta) in Spontaneously Hypertensive Rats (SHRs)

1,2,3,4,†
,
1,2,3,4,†
,
1,2,3,4
,
1,2,3,4
,
1,2,3,4
,
5,* and 1,2,3,4,*
1
CAS Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China
2
Lab for Marine Biology and Biotechnology, Qingdao National Lab for Marine Sci. & Tech, Qingdao 266071, China
3
University of Chinese Academy of Sciences, Beijing 100049, China
4
Center for Ocean Mega-Science, Chinese Academy of Sciences, 7 Nanhai Road, Qingdao 266071, China
5
College of Marine Life Sciences, Ocean University of China, Qingdao 266071, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 23 July 2018 / Revised: 10 August 2018 / Accepted: 21 August 2018 / Published: 27 August 2018
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Abstract

A variety of biologically active products have been isolated from Gracilariopsis lemaneiformis. In the present study, two novel angiotensin-converting enzyme (ACE) inhibitory peptides, FQIN [M(O)] CILR, and TGAPCR, were screened and identified from G. lemaneiformis protein hydrolysates by LC-MS/MS. The IC50 values of FQIN [M(O)] CILR and TGAPCR were 9.64 ± 0.36 μM and 23.94 ± 0.82 μM, respectively. In the stability study, both peptides showed stabilities of pH, temperature, simulated gastrointestinal digestion, and ACE hydrolysis. The Lineweaver–Burk plot showed that the two peptides were noncompetitive inhibitors of ACE. Molecular docking simulated the intermolecular interactions of two peptides and ACE, and the two peptides formed hydrogen bonds with the active pockets of ACE. However, FQIN [M(O)] CILR was more closely linked to the active pockets of ACE, thereby exerting better ACE inhibition. Spontaneously hypertensive rats (SHRs) were studied with an oral dose of 10 mg/kg body weight. Both peptides reduced systolic blood pressure (SBP) and diastolic blood pressure (DBP) in SHRs, of which FQIN [M(O)] CILR was able to reduce the systolic blood pressure by 34 mmHg (SBP) (p < 0.05). Therefore, FQIN [M(O)] CILR was an excellent ACE inhibitory peptide. View Full-Text
Keywords: Gracilariopsis lemaneiformis; ACE-inhibitory activity; peptide; molecular docking; SHRs Gracilariopsis lemaneiformis; ACE-inhibitory activity; peptide; molecular docking; SHRs
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Deng, Z.; Liu, Y.; Wang, J.; Wu, S.; Geng, L.; Sui, Z.; Zhang, Q. Antihypertensive Effects of Two Novel Angiotensin I-Converting Enzyme (ACE) Inhibitory Peptides from Gracilariopsis lemaneiformis (Rhodophyta) in Spontaneously Hypertensive Rats (SHRs). Mar. Drugs 2018, 16, 299.

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