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Jinqiang Zhang, Mukandila Mulumba, Huy Ong, William D Lubell
Macrocyclization has enabled the use of peptides in drug discovery creating a need for methods to synthesize diverse peptide macrocycles. Azapeptides have advanced to clinically used drugs, however, few cyclic azapeptides have been studied. A multiple component "A(3) -macrocyclization" strategy is described for the preparation of diverse cyclic azapeptides and is demonstrated by the synthesis of 15 growth hormone releasing hormone-6 (GHRP-6) analogs. Certain cyclic aza-GHRP-6 analogs exhibited unprecedented affinity for the CD36 receptor, and capacity to modulate Toll-like receptor agonist-induced overproduction of nitric oxide, and reduce pro-inflammatory cytokine and chemokine production in macrophages...
January 16, 2017: Angewandte Chemie
Ayelén Melisa Blanco, Juan Ignacio Bertucci, Aída Sánchez-Bretaño, María Jesús Delgado, Ana Isabel Valenciano, Suraj Unniappan
Ghrelin, a multifunctional gut-brain hormone, is involved in the regulation of gastric functions in mammals. This study aimed to determine whether ghrelin modulates digestive enzymes in goldfish (Carassius auratus). Immunofluorescence microscopy found colocalization of ghrelin, GHS-R1a and the digestive enzymes sucrase-isomaltase, aminopeptidase A, trypsin and lipoprotein lipase in intestinal and hepatopancreatic cells. In vitro ghrelin treatment in intestinal and hepatopancreas explant culture led to a concentration- and time-dependent modulation (mainly stimulatory) of most of the digestive enzymes tested...
February 15, 2017: Molecular and Cellular Endocrinology
Zhijun Liu, Ting Yu, Haitao Yang, Xiuli Tian, 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 the role of endogenous ghrelin in the pathogenesis of 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. Plasma and lung content of ghrelin was examined by ELISA, and mRNA expression of ghrelin was measured by quantitative real-time PCR...
November 25, 2016: Life Sciences
N Subirós, H Pérez-Saad, L Aldana, C L Gibson, W S Borgnakke, D Garcia-Del-Barco
BACKGROUND: Combined therapy with epidermal growth factor (EGF) and growth hormone-releasing peptide 6 (GHRP-6) in stroke models has accumulated evidence of neuroprotective effects from several studies, but needs further support before clinical translation. Comparing EGF + GHRP-6 to hypothermia, a gold neuroprotection standard, may contribute to this purpose. OBJECTIVES: The aims of this study were to compare the neuroprotective effects of a combined therapy based on EGF + GHRP-6 with hypothermia in animal models of (a) global ischemia representing myocardial infarction and (b) focal brain ischemia representing ischemic stroke...
November 2016: Neurological Research
Alina Theisen, Bin Yan, Jeffery M Brown, Michael Morris, Bruno Bellina, Perdita E Barran
We demonstrate the capabilities of a laser-coupled ion mobility mass spectrometer for analysis of peptide sequence and structure showing ultraviolet photodissociation (UVPD) spectra of mass and mobility selected ions. A Synapt G2-S mass spectrometer has been modified to allow photointeraction of ions post the mobility cell. For this work, we have employed a single wavelength laser, which irradiates at 266 nm. We present the unique capabilities of this instrument and demonstrate several key features. Irradiation of luteinizing hormone releasing hormone (LHRH), growth hormone releasing hexapeptide (GHRP-6), and TrpCage (sequence NLYIQWLKDGGPSSGRPPPS) yields extensive b- and y-type fragmentation as well as a- and c-type ions...
October 3, 2016: Analytical Chemistry
Si-Liang Wen, Xian Feng, Zhi-Qiang Chen, Jing Xiao, Wei-Xuan Zhang
OBJECTIVES: We conducted a prospective clinical randomized single-blind placebo-controlled trial (ChiCTR-TRC-14004156) to observe the effect of XiangBin granules on the recovery of gastrointestinal function and levels of brain-gut peptide motilin (MTL); vasoactive intestinal peptide (VIP); growth hormone releasing peptide-ghrelin, GHRP-ghrelin, and corticotropin releasing hormone (CRH), after transabdominal gynecological surgery. STUDY DESIGN: Patients undergoing gynecologic abdominal surgery were randomly divided in a 2:1 ratio (according to the data of pre-trial which was a small sample randomized trial in gynecology inpatient) into two groups: the larger treatment group taking XiangBin granules, and the smaller placebo group taking Chinese herbal placebo...
October 2016: European Journal of Obstetrics, Gynecology, and Reproductive Biology
Yi-Ning Chao, David Sun, Yen-Chun Peng, Yuh-Lin Wu
Cyclooxygenase-2 (COX-2) and interleukin-8 (IL-8) are two important inflammatory mediators in ovulation. Ghrelin may modulate inflammatory signaling via growth hormone secretagogue receptors. We investigated the role of ghrelin in KGN human ovarian granulosa cells using protein kinase C (PKC) activator phorbol 12, 13-didecanoate (PDD) and synthetic ghrelin analog growth hormone releasing peptide-2 (GHRP-2). GHRP-2 attenuated PDD-induced expression of protein and mRNA, the promoter activity of COX-2 and IL-8 genes, and the secretion of prostaglandin E2 (PGE₂) and IL-8...
August 19, 2016: International Journal of Molecular Sciences
Sheng-Kuo Hsieh, Tse-Yu Chung, Yue-Chiun Li, Yuan-Hao Lo, Nan-Hei Lin, Ping-Chung Kuo, Wen-Ying Chen, Jason T C Tzen
ETHNOPHARMACOLOGICAL RELEVANCE: Folium Ginkgo, the dried leaf of Ginkgo biloba L. is a traditional Chinese medicine listed in the Pharmacopoeia of the People's Republic of China with several therapeutic effects, including prevention of aging. It is used as herbal medicine for the treatment of several aging-related diseases. The therapeutic effects of Folium Ginkgo on aging-related diseases are suspected to be similar to the anti-aging effects of growth hormone release induced by ghrelin...
December 4, 2016: Journal of Ethnopharmacology
Yodi Mahendradhata, Jamila Nabieva, Riris Andono Ahmad, Patricia Henley, Pascal Launois, Corinne Merle, Christine Maure, Olaf Horstick, Varalakshmi Elango
BACKGROUND: Good clinical practice (GCP) guidelines have been the source of improvement in the quality of clinical trials; however, there are limitations to the application of GCP in the conduct of health research beyond industry-sponsored clinical trials. The UNICEF/UNDP/World Bank/WHO Special Program for Research and Training in Tropical Disease is promoting good practice in all health research involving human through the Good Health Research Practice (GHRP) training program initiative...
2016: Global Health Action
Fu-Yan Liu, Min-Min Zhang, Ping Zeng, Wen-Wen Liu, Jing-Lei Wang, Bei Yang, Qun Dai, Jie Wei
Ghrelin has been identified as the endogenous ligand for the GHS-R1α (growth hormone secretagogue receptor 1 alpha). Our previous experiments have indicated that ghrelin (i.c.v.) induces antinociceptive effects in acute pain in mice, and the effects were mediated through the central opioid receptors and GHS-R1α. However, which opioid receptor (OR) mediates the antinociceptive effects and the molecular mechanisms are also needed to be further explored. In the present study, the antinociceptive effects of ghrelin (i...
September 2016: Peptides
Cong Liu, Jiawei Huang, Hong Li, Zhangyou Yang, Yiping Zeng, Jing Liu, Yuhui Hao, Rong Li
The therapeutic effect of ghrelin on wound healing was assessed using a rat model of combined radiation and burn injury (CRBI). Rat ghrelin, anti-rat tumor necrosis factor (TNF) α polyclonal antibody (PcAb), or selective antagonists of p38 mitogen-activated protein kinase (MAPK), c-Jun N-terminal kinase (JNK), and growth hormone secretagogue receptor (GHS-R) 1a (SB203580, SP600125, and [D-Lys3]-GHRP-6, respectively), were administered for seven consecutive days. Levels of various signaling molecules were assessed in isolated rat peritoneal macrophages...
2016: Scientific Reports
Yssel Mendoza Marí, Maday Fernández Mayola, Ana Aguilera Barreto, Ariana García Ojalvo, Yilian Bermúdez Alvarez, Ana Janet Mir Benítez, Jorge Berlanga Acosta
In addition to its cytoprotective effects, growth hormone-releasing peptide 6 (GHRP-6) proved to reduce liver fibrotic induration. CD36 as one of the GHRP-6 receptors appears abundantly represented in cutaneous wounds granulation tissue. The healing response in a scenario of CD36 agonistic stimulation had not been previously investigated. Excisional full-thickness wounds (6 mmØ) were created in the dorsum of Wistar rats and topically treated twice a day for 5 days. The universal model of rabbit's ears hypertrophic scars was implemented and the animals were treated daily for 30 days...
2016: Plastic Surgery International
Farrin Babaei-Balderlou, Homayoun Khazali
BACKGROUND: The hormones of hypothalamo-pituitary-gonadal (HPG) axis have facilitative effects on reproductive behavior in mammals. Ghrelin as a starvation hormone has an inhibitory effect on HPG axis' function. Hence, it is postulated that ghrelin may reduce the sexual behavior through inhibiting of HPG axis. The aim of this study was to examine the effects of ghrelin and its antagonist, [D-Lys(3) ]-GHRP-6, on sexual behavior and LH beta-subunit gene expression in male rats. METHODS: In this experimental study, 128 male Wistar rats were divided into two groups...
April 2016: Journal of Reproduction & Infertility
Zhao-Xing Shen, Qian Xiao, Yu-Xing Zhao, Ke-Xiang Zhao
OBJECTIVE: To explore the effects of ghrelin on learning and memory abilities and expressions of DKK-1 and β-catenin in the hippocampus of diabetic rats. METHODS: Sixty male SD rats were randomly assigned into 4 groups, namely the control group, diabetic group, ghrelin-treated diabetic group (DM1 group), and ghrelin- and D-lys3-GHRP-6 (a GHSR-1a receptor antagonist)-treated diabetic group (DM2 group). Diabetic rat models were established by a single intraperitoneal injection of streptozotocin (65 mg/kg)...
April 2016: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
Emma T Brockway, Katherine R Krater, Joaquín A Selva, Shelby E R Wauson, Paul J Currie
Ghrelin administration directly into hypothalamic nuclei, including the arcuate nucleus (ArcN) and the paraventricular nucleus (PVN), alters the expression of stress-related behaviors. In the present study we investigated the effect of feeding status on the ability of ghrelin to induce stress and anxiogenesis. Adult male Sprague Dawley rats were implanted with guide cannula targeting either the ArcN or PVN. In the first experiment we confirmed that ArcN and PVN ghrelin treatment produced anxiety-like behavior as measured using the elevated plus maze (EPM) paradigm...
2016: Peptides
Hiroshi Arimura, Hiroshi Hashiguchi, Kiyoaki Yamamoto, Atsushi Shinnakasu, Aiko Arimura, Akira Kikuchi, Takahisa Deguchi, Mika Habu, Singo Fujio, Kazunori Arita, Yoshihiko Nishio
The aim of this study was to evaluate the ability of the growth hormone-releasing peptide-2 (GHRP-2) test to clinically diagnose hypothalamo-pituitary-adrenal (HPA) axis failure. We performed an insulin tolerance test (ITT), CRH stimulation test, and GHRP-2 test on 47 patients suspected of having a hypothalamo-pituitary disorder. Patients with pituitary disorders had significantly lower ACTH responses to the GHRP-2 test compared to patients with hypothalamic disorders and the control group. In contrast, peak cortisol levels in response to the GHRP-2 test were significantly lower in both hypothalamic and pituitary disorder cases compared with the control group...
June 30, 2016: Endocrine Journal
Yan-Juan Yu, Jing Dong, Zheng-Yao Jiang, Inge Depoortere
The present study was aimed to explore the effects of intraperitoneal injection of growth hormone releasing peptide-6 (GHRP-6), a ghrelin receptor agonist, on food intake and neuronal activity of feeding-related nuclei in the hypothalamus of NMRI mice. Accumulated amount of food intake was measured, and total number of c-fos immunoreactive neurons in arcuate nucleus (ARC), paraventricular nucleus (PVN) and supraoptic nucleus (SON) was counted by immunohistochemistry at 1, 3 and 6 h after the GHRP-6 injection...
February 25, 2016: Sheng Li Xue Bao: [Acta Physiologica Sinica]
Rui Hu, Zhisheng Wang, Quanhui Peng, Huawei Zou, Hongze Wang, Xiaoqiang Yu, Xiaoping Jing, Yixin Wang, Binghai Cao, Shanke Bao, Wenhua Zhang, Suonan Zhao, Hanzhong Ji, Xiangying Kong, Quanxi Niu
UNLABELLED: The objective of this study was to investigate the effects of growth hormone-releasing peptide-2 (GHRP-2) and cysteamine (CS) administration on growth performance in yaks with growth retardation and try to elucidate its regulatory mechanisms. Trial 1, thirty-six 1-year-old Qinghai high plateau yaks (body weight 38-83.2 kg) were randomly chosen for body weight and jugular blood samples collection. The relationship between body weight and serum GHRH (P < 0.05, R = 0.45), GH (P < 0...
2016: PloS One
Gi-Shih Lien, Chien-Huang Lin, You-Lan Yang, Ming-Shun Wu, Bing-Chang Chen
Colon cancer is the third most common malignancy worldwide. Recently, some interesting associations between ghrelin and cancer were reported, and it may participate in colon cancer development. In the present report, we explored the role of the growth hormone secretagogue receptor (GHS-R), Ras, phosphatidylinositol 3-kinase (PI3K), Akt, and mammalian target of rapamycin (mTOR) pathways in the ghrelin-induced proliferation of human colon cancer cells. Ghrelin-caused HT-29 proliferation was reduced by [D-Lys3]-GHRP-6 (a GHS-R inhibitor)...
April 5, 2016: European Journal of Pharmacology
Sunan Li, Juxiong Liu, Qingkang Lv, Chuan Zhang, Shiyao Xu, Dongxue Yang, Bingxu Huang, Yalong Zeng, Yingjie Gao, Wei Wang
The ghrelin peptides were found to circulate in two major forms: acylated ghrelin (AG) and unacylated ghrelin (UAG). Previous studies showed that AG regulates β-casein (CSN2) expression in mammary epithelial cells. However, little is known about the mechanisms by which AG regulates CSN2 gene and protein expression. Evidence suggests that UAG has biological activity through GHSR1a-independent mechanisms. Here, we investigated the possible GHSR1a-mediated effect of UAG on the expression of CSN2 in primary bovine mammary epithelial cells (pbMECs) isolated from lactating cow...
April 2016: Journal of Molecular Endocrinology
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