Antihypertensive and cardioprotective effects of the dipeptide isoleucine-tryptophan and whey protein hydrolysate

Acta Physiol (Oxf). 2015 Dec;215(4):167-76. doi: 10.1111/apha.12578. Epub 2015 Sep 22.

Abstract

Aims: Angiotensin-converting enzyme inhibitors are treatment of choice in hypertensive patients. Clinically used inhibitors exhibit a structural similarity to naturally occurring peptides. This study evaluated antihypertensive and cardioprotective effects of ACE-inhibiting peptides derived from food proteins in spontaneously hypertensive rats.

Methods and results: Isoleucine-tryptophan (in vitro IC50 for ACE = 0.7 μm), a whey protein hydrolysate containing an augmented fraction of isoleucine-tryptophan, or captopril was given to spontaneously hypertensive rats (n = 60) over 14 weeks. Two further groups, receiving either no supplement (Placebo) or intact whey protein, served as controls. Systolic blood pressure age-dependently increased in the Placebo group, whereas the blood pressure rise was effectively blunted by isoleucine-tryptophan, whey protein hydrolysate and captopril (-42 ± 3, -38 ± 5, -55 ± 4 mm Hg vs. Placebo). At study end, myocardial mass was lower in isoleucine-tryptophan and captopril groups but only partially in the hydrolysate group. Coronary flow reserve (1 μm adenosine) was improved in isoleucine-tryptophan and captopril groups. Plasma ACE activity was significantly decreased in isoleucine-tryptophan, hydrolysate and captopril groups, but in aortic tissue only after isoleucine-tryptophan or captopril treatment. This was associated with lowered expression and activity of matrix metalloproteinase-2. Following isoleucine-tryptophan and captopril treatments, gene expression of renin was significantly increased indicating an active feedback within renin-angiotensin system.

Conclusion: Whey protein hydrolysate and isoleucine-tryptophan powerfully inhibit plasma ACE resulting in antihypertensive effects. Moreover, isoleucine-tryptophan blunts tissue ACE activity, reduces matrix metalloproteinase-2 activity and improves coronary flow reserve. Thus, whey protein hydrolysate and particularly isoleucine-tryptophan may serve as innovative food additives with the goal of attenuating hypertension.

Keywords: angiotensin-converting enzyme; arterial hypertension; cardiac hypertrophy; matrix metalloproteinases; whey proteins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin-Converting Enzyme Inhibitors / pharmacology
  • Animals
  • Antihypertensive Agents / pharmacology*
  • Blood Pressure / drug effects
  • Captopril / pharmacology
  • Cardiotonic Agents / pharmacology*
  • Dipeptides / pharmacology*
  • Disease Models, Animal
  • Humans
  • Hypertension / drug therapy
  • Hypertension / metabolism*
  • Hypertension / physiopathology
  • Isoleucine / pharmacology
  • Male
  • Protein Hydrolysates / pharmacology
  • Rats
  • Rats, Inbred SHR
  • Renin-Angiotensin System / drug effects
  • Tryptophan / pharmacology
  • Whey / chemistry*

Substances

  • Angiotensin-Converting Enzyme Inhibitors
  • Antihypertensive Agents
  • Cardiotonic Agents
  • Dipeptides
  • Protein Hydrolysates
  • Isoleucine
  • Tryptophan
  • Captopril