Studies have shown that ghrelin played direct actions in ovarian function, but the direct role of ghrelin in corpus luteum (CL) of pregnant sows has remained obscure. The study aimed to examine the expressions of ghrelin and its functional receptor (GHSR-1a) in the CL of sows during pregnancy, and evaluate the role of ghrelin in CL function of pregnant sows. Immunohistochemistry analysis showed that ghrelin and GHSR-1a are both predominantly localized in the luteal cells of pregnant sows CL. Strong immunoreactivity for ghrelin and GHSR-1a is detected at days 20 (early) and 50 (middle), but weak immunoreactivity is observed at days 90 (late) post mating. Similarly, there is a significant effect of pregnant phase on the expression (mRNA and protein) of ghrelin and GHSR-1a in the CL, with higher levels at days 20 (early) and 50 (middle), and lower values at 90 (late) post mating. In vitro, treatments of luteal cells with ghrelin (from 0.01 to 10 ng/mL) are promoted cell viability and P4 secretion in a dose-dependent manner. Ghrelin is also accelerated the LH-induced P4 secretion in luteal cells. Moreover, ghrelin is induced the release and mRNA expression of LH, and increased the release of prostaglandin (PG)E, but reduced the secretion of PGF in luteal cells. In conclusion, the presences of ghrelin and GHSR-1a in the porcine CL during pregnancy, and the stimulatory effect of ghrelin on luteal cells suggest positive regulation by ghrelin in CL function of pregnant sows.
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http://dx.doi.org/10.1016/j.domaniend.2022.106763 | DOI Listing |
J Ethnopharmacol
January 2025
Graduate Institute of Biotechnology, National Chung-Hsing University, Taichung, 402, Taiwan. Electronic address:
Ethnopharmacological Relevance: The dried fruit of Ligustrum lucidum Ait. (FLL), known as Nuzhenzi, is traditionally recognized for its anti-aging properties in Chinese medicine. Nuezhenide, a water-soluble secoiridoid present in FLL, has demonstrated various pharmacological activities including neuroprotection, enhancement of learning and memory, antiosteoporotic, and antiviral activities.
View Article and Find Full Text PDFVet Res Commun
February 2024
Laboratory Animal Facility, CSIR-Central Drug Research Institute, Lucknow, India.
Growth hormone and insulin like growth factor-1 plays an important role in the regulation of body composition and metabolism. Growth Hormone is released from the pituitary through a specific G-protein coupled receptor (GPCR) called growth hormone secretagogue receptor 1a expressed in the hypothalamus. Ghrelin is a peptide hormone released from the cells in the stomach, which stimulates appetite and food intake in mammals, regulates gut motility, gastric acid secretion, taste sensation, circadian rhythm, learning and memory, oxidative stress, autophagy, glucose metabolism etc.
View Article and Find Full Text PDFJ Pharmacol Exp Ther
August 2023
Clinical Psychoneuroendocrinology and Neuropsychopharmacology Section, Translational Addiction Medicine Branch, National Institute on Drug Abuse Intramural Research Program and National Institute on Alcohol Abuse and Alcoholism Division of Intramural Clinical and Biological Research, National Institutes of Health, Baltimore and Bethesda, Maryland (S.L.D., C.L.P., M.F., L.L.); Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan (S.L.D.); Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark (M.A.H., B.H.); Neurobiology of Addiction Section, Integrative Neuroscience Research Branch, National Institute on Drug Abuse (C.L.P., G.F.K., L.F.V.) and Medication Development Program, National Institute on Drug Abuse Intramural Research Program (A.S., K.C.R., L.L.), National Institutes of Health, Baltimore, Maryland; Department of Mental Health, Johns Hopkins Bloomberg School of Public Health (M.F.) and Division of Addiction Medicine, Department of Medicine, School of Medicine (L.L.), Johns Hopkins University, Baltimore, Maryland; Department of Chemistry (J.E.M., J.L.H.), Department of Biology (J.L.H.), and BioInspired Syracuse (J.L.H.), Syracuse University, Syracuse, New York; Pfizer Inc. Medicine Design, Groton, Connecticut (I.A.S.); Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island (S.A., F.A.); Drug Design and Synthesis Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland (A.S., K.C.R.); and Center for Alcohol Addiction Studies, Department of Behavioral and Social Sciences, School of Public Health, Brown University, Providence, Rhode Island (L.L.)
Preclinical and clinical studies have identified the ghrelin receptor [growth hormone secretagogue receptor (GHSR)1a] as a potential target for treating alcohol use disorder. A recent phase 1a clinical trial of a GHSR1a antagonist/inverse agonist, PF-5190457, in individuals with heavy alcohol drinking identified a previously undetected major hydroxy metabolite of PF-5190457, namely PF-6870961. Here, we further characterized PF-6870961 by screening for off-target interactions in a high-throughput screen and determined its in vitro pharmacodynamic profile at GHSR1a through binding and concentration-response assays.
View Article and Find Full Text PDFTrends Endocrinol Metab
February 2023
Department of Cell Biology, Duke University, Durham, NC 27710, USA.
As allosteric complexes, G-protein-coupled receptors (GPCRs) respond to extracellular stimuli and pleiotropically couple to intracellular transducers to elicit signaling pathway-dependent effects in a process known as biased signaling or functional selectivity. One such GPCR, the ghrelin receptor (GHSR), has a crucial role in restoring and maintaining metabolic homeostasis during disrupted energy balance. Thus, pharmacological modulation of GHSR bias could offer a promising strategy to treat several metabolism-based disorders.
View Article and Find Full Text PDFDomest Anim Endocrinol
January 2023
College of Veterinary Medicine, Northwest A and F University, Yangling, Shaanxi 712100, P.R. China. Electronic address:
Studies have shown that ghrelin played direct actions in ovarian function, but the direct role of ghrelin in corpus luteum (CL) of pregnant sows has remained obscure. The study aimed to examine the expressions of ghrelin and its functional receptor (GHSR-1a) in the CL of sows during pregnancy, and evaluate the role of ghrelin in CL function of pregnant sows. Immunohistochemistry analysis showed that ghrelin and GHSR-1a are both predominantly localized in the luteal cells of pregnant sows CL.
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