Journal
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 69, Issue 19, Pages 5463-5470Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.0c07138
Keywords
umami peptide; DPP-IV inhibitory; ACE inhibitory; interaction mechanism
Funding
- National Natural Science Foundation of China [31771945]
- Science Technology Department of Zhejiang Province [2020C02035, 2018C02051]
- Key Research and Development Program of Ningxia [2019BDE02002]
- Modern Agricultural Technical System Foundation [CARS-42-25]
- Ningbo Natural Science Foundation [2018A610338]
- Ningbo Science Technology Department of China [2019C10065]
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The novel umami peptide IPIPATKT exhibited excellent dual DPP-IV and ACE inhibitory activities, displaying significant physiological effects in cellular and in vivo models.
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.
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