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https://www.readbyqxmd.com/read/29785433/the-immunomodulatory-activity-and-mechanism-of-docosahexenoic-acid-dha-on-immunosuppressive-mice-models
#1
Lirong Han, Huanna Lei, Ziwei Tian, Xu Wang, Dai Cheng, Chunling Wang
In this study, the immunomodulatory activity of docosahexaenoic acid (DHA) on the immunosuppressive BALB/c mice model and its molecular mechanism are elucidated. It was found that the weight indexes of the spleen and thymus were significantly increased by DHA (44.0 mg kg-1 and 88.0 mg kg-1) treatment in the prevention or cure groups. The result of macrophages showed that DHA (44.0 mg kg-1 and 88.0 mg kg-1) could promote the proliferation and phagocytosis activity of macrophages in the prevention or cure groups...
May 22, 2018: Food & Function
https://www.readbyqxmd.com/read/29780684/a-new-insight-into-identification-of-in-silico-analysis-of-natural-compounds-targeting-gpr120
#2
Nagaraju Chinthakunta, Srinivasulu Cheemanapalli, Surekha Chinthakunta, C M Anuradha, Suresh Kumar Chitta
G-protein coupled receptor (GPR120) is an omega-3 fatty acid receptor that inhibits macrophage-induced tissue inflammation. Recent studies revealed GPR120 promotes colorectal carcinoma through modulation of VEGF, IL-8, PGE2, and NF-kB expression. However, three-dimensional structure of GPR120 is not yet available in Protein Data Bank (PDB). In the present study, we focused on a 3-D structural model of GPR120 has been constructed using homology modeling techniques. The structural quality of the predicted GPR120 model was verified using Procheck, Whatif, ProSA, and Verify 3D...
2018: Network Modeling and Analysis in Health Informatics and Bioinformatics
https://www.readbyqxmd.com/read/29777058/gpr40-is-a-low-affinity-epoxyeicosatrienoic-acid-receptor-in-vascular-cells
#3
Sang Kyu Park, Anja Herrnreiter, Sandra L Pfister, Kathryn M Gauthier, Benjamin A Falck, John R Falck, William B Campbell
Endothelium-derived epoxyeicosatrienoic acids (EETs) have numerous vascular activities mediated by G protein--coupled receptors. Long-chain free fatty acids and EETs activate GPR40, prompting us to investigate the role of GPR40 in some vascular EET activities. 14,15-EET, 11,12-EET, arachidonic acid, and the GPR40 agonist GW9508 increase intracellular calcium concentrations in human GPR40-overexpressing HEK293 cells (EC50 = 0.58 ± 0.08 μM, 0.91 ± 0.08 μM, 3.9 ± 0.06 μM and 19 ± 0.37 nM, respectively)...
May 18, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29775920/il-33-stimulates-expression-of-the-gpr84-ex33-fatty-acid-receptor-gene-and-of-cytokine-and-chemokine-genes-in-human-adipocytes
#4
Mohamed S Zaibi, Małgorzata A Kępczyńska, Parvathy Harikumar, Suliman Y Alomar, Paul Trayhurn
Expression of GPCR fatty acid sensor/receptor genes in adipocytes is modulated by inflammatory mediators, particularly IL-1β. In this study we examined whether the IL-1 gene superfamily member, IL-33, also regulates expression of the fatty acid receptor genes in adipocytes. Human fat cells, differentiated from preadipocytes, were incubated with IL-33 at three different dose levels for 3 or 24 h and mRNA measured by qPCR. Treatment with IL-33 induced a dose-dependent increase in GPR84 mRNA at 3 h, the level with the highest dose being 13...
May 15, 2018: Cytokine
https://www.readbyqxmd.com/read/29687443/the-anti-inflammatory-effect-of-10-oxo-trans-11-octadecenoic-acid-ketoc-on-raw-264-7-cells-stimulated-with-porphyromonas-gingivalis-lipopolysaccharide
#5
B Sulijaya, N Takahashi, M Yamada, M Yokoji, K Sato, Y Aoki-Nonaka, T Nakajima, S Kishino, J Ogawa, K Yamazaki
BACKGROUND: There is rapidly developing interest into the role of several anti-inflammatory agents to resolve inflammation in periodontal disease. A bioactive polyunsaturated fatty acid, 10-oxo-trans-11-octadecenoic acid (KetoC), is known to have various beneficial physiological effects; however, the effect of KetoC on inflammation remains unclear. Here, we investigated the effect of KetoC on RAW 264.7 cells stimulated with Porphyromonas gingivalis lipopolysaccharide, and explored the intracellular mechanism responsible for its anti-inflammatory effects...
April 23, 2018: Journal of Periodontal Research
https://www.readbyqxmd.com/read/29679742/adaptive-thermogenesis-by-dietary-n-3-polyunsaturated-fatty-acids-emerging-evidence-and-mechanisms
#6
REVIEW
Rong Fan, Karsten Koehler, Soonkyu Chung
Brown/beige fat plays a crucial role in maintaining energy homeostasis through non-shivering thermogenesis in response to cold temperature and excess nutrition (adaptive thermogenesis). Although numerous molecular and genetic regulators have been identified, relatively little information is available regarding thermogenic dietary molecules. Recently, a growing body of evidence suggests that high consumption of n-3 polyunsaturated fatty acids (PUFA) or activation of GPR120, a membrane receptor of n-3 PUFA, stimulate adaptive thermogenesis...
April 18, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29605534/erratum-to-discovery-of-n-arylpyrroles-as-agonists-of-gpr120-for-the-treatment-of-type-ii-diabetes-bioorg-med-chem-lett-28-2018-841-846
#7
Michael P Winters, Zhihua Sui, Mark Wall, Yuanping Wang, Joseph Gunnet, James Leonard, Hong Hua, Wen Yan, Arthur Suckow, Austin Bell, Wilmelenne Clapper, Celia Jenkinson, Peter Haug, Tatiana Koudriakova, Norman Huebert, William V Murray
No abstract text is available yet for this article.
March 28, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29570170/fatty-acid-receptor-gpr120-a-novel-marker-for-human-melanoma
#8
Johannes Kleemann, Igor Hrgovic, Jan Ter-Nedden, Pia Kleimann, Katja Steinhorst, Katja Härle, Jutta Müller, Roland Kaufmann, Markus Meissner, Stefan Kippenberger
The correlation between ultraviolet radiation of the skin and melanoma incidence in humans is well established. Interestingly, epidemiologic data suggest also a correlation to an increased BMI pointing to metabolic trigger factors in melanoma pathogenesis. To substantiate this connection, we studied the expression of G-protein-coupled receptor 120 (GPR120), a receptor sensitive to unsaturated long-chain free fatty acids in melanoma tissues. One-hundred fourteen tissue sections histologically confirmed as nevi (n=32), primary melanoma (n=39), and melanoma metastasis (n=43) were immunohistochemically stained against GPR120...
March 21, 2018: Melanoma Research
https://www.readbyqxmd.com/read/29456108/discovery-of-n-arylpyrroles-as-agonists-of-gpr120-for-the-treatment-of-type-ii-diabetes
#9
Michael P Winters, Zhihua Sui, Mark Wall, Yuanping Wang, Joseph Gunnet, James Leonard, Hong Hua, Wen Yan, Arthur Suckow, Austin Bell, Wilmelenne Clapper, Celia Jenkinson, Peter Haug, Tatiana Koudriakova, Norman Huebert, William V Murray
The discovery of a novel series of N-arylpyrroles as agonists of GPR120 (FFAR4) is discussed. One lead compound is a potent GPR120 agonist, has good selectivity for related receptor GPR40 (FFAR1), has acceptable PK properties, and is active in 2 models of Type 2 Diabetes in mice.
March 1, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29449902/sers-fluorescence-bimodal-nanoprobes-for-in-vitro-imaging-of-fatty-acid-responsive-receptor-gpr120
#10
Lifu Xiao, Abdul K Parchur, Timothy A Gilbertson, Anhong Zhou
G-protein-coupled receptor 120 (GPR120), as a member of the rhodopsin family of G-protein-coupled receptors, has been shown to function as a sensor for dietary fat in the gustatory and digestive systems. Its specific role in the chemoreception of fatty acids, which is thought to be crucial in understanding the mechanism surrounding the control of fat intake and, accordingly, in the treatment of obesity, remains unclear. Here we report a novel surface-enhanced Raman spectroscopy (SERS)-fluorescence bimodal microscopic technique for detection and imaging of GPR120 in single living cells...
2018: Analytical Methods: Advancing Methods and Applications
https://www.readbyqxmd.com/read/29373685/phytosphingosine-is-a-novel-activator-of-gpr120
#11
Tomotaka Nagasawa, Hikaru Nakamichi, Yoichiro Hama, Shigeki Higashiyama, Yasuyuki Igarashi, Susumu Mitsutake
GPR120 is a receptor for long chain fatty acids and is expressed in small intestinal endocrine cells, L cells and adipose tissue. Activation of GPR120 promotes the secretion of incretin GLP-1, which is known to have effects on anti-metabolic syndrome. As such, GPR120 is a potential target of pharmaceuticals for type II diabetes. In this study, we performed ligand-screening for GPR120 on glycero- and sphingo-type lipids and their derivatives using a TGFα-shedding assay. We found that phytosphingosine (PHS) activates GPR120 in a manner comparable to the natural ligand α-linolenic acid (ALA) and superior to that of the synthetic ligand GW9508...
January 24, 2018: Journal of Biochemistry
https://www.readbyqxmd.com/read/29343498/the-gpr120-agonist-tug-891-promotes-metabolic-health-by-stimulating-mitochondrial-respiration-in-brown-fat
#12
Maaike Schilperoort, Andrea D van Dam, Geerte Hoeke, Irina G Shabalina, Anthony Okolo, Aylin C Hanyaloglu, Lea H Dib, Isabel M Mol, Natarin Caengprasath, Yi-Wah Chan, Sami Damak, Anne Reifel Miller, Tamer Coskun, Bharat Shimpukade, Trond Ulven, Sander Kooijman, Patrick Cn Rensen, Mark Christian
Brown adipose tissue (BAT) activation stimulates energy expenditure in human adults, which makes it an attractive target to combat obesity and related disorders. Recent studies demonstrated a role for G protein-coupled receptor 120 (GPR120) in BAT thermogenesis. Here, we investigated the therapeutic potential of GPR120 agonism and addressed GPR120-mediated signaling in BAT We found that activation of GPR120 by the selective agonist TUG-891 acutely increases fat oxidation and reduces body weight and fat mass in C57Bl/6J mice...
January 17, 2018: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/29343310/effect-of-dietary-fish-oil-on-selected-inflammatory-markers-in-pigs
#13
T Komprda, P Ondráčková, M Vícenová, V Rozíková, N Procházková, L Levá, M Faldyna
The present study tested a hypothesis that dietary fish oil (eicosapentaenoic acid+docosahexaenoic acid) in a commonly achievable dose ameliorates a systemic inflammation in pigs. Two groups of pigs of 16 animals each were fed a diet with either 2.5% of fish oil (F) or a control diet with 2.5% of palm oil (P). After 70 days of fattening, eight F and eight P pigs were challenged (F+; P+) i.v. by lipopolysaccharide. After 3 h, all pigs were sacrificed and blood, liver and visceral adipose tissue (VAT) samples were taken...
January 18, 2018: Animal: An International Journal of Animal Bioscience
https://www.readbyqxmd.com/read/29312596/ra-and-%C3%AF-3-pufa-co-treatment-activates-autophagy-in-cancer-cells
#14
Shenglong Zhu, Guangxiao Lin, Ci Song, Yikuan Wu, Ninghan Feng, Wei Chen, Zhao He, Yong Q Chen
Retinoic acid (RA), is a promising therapeutic agent for the treatment of breast cancer. However, metabolic disorders and drug resistance reduce the efficacy of RA. In this study, we found that RA and ω-3 polyunsaturated fatty acids (ω-3 PUFAs) synergistically induced cell death in vitro and in vivo and autophagy activation. Moreover, RA-induced hypercholesterolemia was completely corrected by ω-3 PUFA supplementation. In addition, we demonstrated that the effects of this combination on the autophagic flux were independent of the two major canonic regulatory complexes controlling autophagic vesicle formation...
December 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29221950/dha-supplementation-prevent-the-progression-of-nash-via-gpr120-signaling
#15
Kazuo Nakamoto, Koki Shimada, Shinichi Harada, Yasuko Morimoto, Akira Hirasawa, Shogo Tokuyama
Nonalcoholic steatohepatitis (NASH) is one of the most common liver diseases involving chronic accumulation of fat and inflammation, often leading to advanced fibrosis, cirrhosis and carcinoma. However, the pathological mechanism for this is unknown. GPR120/FFAR4 has been recognized as a functional fatty acid receptor and an attractive therapeutic target for metabolic diseases. In this study, we investigated the involvement of GPR120/FFAR4 in the pathogenesis of NASH. Mice fed with a 0.1% methionine and choline deficient high-fat (CDAHF) diet showed a significant increase in plasma aspartate transaminase and alanine transaminase levels, fatty deposition, inflammatory cell infiltration, and mild fibrosis...
February 5, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29206860/the-acute-glucose-lowering-effect-of-specific-gpr120-activation-in-mice-is-mainly-driven-by-glucagon-like-peptide-1
#16
Linda Sundström, Susanna Myhre, Monika Sundqvist, Andrea Ahnmark, William McCoull, Piotr Raubo, Sam D Groombridge, Magnus Polla, Ann-Christin Nyström, Lisbeth Kristensson, Mats Någård, Maria Sörhede Winzell
The mechanism behind the glucose lowering effect occurring after specific activation of GPR120 is not completely understood. In this study, a potent and selective GPR120 agonist was developed and its pharmacological properties were compared with the previously described GPR120 agonist Metabolex-36. Effects of both compounds on signaling pathways and GLP-1 secretion were investigated in vitro. The acute glucose lowering effect was studied in lean wild-type and GPR120 null mice following oral or intravenous glucose tolerance tests...
2017: PloS One
https://www.readbyqxmd.com/read/29176006/gpr120-mechanism-of-action-role-and-potential-for-medical-applications
#17
REVIEW
Hanna Karakuła-Juchnowicz, Joanna Róg, Dariusz Juchnowicz, Justyna Morylowska-Topolska
G protein-coupled receptors (GPCRs) constitute a family of transmembrane proteins that mediate many cellular processes. GPR120/FFAR4, a receptor from this family that is activated by fatty acids, has received considerable attention recently. This paper presents a literature review concerning the role of GPR120 and its mechanism of action in animal and human studies as well as the potential use of GPR120 for the treatment of chronic diseases. Two electronic databases - Medline and Google Scholar - were searched for available studies addressing the review topic that were written in English and published from 2000 to June 2017...
November 19, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/29175142/flaxseed-oil-rich-in-omega-3-protects-aorta-against-inflammation-and-endoplasmic-reticulum-stress-partially-mediated-by-gpr120-receptor-in-obese-diabetic-and-dyslipidemic-mice-models
#18
Alexandre Moura-Assis, Milessa Silva Afonso, Vanessa de Oliveira, Joseane Morari, Gustavo Aparecido Dos Santos, Marcia Koike, Ana Maria Lottenberg, Rodrigo Ramos Catharino, Licio Augusto Velloso, Adelino Sanchez Ramos da Silva, L P de Moura, Eduardo Rochete Ropelle, José Rodrigo Pauli, Dennys Esper Corrêa Cintra
The "first hit" to atherogenesis is driven by toll-like receptor 4, endoplasmic reticulum stress and ultimately metabolic dysfunction. In this study, we hypothesized that a flaxseed oil-enriched diet (FS) abolishes these inflammatory signaling pathway and restore metabolic homeostasis by activating the fatty acid receptor GPR120 in aorta of obese mice. Glucose homeostasis was assessed by GTT and ITT; lipidomics was performed using a Hybrid Ion Trap-Orbitrap Mass Spectrometer; serum lipids were measured using colorimetric assays; GPR120 and infiltrating macrophages were analyzed by immunofluorescence; protein immunoprecipitation and gene expression were evaluated by Western blot and RT-PCR, respectively...
March 2018: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/29126901/omega-3-polyunsaturated-fatty-acids-protect-human-hepatoma-cells-from-developing-steatosis-through-ffa4-gpr120
#19
Saeromi Kang, Jin Huang, Bo-Kyung Lee, Young-Suk Jung, Eunok Im, Jung-Min Koh, Dong-Soon Im
Protective effect of omega-3 polyunsaturated fatty acids (n-3 PUFA) on non-alcoholic fatty liver disease has been demonstrated. FFA4 (also known as GPR120; a G protein-coupled receptor) has been suggested to be a target of n-3 PUFA. FFA4 expression in hepatocytes has also been reported from liver biopsies in child fatty liver patients. In order to assess the functional role of FFA4 in hepatic steatosis, we used an in vitro model of liver X receptor (LXR)-mediated hepatocellular steatosis. FFA4 expression was confirmed in Hep3B and HepG2 human hepatoma cells...
February 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29113108/polymorphisms-in-ffar4-gpr120-gene-modulate-insulin-levels-and-sensitivity-after-fish-oil-supplementation
#20
Bastien Vallée Marcotte, Hubert Cormier, Iwona Rudkowska, Simone Lemieux, Patrick Couture, Marie-Claude Vohl
The objective was to test whether FFAR4 single nucleotide polymorphisms (SNPs) are associated with glycemic control-related traits in humans following fish oil supplementation. A total of 210 participants were given 3 g/day of omega-3 (n-3) fatty acids (FA) (1.9-2.2 g of eicosapentaenoic acid (EPA) and 1.1 g of docosahexaenoic acid (DHA)) during six weeks. Biochemical parameters were taken before and after the supplementation. Using the HapMap database and the tagger procedure in Haploview, 12 tagging SNPs in FFAR4 were selected and then genotyped using TaqMan technology...
November 6, 2017: Journal of Personalized Medicine
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