Comparison of an angiotensin-I-converting enzyme inhibitory peptide from tilapia (Oreochromis niloticus) with captopril: inhibition kinetics, in vivo effect, simulated gastrointestinal digestion and a molecular docking study.

Abstract

BACKGROUND:

In order to utilize tilapia skin gelatin hydrolysate protein, which is normally discarded as industrial waste in the process of fish manufacture, we study the in vivo and in vitro angiotensin-I-converting enzyme (ACE) inhibitory activity of the peptide Leu-Ser-Gly-Tyr-Gly-Pro (LSGYGP). The aim was to provide a pharmacological basis of the development of minimal side effects of ACE inhibitors by comparative analysis with captopril in molecular docking.

RESULTS:

This peptide from protein-rich wastes showed excellent ACE inhibitory activity (IC50  = 2.577 μmol L-1 ) and exhibited a mixed noncompetitive inhibitory pattern with Lineweaver-Burk plots. Furthermore, LSGYGP and captopril groups both showed significant decreases in blood pressure after 6 h and maintained good digestive stability over 4 h. Molecular bond interactions differentiate competitive captopril upon hydrogen bond interactions and Zn(II) interaction. The C-terminal Pro generates three interactions (hydrogen bonds, hydrophilic interactions and Van der Waals interactions) in the peptide and effectively interacts with the S1 and S2 pockets of ACE.

CONCLUSION:

LSGYGP, with an IC50 value of 2.577 μmol L-1 , has an antihypertensive effect in spontaneously hypertensive rats. Through comparison with captopril, this study revealed that LSGYGP may be a potential food-derived ACE inhibitory peptide and could act as a functional food ingredient to prevent hypertension. © 2019 Society of Chemical Industry.

• Authors: Jiali Chen, Bomi Ryu, YuanYuan Zhang, Peng Liang, Chengyong Li, Chunxia Zhou, Ping Yang, Pengzhi Hong, Zhong-Ji Qian
• Journal: Journal of the science of food and agriculture (J Sci Food Agric) Vol. 100 Issue 1 Pg. 315-324 (Jan 15 2020) ISSN: 1097-0010 [Electronic] England
• PMID: 31525262 (Publication Type: Comparative Study, Journal Article)
• Copyright: © 2019 Society of Chemical Industry.

Chemical References

• Angiotensin-Converting Enzyme Inhibitors
• Antihypertensive Agents
• Fish Proteins
• Peptides
• Protein Hydrolysates
• Captopril
• Peptidyl-Dipeptidase A

Topics

• Amino Acid Sequence
• Angiotensin-Converting Enzyme Inhibitors (administration & dosage, chemistry, metabolism)
• Animals
• Antihypertensive Agents (administration & dosage, chemistry, metabolism)
• Blood Pressure (drug effects)
• Captopril (administration & dosage, chemistry)
• Cichlids
• Digestion
• Fish Proteins (chemistry)
• Gastrointestinal Tract (metabolism)
• Humans
• Hydrogen Bonding
• Hydrophobic and Hydrophilic Interactions
• Hypertension (drug therapy, metabolism, physiopathology)
• Kinetics
• Male
• Molecular Docking Simulation
• Peptides (chemistry, metabolism, pharmacology)
• Peptidyl-Dipeptidase A (chemistry, metabolism)
• Protein Hydrolysates (chemistry, metabolism)
• Rats
• Rats, Inbred SHR