Novel Umami Peptide IPIPATKT with Dual Dipeptidyl Peptidase-IV and Angiotensin I-Converting Enzyme Inhibitory Activities

被引:44
作者
Chen, Mengdi [1 ]
Pan, Daodong [1 ,2 ]
Zhou, Tianqiong [3 ]
Gao, Xinchang [4 ]
Dang, Yali [1 ]
机构
[1] Ningbo Univ, Coll Food & Pharmaceut Sci, State Key Lab Managing Biot & Chem Threats Qual &, Ningbo 315211, Zhejiang, Peoples R China
[2] Jiangxi Normal Univ, Natl R&D Ctr Freshwater Fish Proc, Nanchang 330022, Jiangxi, Peoples R China
[3] Hangzhou Huajin Pharmaceut Co Ltd, Hangzhou 310000, Peoples R China
[4] Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China
基金
中国国家自然科学基金;
关键词
umami peptide; DPP-IV inhibitory; ACE inhibitory; interaction mechanism; FUNCTIONAL-CHARACTERIZATION; IDENTIFICATION; PURIFICATION; ANTIOXIDANT; CASEIN; SILICO;
D O I
10.1021/acs.jafc.0c07138
中图分类号
S [农业科学];
学科分类号
09 ;
摘要
A novel umami peptide, IPIPATKT, showed excellent dual dipeptidyl peptidase-IV (DPP-IV) and angiotensin I-converting enzyme (ACE) inhibitory activities, the IC50 values were 64 and 265 mu M, respectively. Molecular docking displayed that IPIPATKT was docked into the S1 and S2 pockets of ACE, and it was close to the active site pocket of DPP-IV. The insulinresistant-HepG2 (IR-HepG2) cell model and human umbilical vein endothelial cell (HUVEC) model showed that the peptide significantly increased the content of glucose, the activities of hexokinase, pyruvate kinase, and the concentration of nitric oxide (p < 0.01), while it reduced the content of endothelin-1 (ET-1). IPIPATKT exhibited a hypotensive effect (-23.5 +/- 2.2 mmHg) and attenuated the increase in glucose levels in vivo, as demonstrated using spontaneous hypertensive rats (SHRs) and C57BL/6N mice. We reported the in vivo activities of the umami peptide with dual hypertensive and hypoglycemic effects for the first time.
引用
收藏
页码:5463 / 5470
页数:8
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