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https://www.readbyqxmd.com/read/29590554/lateral-septum-growth-hormone-secretagogue-receptor-affects-food-intake-and-motivation-for-sucrose-reinforcement
#1
Sarah J Terrill, Kaylee D Wall, Nelson D Medina, Calyn B Maske, Diana L Williams
The hormone ghrelin promotes eating and is widely considered to be a hunger signal. Ghrelin receptors, growth hormone secretagogue receptors (GHSRs), are found in a number of specific regions throughout the brain, including the lateral septum (LS), an area not traditionally associated with the control of feeding. Here we investigated whether GHSRs in the LS play a role in the control of food intake. We examined the feeding effects of ghrelin and the GHSR antagonists ([D-Lys3]-GHRP-6 and JMV 2959), at doses subthreshold for effect when delivered to the lateral ventricle...
March 28, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29526750/the-ghrelin-paradox-in-the-control-of-equine-chondrocyte-function-the-good-and-the-bad
#2
Serena Ceriotti, Anna Lange Consiglio, Lavinia Casati, Fausto Cremonesi, Valeria Sibilia, Francesco Ferrucci
Increasing evidence suggests a role for ghrelin in the control of articular inflammatory diseases like osteoarthritis (OA). In the present study we examined the ability of ghrelin to counteract LPS-induced necrosis and apoptosis of chondrocytes and the involvement of GH secretagogue receptor (GHS-R)1a in the protective action of ghrelin. The effects of ghrelin (10-7 -10-11  mol/L) on equine primary cultured chondrocytes viability and necrosis in basal conditions and under LPS treatment (100 ng/ml) were detected by using both acridine orange/propidium iodide staining and annexin-5/propidium iodide staining...
March 8, 2018: Peptides
https://www.readbyqxmd.com/read/29300858/evidence-supporting-a-role-for-constitutive-ghrelin-receptor-signaling-in-fasting-induced-hyperphagia-in-male-mice
#3
Gimena Fernandez, Agustina Cabral, María F Andreoli, Alexandra Labarthe, Céline M'Kadmi, Jorge G Ramos, Jacky Marie, Jean-Alain Fehrentz, Jacques Epelbaum, Virginie Tolle, Mario Perello
Ghrelin is a potent orexigenic peptide hormone that acts through the growth hormone secretagogue receptor (GHSR), a G protein-coupled receptor highly expressed in the hypothalamus. In vitro studies have shown that GHSR displays a high constitutive activity, whose physiological relevance is uncertain. As GHSR gene expression in the hypothalamus is known to increase in fasting conditions, we tested the hypothesis that constitutive GHSR activity at the hypothalamic level drives the fasting-induced hyperphagia...
February 1, 2018: Endocrinology
https://www.readbyqxmd.com/read/29137815/local-injection-of-d-lys-3-ghrp-6-in-the-rat-amygdala-dentate-gyrus-or-ventral-tegmental-area-impairs-memory-consolidation
#4
Siamak Beheshti, Neda Aslani
It is well known that the hormone ghrelin affects learning and memory in different experimental models of learning. Though, the effect of antagonism of ghrelin receptor type 1a (GHS-R1a) in various regions of the brain and on different stages of learning has not been examined. In this study the effect of injection of a GHS-R1a selective antagonist (d-Lys-3-GHRP-6) into the basolateral amygdala, dentate gyrus or ventral tegmental area was examined on memory consolidation in the passive avoidance task. Adult male Wistar rats weighing 230-280g were used...
November 4, 2017: Neuropeptides
https://www.readbyqxmd.com/read/29028172/influences-of-histidine-1-and-azaphenylalanine-4-on-the-affinity-anti-inflammatory-and-antiangiogenic-activities-of-azapeptide-cluster-of-differentiation-36-receptor-modulators
#5
Kelvine Chignen Possi, Mukandila Mulumba, Samy Omri, Yesica Garcia-Ramos, Houda Tahiri, Sylvain Chemtob, Huy Ong, William D Lubell
Azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) exhibit promising affinity, selectivity, and modulator activity on the cluster of differentiation 36 receptor (CD36). For example, [A1 , azaF4 ]- and [azaY4 ]-GHRP-6 (1a and 2b) were previously shown to bind selectively to CD36 and exhibited respectively significant antiangiogenic and slight angiogenic activities in a microvascular sprouting assay using choroid explants. The influences of the 1- and 4-position residues on the affinity, anti-inflammatory, and antiangiogenic activity of these azapeptides have now been studied in detail by the synthesis and analysis of a set of 25 analogues featuring Ala1 or His1 and a variety of aromatic side chains at the aza-amino acid residue in the 4-position...
November 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28993142/ghrelin-upregulates-the-phosphorylation-of-the-glun2b-subunit-of-the-nmda-receptor-by-activating-ghsr1a-and-fyn-in-the-rat-hippocampus
#6
Liza Berrout, Masako Isokawa
Ghrelin and its receptor GHSR1a have been shown to exert numerous physiological functions in the brain, in addition to the well-established orexigenic role in the hypothalamus. Earlier work indicated that ghrelin stimulated the phosphorylation of the GluN1 subunit of the NMDA receptor (NMDAR) and enhanced synaptic transmission in the hippocampus. In the present study, we report that the exogenous application of ghrelin increased GluN2B phosphorylation. This increase was independent of GluN2B subunit activity or NMDAR channel activity...
January 1, 2018: Brain Research
https://www.readbyqxmd.com/read/28985965/ghrelin-projection-from-the-lateral-hypothalamus-area-to-the-dorsal-vagal-complex-and-its-regulation-of-gastric-motility-in-cisplatin-treated-rats
#7
Yanling Gong, Yang Liu, Yaoyao Guo, Manqing Su, Yifan Zhong, Luo Xu, Feifei Guo, Shengli Gao
OBJECTIVE: To investigate ghrelin projection from the lateral hypothalamus area (LHA) to the dorsal vagal complex (DVC) and its regulation of gastric motility in cisplatin-treated rats. MATERIALS AND METHODS: In the present study, the protein and mRNA expression of ghrelin and its receptor GHSR-1a were measured by Western blot and PCR, respectively. The ghrelin fiber projections arising from the LHA and projecting to the DVC were investigated by retrograde tracing combined with fluoro-immunohistochemical staining...
September 28, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28941172/characterization-of-in-vitro-generated-metabolites-of-selected-peptides-2-kda-prohibited-in-sports
#8
Andreas Thomas, Andre Knoop, Wilhelm Schänzer, Mario Thevis
With an increasing number of prohibited substances in doping controls, knowledge about their metabolism is crucial for efficient analysis. While for low molecular mass molecules, standard protocols for in vitro metabolism experiments are well established, the situation with peptidic drugs has been shown to be substantially more heterogeneous and complex. Two principle strategies aiming at simulating the metabolism of lower molecular mass peptides in vitro are presented within this study. The prohibited peptides ARA-290, GHRP-3, and Peforelin, with a to-date unknown metabolism, were chosen as model compounds for these experiments and metabolism after incubation with different blood specimens (EDTA-, heparin-, citrate-plasma, and serum) and exposure to recombinant amidase were investigated...
November 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#9
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28903914/long-term-treatment-with-the-ghrelin-receptor-antagonist-d-lys3-ghrp-6-does-not-improve-glucose-homeostasis-in-nonobese-diabetic-mkr-mice
#10
Rasha Mosa, Lili Huang, Hongzhuo Li, Michael Grist, Derek LeRoith, Chen Chen
Long-term treatment with the ghrelin receptor antagonist [d-Lys3]-GHRP-6 does not improve glucose homeostasis in nonobese diabetic MKR mice. Am J Physiol Regul Integr Comp Physiol 314: R71-R83, 2018. First published September 13, 2017; doi: 10.1152/ajpregu.00157.2017 .-Ghrelin secretion has been associated with increased caloric intake and adiposity. The expressions of ghrelin and its receptor (GHS-R1a) in the pancreas has raised the interest about the role of ghrelin in glucose homeostasis. Most of the studies showed that ghrelin promoted hyperglycemia and inhibited insulin secretion...
January 1, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28893476/growth-hormone-releasing-peptide-6-enhanced-antibody-titers-against-subunit-antigens-in-mice-balb-c-tilapia-oreochromis-niloticus-and-african-catfish-clarias-gariepinus
#11
Rebeca Martínez, Liz Hernández, Lázaro Gil, Yamila Carpio, Antonio Morales, Fidel Herrera, Alina Rodríguez-Mallón, Yeny Leal, Aracelys Blanco, Mario Pablo Estrada
Modern subunit vaccines have excellent safety profiles and improved tolerability, but do not elicit strong immune responses without the addition of adjuvants. Developing a safe and affective adjuvant remains a challenge for peptide-based vaccine design. Growth Hormone Releasing Peptide-6 (GHRP-6) is one of the earliest-developed, synthetic, peptidyl growth hormone secretagogue receptor agonists. These compounds mimic the effect of the endogenous ligand, ghrelin. In the present study, we evaluated the ability of GHRP-6 to enhance the humoral immune response against co-injected antigens in mice, tilapia and African catfish...
September 8, 2017: Vaccine
https://www.readbyqxmd.com/read/28887173/adsorption-effects-of-the-doping-relevant-peptides-insulin-lispro-synachten-tb-500-and-ghrp-5
#12
Péter Judák, Peter Van Eenoo, Koen Deventer
The tendency of peptides to adsorb to surfaces can raise a concern in variety of analytical fields where the qualitative/quantitative measurement of low concentration analytes (ng/mL-pg/mL) is required. To demonstrate the importance of using the optimal glassware/plasticware, four doping relevant model peptides (GHRP 5, TB-500, Insulin Lispro, Synachten) were chosen and their recovery from various surfaces were evaluated. Our experiments showed that choosing expensive consumables with low-bind characteristics is not beneficial in all cases...
November 15, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28871578/secondary-adrenal-insufficiency-following-nivolumab-therapy-in-a-patient-with-metastatic-renal-cell-carcinoma
#13
Toshiro Seki, Atsushi Yasuda, Masayuki Oki, Natsumi Kitajima, Atsushi Takagi, Nobuyuki Nakajima, Akira Miyajima, Masafumi Fukagawa
Currently, nivolumab (an anti-programmed cell death-1 receptor monoclonal antibody) is available for many types of advanced cancers in Japan. However, there have been few detailed case reports about endocrine-related adverse events of this therapy. Here, we report a patient with metastatic renal cell carcinoma who presented with secondary adrenal insufficiency following nivolumab therapy. Endocrinological assessment by rapid adrenocorticotropic hormone (ACTH) and corticotropin-releasing hormone (CRH) tests revealed that the patient's disorder was a secondary adrenal insufficiency due to pituitary dysfunction...
September 20, 2017: Tokai Journal of Experimental and Clinical Medicine
https://www.readbyqxmd.com/read/28830317/growth-hormone-secretagogue-treatment-in-hypogonadal-men-raises-serum-insulin-like-growth-factor-1-levels
#14
John T Sigalos, Alexander W Pastuszak, Andrew Allison, Samuel J Ohlander, Amin Herati, Mark C Lindgren, Larry I Lipshultz
Realizing the reported misuse of human growth hormone (GH), investigation of a safe alternative mechanism for increasing endogenous GH is needed. Several GH secretagogues are available, including GH-releasing peptides (GHRPs) GHRP-2 and GHRP-6, and the GH-releasing hormone analog, sermorelin (SERM). Insulin-like growth factor 1 (IGF-1) serves as a surrogate marker for GH. Here, the effect of GHRP/SERM therapy on IGF-1 levels is evaluated. A retrospective review of medical records was performed for 105 men on testosterone (T) therapy seeking increases in lean body mass and fat loss who were prescribed 100 mcg of GHRP-6, GHRP-2, and SERM three times daily...
November 2017: American Journal of Men's Health
https://www.readbyqxmd.com/read/28751159/ghrelin-ameliorates-acute-lung-injury-induced-by-oleic-acid-via-inhibition-of-endoplasmic-reticulum-stress
#15
Xiuli Tian, Zhijun Liu, Ting Yu, Haitao Yang, Linlin Feng
AIMS: Acute lung injury (ALI) is associated with excessive mortality and lacks appropriate therapy. Ghrelin is a novel peptide that protects the lung against ALI. This study aimed to investigate whether endoplasmic reticulum stress (ERS) mediates the protective effect of ghrelin on ALI. MAIN METHODS: We used a rat oleic acid (OA)-induced ALI model. Pulmonary impairment was detected by hematoxylin and eosin (HE) staining, lung mechanics, wet/dry weight ratio, and arterial blood gas analysis...
July 24, 2017: Life Sciences
https://www.readbyqxmd.com/read/28750241/a-polypeptide-mediated-synthesis-of-green-fluorescent-gold-nanoclusters-for-fe-3-sensing-and-bioimaging
#16
Hua Li, Hong Huang, Jiu-Ju Feng, Xiliang Luo, Ke-Ming Fang, Zhi-Gang Wang, Ai-Jun Wang
In this paper, growth hormone releasing peptide-6 (GHRP-6) is a bioactive polypeptide and acts as the reducing agent and capping ligand for synthesis of bright green fluorescent gold nanoclusters (GHRP-6-Au NCs) by a simple and environmental-friendly aqueous method, with the assistance of NaBr as the fluorescent sensitizer. The obtained GHRP-6-Au NCs had high fluorescent quantum yield (10.7%), and the fluorescence was strongly quenched by the existence of trace Fe(3+). Thus, a new and highly sensitive sensor for the assay of Fe(3+) was constructed based on the analyte-induced fluorescent quenching mechanism...
November 15, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28623445/laparoscopic-sleeve-gastrectomy-resolves-low-ghrp-2-stimulated-growth-hormone-levels-in-obese-patients
#17
Emi Ohara, Hirotake Tokuyama, Takumi Kitamoto, Aya Kitahara, Aiko Hayashi, Hideki Hayashi, Minoru Takemoto, Koutaro Yokote
Because growth hormone (GH) secretion is reportedly decreased in obese patients, we examined not only the factors associated with the decreased GH secretion but also GH response to the GH-releasing peptide (GHRP)-2-load test before and after laparoscopic gastrectomy (LSG). The study comprised 28 individuals aged 19-65 years [mean body mass index (BMI), 39.4 ± 9.4 kg/m(2)]. In the univariate analysis, GH secretion peaks correlated negatively with BMI (r = -0.59, p = 0.001), visceral adipose tissue (r = -0...
August 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28598597/azapeptide-synthesis-methods-for-expanding-side-chain-diversity-for-biomedical-applications
#18
Ramesh Chingle, Caroline Proulx, William D Lubell
Mimicry of bioactive conformations is critical for peptide-based medicinal chemistry because such peptidomimetics may augment stability, enhance affinity, and increase specificity. Azapeptides are peptidomimetics in which the α-carbon(s) of one or more amino acid residues are substituted by nitrogen. The resulting semicarbazide analogues have been shown to reinforce β-turn conformation through the combination of lone pair-lone pair repulsion of the adjacent hydrazine nitrogen and urea planarity. Substitution of a semicarbazide for an amino amide residue in a peptide may retain biological activity and add benefits such as improved metabolic stability...
June 9, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28513740/l-ornithine-stimulates-growth-hormone-release-in-a-manner-dependent-on-the-ghrelin-system
#19
Yee Yin Ho, Junya Nakato, Takafumi Mizushige, Ryuhei Kanamoto, Mamoru Tanida, Saori Akiduki, Kousaku Ohinata
We found that intraduodenal administration of l-ornithine (l-Orn) stimulates growth hormone (GH) secretion in Wistar rats, and then investigated its mechanism. GH-releasing activity after intraduodenal administration of l-Orn was blocked by [d-Lys(3)]-GHRP-6, an antagonist of the ghrelin receptor; however, l-Orn (100 μM) has no affinity for the ghrelin receptor, suggesting that the GH-releasing activity of l-Orn is mediated via ghrelin release and activation of the ghrelin receptor. Intraduodenally administered l-Orn increased ghrelin mRNA expression in the duodenum but not in the stomach or hypothalamus...
June 1, 2017: Food & Function
https://www.readbyqxmd.com/read/28506816/ghrelin-suppresses-cholecystokinin-cck-peptide-yy-pyy-and-glucagon-like-peptide-1-glp-1-in-the-intestine-and-attenuates-the-anorectic-effects-of-cck-pyy-and-glp-1-in-goldfish-carassius-auratus
#20
Ayelén Melisa Blanco, Juan Ignacio Bertucci, Ana Isabel Valenciano, María Jesús Delgado, Suraj Unniappan
Ghrelin is an important gut-derived hormone with an appetite stimulatory role, while most of the intestinal hormones, including cholecystokinin (CCK), peptide YY (PYY) and glucagon-like peptide-1 (GLP-1), are appetite-inhibitors. Whether these important peptides with opposing roles on food intake interact to regulate energy balance in fish is currently unknown. The aim of this study was to characterize the putative crosstalk between ghrelin and CCK, PYY and GLP-1 in goldfish (Carassius auratus). We first determined the localization of CCK, PYY and GLP-1 in relation to ghrelin and its main receptor GHS-R1a (growth hormone secretagogue 1a) in the goldfish intestine by immunohistochemistry...
May 18, 2017: Hormones and Behavior
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