Abstract

The renin-angiotensin-aldosterone system (RAAS) plays an important role in regulating hypertension by controlling vasoconstriction and intravascular fluid volume. RAAS itself is largely regulated by the actions of renin (EC 3.4.23.15) and the angiotensin-I-converting enzyme (ACE-I; EC 3.4.15.1). The enzyme dipeptidyl peptidase-IV (DPP-IV; EC 3.4.14.5) also plays a role in the development of type-2 diabetes. The inhibition of the renin, ACE-I, and DPP-IV enzymes has therefore become a key therapeutic target for the treatment of hypertension and diabetes. The aim of this study was to assess the bioactivity of different oat (Avena sativa) protein isolates and their ability to inhibit the renin, ACE-I, and DPP-IV enzymes. In silico analysis was carried out to predictthe likelihood of bioactive inhibitory peptides occurring from oat protein hydrolysates following in silico hydrolysis with the proteases papain and ficin. Nine peptides, including FFG, IFFFL, PFL, WWK, WCY, FPIL, CPA, FLLA, and FEPL were subsequently chemically synthesised, and their bioactivities were confirmed using in vitro bioassays. The isolated oat proteins derived from seven different oat varieties were found to inhibit the ACE-I enzyme by between 86.5 ± 10.7% and 96.5 ± 25.8%, renin by between 40.5 ± 21.5% and 70.9 ± 7.6%, and DPP-IV by between 3.7 ± 3.9% and 46.2 ± 28.8%. The activity of the synthesised peptides was also determined.

Highlights

  • High blood pressure is the single largest risk factor attributed to deaths worldwide

  • renin-angiotensin-aldosterone system (RAAS) itself is largely regulated by the actions of the enzyme angiotensin-I-converting enzyme (ACE-I; EC 3.4.15.1), which increases blood pressure [3]

  • In silico analysis of oat protein isolates identified a number of bioactive peptides that had previously been reported in the BIOPEP database (Table 3)

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Summary

Introduction

High blood pressure is the single largest risk factor attributed to deaths worldwide. It is responsible for 12.8% of deaths, and affects all countries and income groups [1]. High systolic blood pressure is globally attributable to 51% of strokes, 45% of ischaemic heart disease, and between 37%. (Southeast Asia) and 54% (European countries) of cardiovascular deaths [1]. The renin-angiotensin-aldosterone system (RAAS) plays an important role in regulating blood pressure by controlling arteriolar vasoconstriction and intravascular fluid volume. RAAS itself is largely regulated by the actions of the enzyme angiotensin-I-converting enzyme (ACE-I; EC 3.4.15.1), which increases blood pressure [3]

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