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https://www.readbyqxmd.com/read/27770021/in-vivo-studies-validating-multitargeting-of-prostanoid-receptors-for-achieving-superior-anti-inflammatory-effects
#1
David F Woodward, Jenny W Wang, Ming Ni, Alex Bauer, Jose L Martos, Robert W Carling, Neil J Poloso
The purpose of these studies was to test the hypothesis that a selected polypharmacological approach for treating the prostanoid-mediated component of inflammatory diseases would produce a therapeutic effect superior to global inhibition of prostaglandin (PG) biosynthesis by aspirin-like drugs. The compound studied was AGN 211377, which had been previously shown to produce a superior effect on cytokine release from human macrophages compared with cyclooxygenase (COX) inhibitors. AGN 211377 antagonizes prostanoid prostaglandin D2 (DP)1, DP2, prostaglandin E2 (EP)1, EP4, prostaglandin F2α, and thromboxane A2 receptors but not anti-inflammatory EP2, prostaglandin I2, or EP3 receptors...
October 21, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27763812/prostanoid-receptor-antagonist-effects-on-intraocular-pressure-supported-by-ocular-biodisposition-experiments
#2
David F Woodward, Stacey L Wenthur, Tara L Rudebush, Shan Fan, Carol B Toris
PURPOSE: Since all prostanoid receptors affect intraocular pressure (IOP) and endogenous prostanoids are found in ocular tissues, the pressor effects of prostanoid antagonists were comprehensively evaluated. The absence of effects of most of these antagonists was not entirely anticipated. To ensure no false-negative results, ocular biodisposition studies were conducted. METHODS: Monkeys with laser-induced ocular hypertension were used to study antagonist effects on IOP...
October 20, 2016: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27739618/stimulating-trpv1-externalization-and-synthesis-in-dorsal-root-ganglion-neurons-contributes-to-pge2-potentiation-of-trpv1-activity-and-nociceptor-sensitization
#3
W Ma, B St-Jacques, U Rudakou, Y N Kim
BACKGROUND: Persistent peripheral sensitization contributes to chronic pain. Plasticity of nociceptive dorsal root ganglion (DRG) neurons (nociceptors) induced by pro-inflammatory mediators contributes to sensitization. Prostaglandin E2 (PGE2) enriched in injured tissues is known not only directly to sensitize DRG neurons, but also to potentiate sensitizing effects of other pain mediators such as capsaicin and its receptor transient receptor potential vanilloid-1 (TRPV1). It remains unknown whether PGE2 potentiates TRPV1 activity by stimulating its synthesis, cell surface and axonal trafficking in DRG neurons...
October 14, 2016: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/27711210/signaling-of-prostaglandin-e-receptors-ep3-and-ep4-facilitates-wound-healing-and-lymphangiogenesis-with-enhanced-recruitment-of-m2-macrophages-in-mice
#4
Kanako Hosono, Risa Isonaka, Tadashi Kawakami, Shuh Narumiya, Masataka Majima
Lymphangiogenesis plays an important role in homeostasis, metabolism, and immunity, and also occurs during wound-healing. Here, we examined the roles of prostaglandin E2 (PGE2) receptor (EP) signaling in enhancement of lymphangiogenesis in wound healing processes. The hole-punch was made in the ears of male C57BL/6 mice using a metal ear punch. Healing process and lymphangiogenesis together with macrophage recruitment were analyzed in EP knockout mice. Lymphangiogenesis was up-regulated in the granulation tissues at the margins of punched-hole wounds in mouse ears, and this increase was accompanied by increased expression levels of COX-2 and microsomal prostaglandin E synthase-1...
2016: PloS One
https://www.readbyqxmd.com/read/27664754/the-ep1-ep3-receptor-agonist-17-pt-pge2-acts-as-an-ep4-receptor-agonist-on-endothelial-barrier-function-and-in-a-model-of-lps-induced-pulmonary-inflammation
#5
Theiler Anna, Konya Viktoria, Pasterk Lisa, Maric Jovana, Bärnthaler Thomas, Lanz Ilse, Platzer Wolfgang, Schuligoi Rufina, Heinemann Akos
Endothelial dysfunction is a hallmark of inflammatory conditions. We recently demonstrated that prostaglandin (PG)E2 enhances the resistance of pulmonary endothelium in vitro and counteracts lipopolysaccharide (LPS)-induced pulmonary inflammation in vivo via EP4 receptors. The aim of this study was to investigate the role of the EP1/EP3 receptor agonist 17-phenyl-trinor-(pt)-PGE2 on acute lung inflammation in a mouse model. In LPS-induced pulmonary inflammation in mice, 17-pt.-PGE2 reduced neutrophil infiltration and inhibited vascular leakage...
September 21, 2016: Vascular Pharmacology
https://www.readbyqxmd.com/read/27605391/deorphaning-the-macromolecular-targets-of-the-natural-anticancer-compound-doliculide
#6
Gisbert Schneider, Daniel Reker, Tao Chen, Kurt Hauenstein, Petra Schneider, Karl-Heinz Altmann
The cyclodepsipeptide doliculide is a marine natural product with strong actin-polymerizing and anticancer activities. Evidence for doliculide acting as a potent and subtype-selective antagonist of prostanoid E receptor 3 (EP3) is presented. Computational target prediction suggested that this membrane receptor is a likely macromolecular target and enabled immediate in vitro validation. This proof-of-concept study demonstrates the in silico deorphanization of phenotypic screening hits as a viable concept for future natural-product-inspired chemical biology and drug discovery efforts...
September 26, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27581447/periaqueductal-grey-ep3-receptors-facilitate-spinal-nociception-in-arthritic-secondary-hypersensitivity
#7
R A R Drake, J L Leith, F Almahasneh, J Martindale, A W Wilson, B Lumb, L F Donaldson
UNLABELLED: Descending controls on spinal nociceptive processing play a pivotal role in shaping the pain experience after tissue injury. Secondary hypersensitivity develops within undamaged tissue adjacent and distant to damaged sites. Spinal neuronal pools innervating regions of secondary hypersensitivity are dominated by descending facilitation that amplifies spinal inputs from unsensitized peripheral nociceptors. Cyclooxygenase-prostaglandin (PG) E2 signaling within the ventrolateral periaqueductal gray (vlPAG) is pronociceptive in naive and acutely inflamed animals, but its contributions in more prolonged inflammation and, importantly, secondary hypersensitivity remain unknown...
August 31, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27572469/rostral-ventrolateral-medulla-ep3-receptor-mediates-the-sympathoexcitatory-and-pressor-effects-of-prostaglandin-e2-in-conscious-rats
#8
Samar Rezq, Abdel A Abdel-Rahman
Whereas few studies have dealt with the central sympathoexcitatory action of the inflammatory prostanoid prostaglandin E2 (PGE2), there is no information on the expression and cardiovascular function of different PGE2 (EP) receptors in one of the major cardiovascular-regulating nuclei, the rostral ventrolateral medulla (RVLM). The current study aimed at filling this knowledge gap as well as elucidating the implicated molecular mechanisms. To achieve these goals, we showed the expression of EP2, EP3, and EP4 receptors in the RVLM and investigated their cardiovascular roles in conscious rats, ex vivo as well as in cultured PC12 cells...
November 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27512093/role-of-the-prostaglandin-e2-receptor-agonists-in-tgf-%C3%AE-1-induced-mesangial-cell-damage
#9
Pe-Ipei Xi, Yu-Yin Xu, Xiao-Lan Chen, Ya-Ping Fan, Jian-Hua Wu
PGE2 exerts its biological effect through binding to various EP receptors that result inactivation of various signal transduction pathways.It also plays an important role in mice glomerular mesangial cells (MCs) damage induced by transforming growth factor-β1 (TGF-β1); however, the molecular mechanisms remain unknown. In present study, we tested the efficacy of four selective agonists of PGE2  receptor, EP1A (17-phenyl trinor prostaglandin E 2:  ethyl amid), EP2A (butaprost), EP3A (sulprostone) and EP4A (cay10580), on mice MCs...
August 10, 2016: Bioscience Reports
https://www.readbyqxmd.com/read/27502370/prostaglandin-e2-reduces-cardiac-contractility-via-ep3-receptor
#10
Xiaosong Gu, Jiang Xu, Liping Zhu, Timothy Bryson, Xiao-Ping Yang, Edward Peterson, Pamela Harding
BACKGROUND: Prostaglandin E2 (PGE2) EP receptors EP3 and EP4 signal via decreased and increased cAMP production, respectively. Previously, we reported that cardiomyocyte-specific EP4 knockout mice develop dilated cardiomyopathy with reduced ejection fraction. Thus, we hypothesized that PGE2 increases contractility via EP4 but decreases contractility via EP3. METHODS AND RESULTS: The effects of PGE2 and the EP1/EP3 agonist sulprostone on contractility were examined in the mouse Langendorff preparation and in adult mouse cardiomyocytes...
August 2016: Circulation. Heart Failure
https://www.readbyqxmd.com/read/27484807/therapeutic-effects-of-human-gingiva-derived-mesenchymal-stromal-cells-on-murine-contact-hypersensitivity-via-prostaglandin-e2-ep3-signaling
#11
Pei Li, Yuming Zhao, Lihong Ge
BACKGROUND: The immunomodulatory and anti-inflammatory functions of human gingiva-derived mesenchymal stromal cells (GMSCs) have been demonstrated in contact hypersensitivity (CHS) models; however, their therapeutic effect during the late phase of CHS has been poor. METHODS: The murine CHS model was induced by applying oxazolone to the ears of mice. Mesenchymal stromal cells were applied via two methods (intravenous or local injection) at three time points: 1 day before sensitization, 1 day before challenge, or 1 h after challenge...
2016: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/27475644/actinidia-chinensis-planch-root-extract-acroots-inhibits-hepatocellular-carcinoma-progression-by-inhibiting-ep3-expression
#12
Tingting Fang, Jiayun Hou, Mingyan He, Lingyan Wang, Minghuan Zheng, Xiangdong Wang, Jinglin Xia
A wide range of studies has demonstrated the potent anticancer activity of Chinese herbs. Here, we evaluated the anticancer activity and molecular mechanisms of Actinidia chinensis root extract (acRoots) on hepatocellular carcinoma (HCC). HepG2 HCC cells were treated with various concentrations of acRoots for 72 h and examined by mRNA expression profiling, revealing alterations in cellular immunity, inflammation, proliferation, cell cycle, and metabolic signaling responses. Further analysis of the altered genes in cellular immunity and inflammation gene clusters identified prostaglandin E receptor 3 (EP3) as a key regulator of gene expression in response to acRoots...
July 30, 2016: Cell Biology and Toxicology
https://www.readbyqxmd.com/read/27473979/prostaglandin-e2-exerts-the-proapoptotic-and-antiproliferative-effects-on-bovine-nk-cells
#13
Tomasz Maślanka, Małgorzata Chrostowska, Iwona Otrocka-Domagała, Anna Snarska, Mateusz Mikiewicz, Monika Zuśka-Prot, Agnieszka Jasiecka, Hubert Ziółkowski, Włodzimierz Markiewicz, Jerzy J Jaroszewski
The aim of this research was to determine whether prostaglandin E2 (PGE2) affects bovine NK cells in respect of their counts, apoptosis and proliferation, and if it does, then which of the PGE2 receptor (EP) subtype(s) mediate(s) these effects. We here report that long-term, but not short-term, exposure of bovine peripheral blood mononuclear cells to PGE2 at 10(-5)M, 10(-6)M and 10(-7)M, but not at 10(-8)M, caused a significant increase in the percentage of early apoptotic cells among NK cell subset. Moreover, PGE2 at 10(-5)M and 10(-6)M, but not at 10(-7)M and 10(-8)M, induced a considerable decrease in the absolute count of NK cells...
August 2016: Research in Veterinary Science
https://www.readbyqxmd.com/read/27465993/the-ep3-receptor-regulates-water-excretion-in-response-to-high-salt-intake
#14
Shoujin Hao, AnnMarie DelliPizzi, Mariana Quiroz-Munoz, Houli Jiang, Nicholas R Ferreri
The mechanisms by which prostanoids contribute to the maintenance of whole body water homeostasis are complex and not fully understood. The present study demonstrates that an EP3-dependent feedback mechanism contributes to the regulation of water homeostasis under high-salt conditions. Rats on a normal diet and tap water were placed in metabolic cages and given either sulprostone (20 μg·kg(-1)·day(-1)) or vehicle for 3 days to activate EP3 receptors in the thick ascending limb (TAL). Treatment was continued for another 3 days in rats given either 1% NaCl in the drinking water or tap water...
October 1, 2016: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/27441774/13-effect-of-low-intensity-pulsed-ultrasound-lipus-on-remote-bone-marrow-in-rats-with-healing-socket
#15
Kouki Hidaka, Chihiro Miyamoto, Akira Kawata, Makiko Saita, Ryota Kawamata, Yojiro Maehata, Masato Minabe, Satoko W Takahashi, Shun-Suke Takahashi, Yuko Mikuni-Takagaki
OBJECTIVE: We reported at the previous annual meeting that LIPUS treatment of the molar tooth sockets of retired breeder rats accelerated alveolar bone healing, and that associated humoral effects were seen with elevated blood flow. Namely, LIPUS induced VEGF/angiogenesis along with elevated baseline blood flow rate, which was further associated with a sudden depression of blood flow rate in the socket immediately after cessation of LIPUS treatment. Prior injection with EP4 PGE2 receptor antagonist, but not EP3 antagonist, abolished this LIPUS-induced depression, and topical application of PGE2 to the socket epithelium mimicked the LIPUS-induced depression...
August 2016: Journal of Orthopaedic Trauma
https://www.readbyqxmd.com/read/27439062/c-jun-n-terminal-kinase-mediates-prostaglandin-induced-sympathoexcitation-in-rats-with-chronic-heart-failure-by-reducing-gad1-and-gabra1-expression
#16
Renjun Wang, Wen Zhang, Zengxiang Dong, Yunfeng Qi, Michael Hultström, Xiaofu Zhou, En Yin Lai
AIM: Prostaglandin E2 mediates sympathoexcitation in chronic heart failure (CHF) through EP3 receptors (PTGER3) in the paraventricular nucleus (PVN). The aim of the present study was investigate the role of c-Jun N-terminal kinase (JNK) in expressional regulation of gamma-aminobutyric acid signaling in PVN of CHF rats. METHODS: CHF was induced by left coronary ligation in wistar rats. Renal sympathetic nerve activity and mean arterial pressure responses to the PVN infusion were determined in anesthetized rats...
July 20, 2016: Acta Physiologica
https://www.readbyqxmd.com/read/27436752/prostaglandin-e2-receptor-ep3-regulates-both-adipogenesis-and-lipolysis-in-mouse-white-adipose-tissue
#17
Hu Xu, Jia-Lin Fu, Yi-Fei Miao, Chun-Jiong Wang, Qi-Fei Han, Sha Li, Shi-Zheng Huang, Sheng-Nan Du, Yu-Xiang Qiu, Ji-Chun Yang, Jan-Åke Gustafsson, Richard M Breyer, Feng Zheng, Nan-Ping Wang, Xiao-Yan Zhang, You-Fei Guan
Among the four prostaglandin E2 receptors, EP3 receptor is the one most abundantly expressed in white adipose tissue (WAT). The mouse EP3 gene gives rise to three isoforms, namely EP3α, EP3β, and EP3γ, which differ only at their C-terminal tails. To date, functions of EP3 receptor and its isoforms in WAT remain incompletely characterized. In this study, we found that the expression of all EP3 isoforms were downregulated in WAT of both db/db and high-fat diet-induced obese mice. Genetic ablation of three EP3 receptor isoforms (EP3(-/-) mice) or EP3α and EP3γ isoforms with EP3β intact (EP3β mice) led to an obese phenotype with increased food intake, decreased motor activity, reduced insulin sensitivity, and elevated serum triglycerides...
July 19, 2016: Journal of Molecular Cell Biology
https://www.readbyqxmd.com/read/27413198/inhibition-of-mitochondrial-complex-1-restores-the-downregulation-of-aquaporins-in-obstructive-nephropathy
#18
Ying Sun, Yue Zhang, Yangyang Zhu, Aihua Zhang, Songming Huang, Xiaoxing Yin, Guixia Ding, Mi Liu, Zhanjun Jia
Obstructive kidney disease is a common complication in the clinic. Downregulation of aquaporins (AQPs) in obstructed kidneys has been thought as a key factor leading to the polyuria and impairment of urine-concentrating capability after the release of kidney obstruction. The present study was to investigate the role of mitochondrial complex-1 in modulating AQPs in obstructive nephropathy. Following 7-day unilateral ureteral obstruction (UUO), AQP1, AQP2, AQP3, and V2 receptor were remarkably reduced as determined by qRT-PCR and/or Western blotting...
July 13, 2016: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/27400965/long-term-exposure-to-pge2-causes-homologous-desensitization-of-receptor-mediated-activation-of-protein-kinase-a
#19
Ramy Habashy Malty, Andy Hudmon, Jill C Fehrenbacher, Michael R Vasko
BACKGROUND: Acute exposure to prostaglandin E2 (PGE2) activates EP receptors in sensory neurons which triggers the cAMP-dependent protein kinase A (PKA) signaling cascade resulting in enhanced excitability of the neurons. With long-term exposure to PGE2, however, the activation of PKA does not appear to mediate persistent PGE2-induced sensitization. Consequently, we examined whether homologous desensitization of PGE2-mediated PKA activation occurs after long-term exposure of isolated sensory neurons to the eicosanoid...
2016: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/27375005/the-involvement-of-prostaglandin-e2-in-interleukin-1%C3%AE-evoked-anorexia-is-strain-dependent
#20
Anna Nilsson, Louise Elander, Martin Hallbeck, Unn Örtegren Kugelberg, David Engblom, Anders Blomqvist
From experiments in mice in which the prostaglandin E2 (PGE2) synthesizing enzyme mPGES-1 was genetically deleted, as well as from experiments in which PGE2 was injected directly into the brain, PGE2 has been implicated as a mediator of inflammatory induced anorexia. Here we aimed at examining which PGE2 receptor (EP1-4) that was critical for the anorexic response to peripherally injected interleukin-1β (IL-1β). However, deletion of neither EP receptor in mice, either globally (for EP1, EP2, and EP3) or selectively in the nervous system (EP4), had any effect on the IL-1β induced anorexia...
June 29, 2016: Brain, Behavior, and Immunity
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