Abstract：
:Two food-derived ACE inhibitory peptides, Ile-Pro-Pro (IPP) and Leu-Lys-Pro (LKP), may have potential as alternative treatments for treatment of mild- or pre-hypertension. Lack of stability to secretory and intracellular peptidases and poor permeability across intestinal epithelia are typical limiting factors of oral delivery of peptides. The stability of IPP and LKP was confirmed in vitro in rat intestinal washes, and intestinal and liver homogenates over 60min. A positive protein control for peptidases, insulin, was significantly digested in each format over the same period. Neither tripeptide showed cytotoxic activity on Caco-2 and Hep G2 cells using the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay, even after chronic exposure. The basal Papp of fluorescein isothiocyanate (FITC)-labeled IPP and FITC-LKP across isolated rat jejunal and colonic mucosae were low, but were significantly increased in each tissue type by the medium chain fatty acids (MCFA) permeation enhancers, sodium caprate (C10) and the sodium salt of 10-undecylenic acid (uC11). IPP and LKP were therefore stable against intestinal and liver peptidases and were non-cytotoxic; their Papp values across rat intestinal mucosae were low, but could be increased by MCFA. There is potential to make on oral dosage form once in vivo pharmacology is confirmed.
journal_name
Peptidesjournal_title
Peptidesauthors
Gleeson JP,Heade J,Ryan SM,Brayden DJdoi
10.1016/j.peptides.2015.05.009subject
Has Abstractpub_date
2015-09-01 00:00:00pages
1-7eissn
0196-9781issn
1873-5169pii
S0196-9781(15)00165-5journal_volume
71pub_type
杂志文章相关文献
PEPTIDES文献大全abstract：:Using a biologically active radioligand, [Tyr(125I)10]VIP, we have identified and characterized receptors for vasoactive intestinal peptide (VIP) on membranes prepared from the rat superior mesenteric artery and bovine coronary arteries. Binding was specific, saturable, reversible and dependent on time and temperature...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(87)90013-1
更新日期：1987-05-01 00:00:00
abstract：:The extractability of neurotensin (NT) from porcine ileal mucosa was studied by comparison of eight extraction procedures. Tissue content of neurotensin-like immunoreactivity was quantitated and characterized by sequence-specific radioimmunoassays and gel filtration chromatography. Homogenization prior to boiling in e...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(87)90038-6
更新日期：1987-07-01 00:00:00
abstract：:Effects of Met-enkephalin (Met-ENK) and opioid antagonists on H2O2 release by peritoneal macrophages from DA and AO rats were investigated. Met-ENK increased and decreased H2O2 production by macrophages of DA and AO rats, respectively. These effects were antagonized by low, but not high, concentrations of naloxone and...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(95)02003-f
更新日期：1995-01-01 00:00:00
abstract：:The immunoregulatory role of methionine-enkephalin (Met-enk) is well studied in mammals, but has not been explored in ectotherms despite the fact that this peptide is highly conserved in vertebrates. The present study demonstrates the diverse effects of Met-enk depending on its concentration and specific function of s...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2009.02.016
更新日期：2009-06-01 00:00:00
abstract：:The neuropeptide calcitonin gene-related peptide (CGRP) may play a role in neurogenic inflammation, tissue remodeling of the uterine cervix, promoting vasodilation, parturition, and processing of sensory information in the spinal cord. CGRP-immunoreactive nerves of the cervix and spinal cord have been studied but cell...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(01)00638-6
更新日期：2002-03-01 00:00:00
abstract：:The temporins are a family of hydrophobic, C-terminally alpha-amidated antimicrobial peptides that are synthesized in the skins of a wide range of species of frogs belonging to the genus Rana. In the present study, we investigated using RT-PCR the expression of preprotemporin mRNAs in extradermal tissues of Tago's bro...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2006.03.023
更新日期：2006-09-01 00:00:00
abstract：:This work determined Plasmodium falciparum merozoite surface protein-8 (MSP-8) regions specifically binding to membrane surface receptors on human erythrocytes. Five high activity binding peptides (HABPs), whose binding to erythrocytes became saturable and sensitive on being treated with neuraminidase and chymotrypsin...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(03)00185-2
更新日期：2003-07-01 00:00:00
abstract：:The effect of caseinomacropeptide (CMP) (the [106-169] fragment of kappa-casein produced during digestion of milk protein), was studied in anesthetized rats using bile diversion for a pure pancreatic juice collection system. Intraduodenal administration of CMP induced a dose-related specific stimulation of pancreatic ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(00)00307-7
更新日期：2000-10-01 00:00:00
abstract：:We investigated the effect of synthetic antimicrobial decapeptide KSL-W (KKVVFWVKFK) on normal human gingival fibroblast growth, migration, collagen gel contraction, and α-smooth muscle actin protein expression. Results show that in addition to promoting fibroblast adhesion by increasing F-actin production, peptide KS...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2017.05.003
更新日期：2017-07-01 00:00:00
abstract：:In the rat small intestine, neurotrophin-3 immunoreactivity was identified in ganglion cells and in processes mostly innervating the mucosa and occasionally the muscle layer and vasculature. The vast majority of neurotrophin-3 immunoreactive neurons contained vasoactive intestinal polypeptide (VIP), but not substance ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(00)00286-2
更新日期：2000-09-01 00:00:00
abstract：:Neuropeptides related to vertebrate tachykinins have been identified in Drosophila and are referred to as drosotachykinins, or DTKs. Two Drosophila G protein-coupled receptors, designated NKD (neurokinin receptor from Drosophila; CG6515) and DTKR (Drosophila tachykinin receptor; CG7887), display sequence similarities ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2008.10.012
更新日期：2009-03-01 00:00:00
abstract：:Neuropeptide S (NPS), the endogenous ligand of NPS receptor (NPSR), regulates many biological functions, including arousal, anxiety, locomotion and food intake. NPSR mRNA is expressed in several regions of central autonomic network through which the brain controls visceromotor and other responses essential for surviva...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2009.03.012
更新日期：2009-07-01 00:00:00
abstract：:Because plasma levels of protein C (PC) or activated protein C (APC) are altered in certain diseases associated with vascular dysfunction, and APC has therapeutic potential in preventing microvascular coagulation in severe sepsis, potential vascular effects of PC and APC were compared to those of the vasoactive peptid...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(00)00264-3
更新日期：2000-08-01 00:00:00
abstract：:Members of the neprilysin family of neutral endopeptidases (M13) are typically membrane-bound enzymes known to be involved in the extra-cellular metabolism of signalling peptides and have important roles during mammalian embryogenesis. In this study we show that membranes prepared from embryos of Drosophila melanogast...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2006.08.032
更新日期：2007-01-01 00:00:00
abstract：:It is well known that neuropeptide Y (NPY) and gamma-aminobutyric acid (GABA) exert antiepileptic effects in animal models. It has recently been shown that ghrelin neurons increase the activities of GABA and NPY in the brain. Therefore it can be said that ghrelin is an antiepileptic agent. In this study we aimed to in...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2007.04.003
更新日期：2007-06-01 00:00:00
abstract：:We have studied the in vitro effect of VIP and histamine on ultrastructure of the parietal cells in isolated guinea pig fundic glands. The morphological changes induced by histamine in the parietal cells can be compared to those observed after histamine stimulation in vivo or in vitro on gastric mucosa preparations. I...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(84)90219-5
更新日期：1984-03-01 00:00:00
abstract：:We have used high performance liquid chromatography and radioimmunoassay to characterize the CCK-like molecules in the central nervous system. The major form of CCK is the sulfated octapeptide. This molecule is distributed unevenly among various brain regions; the highest levels are found in the cortex and striatum. W...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(81)90015-2
更新日期：1981-01-01 00:00:00
abstract：:The vasoactive peptide urotensin-II (U-II) is best known for its ability to regulate peripheral vascular and cardiac contractile function in vivo, and recent in vitro studies have suggested a role for the peptide in the control of vascular remodeling by inducing smooth muscle proliferation and fibroblast-mediated coll...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2005.05.028
更新日期：2005-12-01 00:00:00
abstract：:A functional study has been performed to characterise the Y receptors responsible for NPY, PYY and PP-stimulated responses in mouse colonic mucosal preparations. Electrogenic ion secretion was stimulated with VIP following which NPY, PYY and PP analogues were, to varying degrees, inhibitory. PYY(3-36), hPP, Gln(23)hPP...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(01)00355-2
更新日期：2001-03-01 00:00:00
abstract：:Expression of the two gonadotropin-releasing hormone homologue peptides GnRHI and GnRHII and their receptor GnRHR has been demonstrated in a number of malignancies. In hormone-dependent breast cancer, GnRH analogs are used for therapy in premenopausal women. Gene expression of GnRHI, II and R was studied in breast bio...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2012.12.016
更新日期：2013-04-01 00:00:00
abstract：:Vasoactive intestinal peptide (VIP) is a potent anti-inflammatory agent. In addition to the deactivation of macrophages, dendritic cells, and microglia, VIP shifts the Th1/Th2 balance, promoting the preferential differentiation and survival of Th2 cells, to the detriment of the proinflammatory Th1 effectors. Several m...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2007.03.015
更新日期：2007-09-01 00:00:00
abstract：:Diapause pupae of the swallowtail butterfly Papilio xuthus L. exhibit diapause-green, orange and brownish-orange color polymorphism. Development of orange pupae involves a neuroendocrine factor inducing orange pupa (Orange-Pupa-Inducing Factor, OPIF), which is secreted from the head-thoracic region during late pharate...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2005.06.025
更新日期：2006-03-01 00:00:00
abstract：:Venom small peptides that target neurotrophin receptors might be beneficial in neurodegeneration, including Parkinsońs disease (PD). Their small size, ease of synthesis, structural stability and target selectivity make them important tools to overcome the limitations of endogenous neurotrophins as therapeutic agents. ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2018.04.012
更新日期：2018-06-01 00:00:00
abstract：:A retrograde facilitation has been demonstrated in the one trial step-down inhibitory avoidance of melanin-concentrating hormone (MCH), when it was infused into rat hippocampal formation. Considering the high density of specific binding sites for the MCH peptide on the hippocampus and the participation of this structu...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(01)00591-5
更新日期：2002-01-01 00:00:00
abstract：:Melanocortins (MCs) are multifunctional peptide hormones that regulate a diversity of physiological functions. MCs have been implicated in sexual function in animals. We document here that a MC analog, Melanotan II (MTII), can enhance sexual function in human males (erectile activity) and females (increased levels of ...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/j.peptides.2005.01.023
更新日期：2005-10-01 00:00:00
abstract：:We sought to establish Endothelin (ET-3) role in the central regulation of bile secretion in the rat. The intracerebroventricular (icv) injection of ET-3 evoked a cholestatic or a choleretic effect depending on the administered dose. Lower doses increased bile flow and bicarbonate excretion, whereas higher doses decre...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2005.02.003
更新日期：2005-07-01 00:00:00
abstract：:In the Nucleus Ambiguus (NA) mu-receptors increased mean arterial pressure (MAP) and heart rate (HR) and kappa-receptors decreased MAP without altering HR. Mu-receptors in the Dorsal Motor Nucleus of the Vagus (DMV) increased MAP without changing HR whereas kappa-receptors in the DMV decreased HR without changing MAP....
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(88)90225-2
更新日期：1988-01-01 00:00:00
abstract：:Neuropeptide Y (NPY) injected into the hypothalamus stimulates feeding and affects pituitary secretion. Insulin-deficient diabetes and food deprivation markedly increase hypothalamic NPY and NPY mRNA levels, suggesting increased activity of NPYergic pathways in the hypothalamus, which could account for hyperphagia and...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(93)90070-w
更新日期：1993-09-01 00:00:00
abstract：:Obestatin is purported to be a peptide hormone encoded in preproghrelin. We studied the metabolic effects of continuous infusion of obestatin via subcutaneously implanted osmotic mini-pumps. Administration of up to 500nmol/kg body weight/day obestatin did not change 24h cumulative food intake or body weight in rats. S...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2008.03.023
更新日期：2008-08-01 00:00:00
abstract：:Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2 (NPFF), an endogenous mammalian antiopioid peptide, has been shown by other laboratories to attenuate the acute antinociceptive effects of morphine, the development of morphine tolerance, and naloxone-induced withdrawal in morphine-dependent rats. The present study determined the ef...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(93)90187-l
更新日期：1993-11-01 00:00:00
