Novel angiotensin-converting enzyme and pancreatic lipase oligopeptide inhibitors from fermented rice bran

Jingfei Hu; Huanyu Wang; Nanhai Weng; Tong Wei; Xueqing Tian; Jing Lu; Mingsheng Lyu; Shujun Wang

doi:10.3389/fnut.2022.1010005

Novel angiotensin-converting enzyme and pancreatic lipase oligopeptide inhibitors from fermented rice bran

Front Nutr. 2022 Sep 15:9:1010005. doi: 10.3389/fnut.2022.1010005. eCollection 2022.

Authors

Jingfei Hu^{1

2

3}, Huanyu Wang^{1

2

3}, Nanhai Weng^{1

2

3}, Tong Wei^{1

2

3}, Xueqing Tian^{1

2

3}, Jing Lu^{1

2

3}, Mingsheng Lyu^{1

2

3}, Shujun Wang^{1

2

3}

Affiliations

¹ Jiangsu Key Laboratory of Marine Bioresources and Environment, Jiangsu Ocean University, Lianyungang, China.
² Jiangsu Key Laboratory of Marine Biotechnology, Jiangsu Ocean University, Lianyungang, China.
³ Co-Innovation Center of Jiangsu Marine Bio-industry Technology, Jiangsu Ocean University, Lianyungang, China.

Abstract

This study determined the inhibitory activity of oligopeptides against angiotensin-converting enzyme (ACE) and pancreatic lipase through in vitro tests, molecular docking, and enzyme inhibition. The results showed that the IC₅₀ of GLLGY, HWP, and VYGF for ACE inhibition was 1 mg/mL, and the IC₅₀ of HWP for pancreatic lipase was 3.95 mg/mL. Molecular docking revealed that the binding energies between GLLGY, HWP, and VYGF and ACE were -9.0, -8.4, and -9.2 kcal/mol, respectively. The binding free energy between HWP and pancreatic lipase was -7.3 kcal/mol. GLLGY, HWP, and VYGF inhibited ACE compentitively. HWP inhibited pancreatic lipase through non-competition. in vitro simulated gastrointestinal digestion, the three oligopeptides still had inhibitory activity and low toxicity. The results revealed that the peptides GLLGY, HWP, and VYGF may be suitable candidates for further research on ACE inhibition, and HWP may be a suitable candidate for studying pancreatic lipase inhibition.

Keywords: ACE; bioactive oligopeptides; inhibitory kinetic; molecular docking; pancreatic lipase.