0000000000300111
AUTHOR
Pedro Ruiz-giménez
Unraveling the mechanisms of action of lactoferrin-derived antihypertensive peptides: ACE inhibition and beyond
Hypertension is one of the most important causes of cardiovascular and renal morbidity and mortality, and it represents a serious health problem in Western countries. Over the last few decades scientific interest in food-derived antihypertensive peptides has grown as an alternative to drugs in the control of systemic blood pressure. Most of these peptides target the angiotensin I-converting enzyme (ACE) but emerging evidence points to other antihypertensive mechanisms beyond ACE inhibition. The milk protein lactoferrin (LF) is a good source of orally active antihypertensive peptides the characterization of which, including ex vivo functional assays and in vivo approaches, shows that they mi…
Novel antihypertensive hexa- and heptapeptides with ACE-inhibiting properties: From the in vitro ACE assay to the spontaneously hypertensive rat
Bioactive ACE inhibiting peptides are gaining interest in hypertension treatment. We have designed and screened six synthetic heptapeptides (PACEI48 to PACEI53) based on two hexapeptide leads (PACEI32 and PACEI34) to improve ACE inhibitory properties and assess their antihypertensive effects. ACE activity was assayed in vitro and ex vivo. Selected peptides were administered to spontaneously hypertensive rats (SHRs) and normotensive Wistar-Kyoto (WKY) rats. In vitro cytotoxicity was assessed with the MTT reduction test. The six heptapeptides at low micromolar concentration produced different degrees of in vitro inhibition of ACE activity using the synthetic substrate HHL or the natural subst…
Bovine lactoferrin pepsin hydrolysate exerts inhibitory effect on angiotensin I-converting enzyme-dependent vasoconstriction
Abstract The inhibitory effect of a pepsin hydrolysate of bovine lactoferrin (LFH) on angiotensin I-converting enzyme (ACE) has been examined using in vitro and ex vivo functional assays. In vitro assays showed a LFH inhibitory effect on ACE activity with an IC 50 value of 0.95±0.06 mg mL −1 . Ex vivo functional assays using rabbit carotid artery segments showed a LFH inhibitory effect on ACE-dependent angiotensin I-induced contraction, but not on angiotensin II-induced contraction, suggesting that the effect of LFH is not due to antagonism of receptors for angiotensin II. LFH was shown to possess ACE inhibitory effect with potential to modulate hypertension, although the possible inhibitor…
Antihypertensive properties of lactoferricin B-derived peptides.
A set of eight lactoferricin B (LfcinB)-derived peptides was examined for inhibitory effects on angiotensin I-converting enzyme (ACE) activity and ACE-dependent vasoconstriction, and their hypotensive effect in spontaneously hypertensive rats (SHR). Peptides were derived from different elongations both at the C-terminal and N-terminal ends of the representative peptide LfcinB(20-25), which is known as the LfcinB antimicrobial core. All of the eight LfcinB-derived peptides showed in vitro inhibitory effects on ACE activity with different IC(50) values. Moreover, seven of them showed ex vivo inhibitory effects on ACE-dependent vasoconstriction. No clear correlation between in vitro and ex viv…
Antihypertensive effect of a bovine lactoferrin pepsin hydrolysate: Identification of novel active peptides
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