Abstract：
:Selective GLP-1 secretagogues represent a novel potential therapy for type 2 diabetes mellitus. This study examined the GLP-1 secretory activity of the ethnomedicinal plant, Fagonia cretica, which is postulated to possess anti-diabetic activity. After extraction and fractionation extracts and purified compounds were tested for GLP-1 and GIP secretory activity in pGIP/neo STC-1 cells. Intracellular levels of incretin hormones and their gene expression were also determined. Crude F. cretica extracts stimulated both GLP-1 and GIP secretion, increased cellular hormone content, and upregulated gene expression of proglucagon, GIP and prohormone convertase. However, ethyl acetate partitioning significantly enriched GLP-1 secretory activity and this fraction underwent bioactivity-guided fractionation. Three isolated compounds were potent and selective GLP-1 secretagogues: quinovic acid (QA) and two QA derivatives, QA-3β-O-β-D-glycopyranoside and QA-3β-O-β-D-glucopyranosyl-(28→1)-β-D-glucopyranosyl ester. All QA compounds activated the TGR5 receptor and increased intracellular incretin levels and gene expression. QA derivatives were more potent GLP-1 secretagogues than QA. This is the first time that QA and its naturally-occurring derivatives have been shown to activate TGR5 and stimulate GLP-1 secretion. These data provide a plausible mechanism for the ethnomedicinal use of F. cretica and may assist in the ongoing development of selective GLP-1 agonists.
journal_name
Peptidesjournal_title
Peptidesauthors
Jafri L,Saleem S,Calderwood D,Gillespie A,Mirza B,Green BDdoi
10.1016/j.peptides.2016.01.015subject
Has Abstractpub_date
2016-04-01 00:00:00pages
51-8eissn
0196-9781issn
1873-5169pii
S0196-9781(16)30015-8journal_volume
78pub_type
杂志文章相关文献
PEPTIDES文献大全abstract：:The cellular distribution of PP and PYY in mammals is reviewed. Expression of PP is restricted to endocrine cells mainly present in the pancreas predominantly in the duodenal portion (head) but also found in small numbers in the gastro-intestinal tract. PYY has a dual expression in both endocrine cells and neurons. PY...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/s0196-9781(01)00601-5
更新日期：2002-02-01 00:00:00
abstract：:Corticotropin releasing hormone (CRH) stimulates pituitary ACTH secretion through type-1 CRH (CRH1) receptors. Stimulation of the hypothalamic pituitary adrenal (HPA) axis as well as increased corticotroph responsiveness during stress and adrenalectomy are associated with marked pituitary CRH binding downregulation. T...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/s0196-9781(01)00390-4
更新日期：2001-05-01 00:00:00
abstract：:Although a great deal is published on the MCH neurons, very few works were devoted to the study of their development. However, existing literature points out two important traits: first, these neurons differentiate a MCH phenotype very early in all species studied so far, which might suggest a role for the MCH peptide...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/j.peptides.2009.07.016
更新日期：2009-11-01 00:00:00
abstract：:Atrial natriuretic peptide (ANP) is increasingly expressed on airway and inhibits pulmonary arterial remodeling. However, the role of ANP in remodeling of respiratory system is still unclear. The role of ANP on airway remodeling and the possible mechanism was explored in this study. Both human bronchial epithelial 16H...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2017.02.002
更新日期：2017-04-01 00:00:00
abstract：:Many animal studies show an enhancing effect of vasopressin (VP) on memory, but not all human studies could confirm this finding. This study examined the influence of post-learning administration of VP (40 IU, intranasally) on the consolidation of declarative memories in healthy humans during different intervals of sl...
journal_title：Peptides
pub_type： 临床试验,杂志文章
doi：10.1016/s0196-9781(01)00625-8
更新日期：2002-03-01 00:00:00
abstract：:The binding and internalization of a cytotoxic analogue of luteinizing hormone-releasing hormone (LH-RH), T-98 (agonist [D-Lys6]LH-RH linked to glutaryl-2-(hydroxymethyl)anthraquinone), by rat anterior pituitary cells was investigated. Analogue T-98 was bound to pituitary membrane binding sites for LH-RH with a high a...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(94)90024-8
更新日期：1994-01-01 00:00:00
abstract：:The oligopeptide transporter (PepT1) is located on the brush-border membrane of the intestinal epithelium which has been regarded as a mediator of protein absorption. Here, we cloned and characterized PepT1 genes from diploid (red crucian carp), triploid and tetraploid fish. Then, the PepT1 expression pattern in diffe...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2013.12.017
更新日期：2014-02-01 00:00:00
abstract：:The Manduca allatotropin (Mas-AT) gene is expressed as at least three mRNA isoforms that differ from each other by alternative splicing. The location at which the alternative exons are included in the mature mRNAs occur within the open reading frame, so that three different propeptides are predicted as translation pro...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(00)00378-8
更新日期：2001-02-01 00:00:00
abstract：:A novel peptide, de7b, was isolated from the venom of Conus delessertii, a worm-hunting species collected in the Caribbean Sea off the Yucatan Peninsula. Its primary structure was determined by automated Edman degradation and confirmed by mass spectrometry: it contains 28 amino acids, including six Cys residues. Pepti...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2008.12.005
更新日期：2009-03-01 00:00:00
abstract：:Herein the effect of orexin receptor type-1 antagonist SB-334867 on the development of tolerance to analgesic effects of morphine was studied in rats. To incite tolerance, morphine sulfate was injected intraperitoneally (i.p., 10mg/kg) once a day for 7 days. The tail flick test was used to evaluate antinociceptive eff...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2012.02.023
更新日期：2012-05-01 00:00:00
abstract：:This study determined the long-term influence of prenatal nicotine exposure (PN) on blood pressure and vascular functions in the aged offspring rats. PN did not affect body weight and plasma adrenocorticotropic hormone level; however, it significantly reduced plasma angiotensin I and angiotensin II in both sexes. Syst...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2013.02.019
更新日期：2013-06-01 00:00:00
abstract：:Nonmammalian peptides of the tachykinin, bombesin and opioid families, injected into the brain ventricles, potently and specifically affect drinking behaviour of rats and pigeons. These peptides, or at least their counterparts, have been found in the brain of mammals and birds. It has been hypothesized that these endo...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(85)90372-9
更新日期：1985-01-01 00:00:00
abstract：:Obesity is a chronic inflammatory disease significantly risen worldwide, especially among children. Adipokines, secreted from adipose tissue, are hormones involved in various cellular processes such as energy metabolism and inflammation. Among the others, adiponectin is gaining increasing interest for its insulin-sent...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2014.11.007
更新日期：2015-01-01 00:00:00
abstract：:Neuropeptide FF (NPFF) has certain antiopiate actions and may play a role in opiate tolerance and dependence. Third ventricle injection of 10 micrograms NPFF induces a quasimorphine abstinence syndrome in opiate-naive rats. Nitric oxide synthesis may also contribute to opiate tolerance and dependence. The present stud...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(96)00035-6
更新日期：1996-01-01 00:00:00
abstract：:Using the indirect immunofluorescence method, enkephalin-like immunoreactivity was visualized on human fetus spinal cord sections (gestational age from 17 to 25 weeks). Immunolabeled varicose fibers and terminal-like structures were seen through the whole length fetal spinal cord principally in the dorsal gray, in the...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(88)90018-6
更新日期：1988-01-01 00:00:00
abstract：:Neuropeptide Y (NPY) is one of the most potent stimulants of food intake in mammals, but very little is known about NPY actions in fish. The present study investigated the role of NPY in food intake in the rainbow trout (Oncorhynchus mykiss). Food intake was monitored at different times after intracerebroventricular a...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2005.09.014
更新日期：2006-04-01 00:00:00
abstract：:Rats were injected IP with a 0.1 mg/kg dose of MIF-I, naloxone, dynorphin, [D-Phe4]-Met-enkephalin, [D-Ala2, F5Phe4]-Met-enkephalin-NH2, or the diluent vehicle, placed in their home cages for ten minutes, and then given ad lib access to either 20% sucrose, 10% sucrose, water, 0.01% quinine, or 0.02% quinine in a repea...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(80)90014-5
更新日期：1980-01-01 00:00:00
abstract：:The specific binding of 125I-labeled vasoactive intestinal peptide (VIP) to brain membranes from the forebrain and hindbrain regions of 2 to 37-day postnatal rats was measured. In both regions of the brain, VIP binding was low but detectable two days after birth and rose markedly between postnatal days 7 and 17. This ...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(85)90071-3
更新日期：1985-01-01 00:00:00
abstract：:Naltrexone, an opiate antagonist, was administered to young obese (ob/ob) and lean mice for five weeks. Animals had continuous access to food and received 10 mg/kg SC twice daily with equivalent volumes of saline given to controls. The effects on body weight, and pituitary and plasma levels of beta-endorphin-like mate...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(80)90008-x
更新日期：1980-01-01 00:00:00
abstract：:Previous reports have demonstrated that systemic injection of cholecystokinin (CCK) in rats produces dose-related decreases in food intake, increases in neurohypophyseal secretion of oxytocin (OT), and decreases in gastric emptying. The present studies determined whether systemic injection of bombesin (BBS), another p...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(88)90194-5
更新日期：1988-11-01 00:00:00
abstract：:Angiotensin (Ang)--a peptide that is part of the renin-angiotensin system-induces vasoconstriction and a subsequent increase in blood pressure; Ang peptides, especially AngII, can also act as potent pro-inflammatory mediators. Platelet-activating factor (PAF) is a potent phospholipid mediator that is implicated in man...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2015.09.002
更新日期：2015-11-01 00:00:00
abstract：:The effects of hypergravity on the gene expression of the hypothalamic feeding-related neuropeptides in sham-operated (Sham) and vestibular-lesioned (VL) mice were examined by in situ hybridization histochemistry. Corticotrophin-releasing hormone (CRH) in the paraventricular nucleus was increased significantly in Sham...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2018.05.004
更新日期：2018-07-01 00:00:00
abstract：:The insect kinin neuropeptides have been implicated in the regulation of water balance, digestive organ contraction, and energy mobilization in a number of insect species. A previous solution conformation study of an active, restricted-conformation cyclic analog, identified two possible turn conformations as the likel...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(01)00651-9
更新日期：2002-04-01 00:00:00
abstract：:Investigators studying the primary culprit responsible for Alzheimer disease have, for the past two decades, primarily focused on amyloid-beta (Abeta). Here, we put Abeta on trial and review evidence amassed by the prosecution that implicate Abeta and also consider arguments and evidence gathered by the defense team w...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/s0196-9781(02)00069-4
更新日期：2002-07-01 00:00:00
abstract：:Angiotensin II (ANG II) receptors were present in the thymus of newborn rats (179 +/- 34 fmol/mg protein). In newborns, binding was predominantly localized in the trabecula, and was selectively displaced by the AT2 ligand CGP 42112A (83-85%) and to a lower extent by the AT1 antagonist losartan (15-17%), indicating a m...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(94)90036-1
更新日期：1994-01-01 00:00:00
abstract：:An antifungal peptide with a molecular mass of 9412 and an N-terminal sequence exhibiting notable homology to those of lipid transfer proteins was isolated from seeds of the vegetable Brassica campestris. The purification protocol entailed ion exchange chromatography on Q-Sepharose, affinity chromatography on Affi-gel...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2007.06.028
更新日期：2007-08-01 00:00:00
abstract：:The effects of proadrenomedullin N-terminal 20 peptide (PAMP) and adrenotensin (ADT) on adrenomedullin (ADM)-induced vasodilation were investigated in aortic rings from rat. ADM (10(-9) to 10(-7)M) relaxed the aorta preconstricted with phenylephrine in a concentration-dependent manner. Denudation of endothelium or pre...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/s0196-9781(03)00109-8
更新日期：2003-04-01 00:00:00
abstract：:The major active product of ghrelin gene is a 28-amino acid peptide acylated at the serine 3 position with an octanoyl group, called simply ghrelin. Ghrelin has a multiplicity of physiological functions, affecting GH release, food intake, energy and glucose homeostasis, gastrointestinal, cardiovascular, pulmonary and ...
journal_title：Peptides
pub_type： 杂志文章,评审
doi：10.1016/j.peptides.2008.02.018
更新日期：2008-07-01 00:00:00
abstract：:Glucocorticoids have been shown to decrease CRF receptor binding in the anterior pituitary. To determine whether glucocorticoids or CRF peptide modulate CRF-R1 gene expression, CRF-R1 mRNA levels in rat pituitary and brain were measured after administration of a synthetic glucocorticoid, dexamethasone (DEX) or rat/hum...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/0196-9781(96)00014-9
更新日期：1996-01-01 00:00:00
abstract：:Neurotensin (NT) produces behavioral and physiological effects, including analgesia and hypotheria, when administered into the CNS. Fischer and Lewis rats exhibit differential behavioral responses to central NT receptor activation. To further characterize these differences, we assessed central NT-induced analgesia and...
journal_title：Peptides
pub_type： 杂志文章
doi：10.1016/j.peptides.2003.06.004
更新日期：2003-08-01 00:00:00
