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https://www.readbyqxmd.com/read/28887275/ffa4-gpr120-as-a-fatty-acid-sensor-involved-in-appetite-control-insulin-sensitivity-and-inflammation-regulation
#1
REVIEW
Dong-Soon Im
Unsaturated long-chain fatty acids have been suggested to be beneficial in the context of cardiovascular disorders based in epidemiologic studies conducted in Greenland and Mediterranean. DHA and EPA are omega-3 polyunsaturated fatty acids that are plentiful in fish oil, and oleic acid is an omega-9 monounsaturated fatty acid, rich in olive oil. Dietary intake of these unsaturated long-chain fatty acids have been associated with insulin sensitivity and weight loss, which contrasts with the impairment of insulin sensitivity and weight gain associated with high intakes of saturated long-chain fatty acids...
September 8, 2017: Molecular Aspects of Medicine
https://www.readbyqxmd.com/read/28871231/expression-of-the-fatty-acid-receptors-gpr84-and-gpr120-and-cytodifferentiation-of-epithelial-cells-in-the-gastric-mucosa-of-mouse-pups-in-the-course-of-dietary-transition
#2
Patricia Widmayer, Soumya Kusumakshi, Franziska A Hägele, Ulrich Boehm, Heinz Breer
During weaning, the ingested food of mouse pups changes from exclusively milk to solid food. In contrast to the protein- and carbohydrate-rich solid food, high fat milk is characterized primarily by fatty acids of medium chain length particularly important for the suckling pups. Therefore, it seems conceivable that the stomach mucosa may be specialized for detecting these important nutrients during the suckling phase. Here, we analyzed the expression of the G protein coupled receptors GPR84 and GPR120 (FFAR4), which are considered to be receptors for medium and long chain fatty acids (LCFAs), respectively...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28855632/resolution-agonist-15-epi-lipoxin-a4-programs-early-activation-of-resolving-phase-in-post-myocardial-infarction-healing
#3
Vasundhara Kain, Fei Liu, Veronika Kozlovskaya, Kevin A Ingle, Subhashini Bolisetty, Anupam Agarwal, Santosh Khedkar, Sumanth D Prabhu, Eugenia Kharlampieva, Ganesh V Halade
Following myocardial infarction (MI), overactive inflammation remodels the left ventricle (LV) leading to heart failure coinciding with reduced levels of 15-epi-Lipoxin A4 (15-epi LXA4). However, the role of 15-epi LXA4 in post-MI acute inflammatory response and resolving phase is unclear. We hypothesize that liposomal fusion of 15-epi-LXA4 (Lipo-15-epi-LXA4) or free 15-epi-LXA4 will expedite the resolving phase in post-MI inflammation. 8 to 12-week-old male C57BL/6 mice were subjected to permanent coronary artery ligation...
August 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28841192/eicosapentaenoic-acid-epa-induced-macrophages-activation-through-gpr120-mediated-raf-erk1-2-ikk%C3%AE-nf-%C3%AE%C2%BAb-p65-signaling-pathways
#4
Lirong Han, Shumin Song, Yabing Niu, Meng Meng, Chunling Wang
Objectives: To investigate the immunomodulatory effect and molecular mechanisms of Eicosapentaenoic acid (EPA, a typical kind of n-3PUFAs) on RAW264.7 cells. Methods: A variety of research methods, including the RAW264.7 cells culture, cell proliferation assays, morphologic observations, measurements of NO production, cytokine assays, nuclear protein extractions, western blot analyses and NF-κB p65 immunofluorescence assays were used in this study. Results: The results showed that EPA could increase the proliferation index and enhance the release of nitric oxide (NO) and cytokines in RAW264...
August 25, 2017: Nutrients
https://www.readbyqxmd.com/read/28835131/il-1%C3%AE-and-tnf%C3%AE-inhibit-gpr120-ffar4-and-stimulate-gpr84-ex33-and-gpr41-ffar3-fatty-acid-receptor-expression-in-human-adipocytes-implications-for-the-anti-inflammatory-action-of-n-3-fatty-acids
#5
Laura Muredda, Małgorzata A Kępczyńska, Mohamed S Zaibi, Suliman Y Alomar, Paul Trayhurn
Regulation of the expression of GPCR fatty acid receptor genes has been examined in human adipocytes differentiated in culture. TNFα and IL-1β induced a marked reduction in GPR120 expression, mRNA level falling 17-fold at 24 h in adipocytes incubated with TNFα. In contrast, GPR84 mRNA was dramatically increased by these cytokines (>500-fold for IL-1β at 4 h); GPR41 expression was also stimulated. Rosiglitazone did not affect GPR84 expression, but GPR120 and GPR41 expression increased. Dexamethasone, insulin, linoleic and docosahexaenoic acids (DHA), and TUG891 (GPR120 agonist) had little effect on GPR120 and GPR84 expression...
August 24, 2017: Archives of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28812027/l-theanine-administration-modulates-the-absorption-of-dietary-nutrients-and-expression-of-transporters-and-receptors-in-the-intestinal-mucosa-of-rats
#6
Qiongxian Yan, Haiou Tong, Shaoxun Tang, Zhiliang Tan, Xuefeng Han, Chuanshe Zhou
L-theanine has various advantageous functions for human health; whether or not it could mediate the nutrients absorption is unknown yet. The effects of L-theanine on intestinal nutrients absorption were investigated using rats ingesting L-theanine solution (0, 50, 200, and 400 mg/kg body weight) per day for two weeks. The decline of insulin secretion and glucose concentration in the serum was observed by L-theanine. Urea and high-density lipoprotein were also reduced by 50 mg/kg L-theanine. Jejunal and ileac basic amino acids transporters SLC7a1 and SLC7a9, neutral SLC1a5 and SLC16a10, and acidic SLC1a1 expression were upregulated...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28771713/epa-blocks-tnf-%C3%AE-induced-inhibition-of-sugar-uptake-in-caco-2-cells-via-gpr120-and-ampk
#7
Rosa Castilla-Madrigal, Jaione Barrenetxe, María J Moreno-Aliaga, María Pilar Lostao
The aim of the present work was to investigate in Caco-2 cells whether eicosapentaenoic acid (EPA), an omega-3 polyunsaturated fatty acid, could block the inhibitory effect of tumor necrosis factor-α (TNF-α) on sugar transport, and identify the intracellular signaling pathways involved. After pre-incubation of the Caco-2 cells with TNF-α and EPA for 1 h, EPA prevented the inhibitory effect of the cytokine on α-methyl-D-glucose (αMG) uptake (15 min) and on SGLT1 expression at the brush border membrane, measured by Western blot...
August 3, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28771600/eicosapentaenoic-acid-prevents-arterial-calcification-in-klotho-mutant-mice
#8
Kazufumi Nakamura, Daiji Miura, Yukihiro Saito, Kei Yunoki, Yasushi Koyama, Minoru Satoh, Megumi Kondo, Kazuhiro Osawa, Omer F Hatipoglu, Toru Miyoshi, Masashi Yoshida, Hiroshi Morita, Hiroshi Ito
BACKGROUND: The klotho gene was identified as an "aging-suppressor" gene that accelerates arterial calcification when disrupted. Serum and vascular klotho levels are reduced in patients with chronic kidney disease, and the reduced levels are associated with arterial calcification. Intake of eicosapentaenoic acid (EPA), an n-3 fatty acid, reduces the risk of fatal coronary artery disease. However, the effects of EPA on arterial calcification have not been fully elucidated. The aim of this study was to determine the effect of EPA on arterial calcification in klotho mutant mice...
2017: PloS One
https://www.readbyqxmd.com/read/28734639/ffa4-gpr120-pharmacology-and-therapeutic-opportunities
#9
REVIEW
Graeme Milligan, Elisa Alvarez-Curto, Brian D Hudson, Rudi Prihandoko, Andrew B Tobin
Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor (GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Although no clinical studies have yet been initiated to assess efficacy in this indication, a significant number of primary publications and patents have highlighted the ability of agonists with potency at FFA4 to improve glucose disposition and enhance insulin sensitivity in animal models...
September 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28712865/stearic-acid-suppresses-mammary-gland-development-by-inhibiting-pi3k-akt-signaling-pathway-through-gpr120-in-pubertal-mice
#10
Yingying Meng, Cong Yuan, Jing Zhang, Fenglin Zhang, Qin Fu, Xiaotong Zhu, Gang Shu, Lina Wang, Ping Gao, Qianyun Xi, Jiajie Sun, Yongliang Zhang, Qingyan Jiang, Songbo Wang
It has been demonstrated that dietary high fat diet negatively affects the pubertal mammary gland development. The aim of the present study was to investigate the effects of stearic acid (SA), an 18-carbon chain saturated fatty acid, on mammary gland development in pubertal mice and to explore the underlying mechanism. Our results demonstrated that dietary supplementation of 2% SA suppressed mammary duct development, with significant reduction of terminal end bud (TEB) number and ductal branch. In accord, the expression of proliferative marker Cyclin D1 was markedly decreased by dietary SA...
September 9, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28676689/eicosapentaenoic-acid-and-5-hepe-enhance-macrophage-mediated-treg-induction-in-mice
#11
Toshiharu Onodera, Atsunori Fukuhara, Jihoon Shin, Tomonori Hayakawa, Michio Otsuki, Iichiro Shimomura
Eicosapentaenoic acid (EPA) is an omega-3 fatty acid with immunomodulatory and anti-inflammatory effects. Beyond its direct effects, the metabolic products of EPA also regulate various immune responses. Animal experiments demonstrated that EPA reduces adipose inflammation in high fat diet-induced obese mouse. However, the effects of EPA on infiltrated immune cell populations in adipose tissue and underlying mechanisms remain to be elucidated. We performed flow cytometry of stromal vascular fraction of epididymal adipose tissues from C57BL/6J and ob/ob mice fed normal chow mixed with or without 5% EPA...
July 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28642104/design-synthesis-and-sar-of-a-novel-series-of-heterocyclic-phenylpropanoic-acids-as-gpr120-agonists
#12
Xuqing Zhang, Chaozhong Cai, Michael Winters, Michele Wells, Mark Wall, James Lanter, Zhihua Sui, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Yuanping Wang, Wen Yan, Arthur Suckow, Hong Hua, Austin Bell, Peter Haug, Wilma Clapper, Celia Jenkinson, Joseph Gunnet, James Leonard, William V Murray
A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
August 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28583918/gpr120-suppresses-adipose-tissue-lipolysis-and-synergizes-with-gpr40-in-antidiabetic-efficacy
#13
Santhosh Satapati, Ying Qian, Margaret S Wu, Aleksandr Petrov, Ge Dai, Sheng-Ping Wang, Yonghua Zhu, Xiaolan Shen, Eric S Muise, Ying Chen, Emanuel Zycband, Adam Weinglass, Jerry Di Salvo, John S Debenham, Jason M Cox, Ping Lan, Vinit Shah, Stephen F Previs, Mark Erion, David E Kelley, Liangsu Wang, Andrew D Howard, Jin Shang
GPR40 and GPR120 are fatty acid sensors that play important roles in glucose and energy homeostasis. GPR40 potentiates glucose-dependent insulin secretion and demonstrated in clinical studies robust glucose lowering in type 2 diabetes. GPR120 improves insulin sensitivity in rodents, albeit its mechanism of action is not fully understood. Here, we postulated that the antidiabetic efficacy of GPR40 could be enhanced by coactivating GPR120. A combination of GPR40 and GPR120 agonists in db/db mice, as well as a single molecule with dual agonist activities, achieved superior glycemic control compared with either monotherapy...
August 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/28503189/eicosapentaenoic-acid-shows-anti-inflammatory-effect-via-gpr120-in-3t3-l1-adipocytes-and-attenuates-adipose-tissue-inflammation-in-diet-induced-obese-mice
#14
Hodaka Yamada, Tomio Umemoto, Masafumi Kakei, Shin-Ichi Momomura, Masanobu Kawakami, San-E Ishikawa, Kazuo Hara
BACKGROUND: Saturated fatty acids have been shown to cause insulin resistance and low-grade chronic inflammation, whereas unsaturated fatty acids suppress inflammation via G-protein coupled receptor 120 (GPR120) in macrophages. However, the anti-inflammatory effects of unsaturated fatty acids in adipocytes have yet to be elucidated. Hence, the aims of the present study were to evaluate the anti-inflammatory effects of eicosapentaenoic acid (EPA) via GPR120 in adipocytes. METHODS: We used 250 μM palmitate as a representative saturated fatty acid...
2017: Nutrition & Metabolism
https://www.readbyqxmd.com/read/28495174/ppar%C3%AE-mediated-g-protein-coupled-receptor-120-signaling-pathway-promotes-transcriptional-activation-of-mir-143-in-adipocytes
#15
In-Seon Bae, Phil June Park, Jeong Hwa Lee, Eun-Gyung Cho, Tae Ryong Lee, Sang Hoon Kim
MicroRNAs (miRNAs), the small noncoding RNAs, regulate various biological processes such as adipogenesis. MicroRNA-143 (miR-143) promotes adipocyte differentiation, and is correlated with obesity in mice fed a high-fat diet. However, the transcriptional regulation of miR-143 is largely unknown. In this study, we identified that miR-143 is a target of peroxisome proliferator-activated receptor γ (PPARγ), a key transcription factor in adipogenesis. Four putative peroxisome proliferator response elements (PPREs) were identified in the miR-143 promoter region...
August 30, 2017: Gene
https://www.readbyqxmd.com/read/28455435/cd40l-dependent-pathway-is-active-at-various-stages-of-rheumatoid-arthritis-disease-progression
#16
Yanxia Guo, Alice M Walsh, Ursula Fearon, Malcolm D Smith, Mihir D Wechalekar, Xuefeng Yin, Suzanne Cole, Carl Orr, Trudy McGarry, Mary Canavan, Stephan Kelly, Tai-An Lin, Xuejun Liu, Susanna M Proudman, Douglas J Veale, Costantino Pitzalis, Sunil Nagpal
The inflammatory CD40-CD40L pathway is implicated in various autoimmune diseases, but the activity status of this pathway in various stages of rheumatoid arthritis (RA) progression is unknown. In this study, we used gene signatures of CD40L stimulation derived from human immature dendritic cells and naive B cells to assess the expression of CD40-downstream genes in synovial tissues from anti-citrullinated protein Ab-positive arthralgia, undifferentiated arthritis (UA), early RA, and established RA cohorts in comparison with healthy donors...
April 28, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28446241/polyunsaturated-fatty-acid-receptors-gpr40-and-gpr120-are-expressed-in-the-hypothalamus-and-control-energy-homeostasis-and-inflammation
#17
Nathalia R V Dragano, Carina Solon, Albina F Ramalho, Rodrigo F de Moura, Daniela S Razolli, Elisabeth Christiansen, Carlos Azevedo, Trond Ulven, Licio A Velloso
BACKGROUND: The consumption of large amounts of dietary fats is one of the most important environmental factors contributing to the development of obesity and metabolic disorders. GPR120 and GPR40 are polyunsaturated fatty acid receptors that exert a number of systemic effects that are beneficial for metabolic and inflammatory diseases. Here, we evaluate the expression and potential role of hypothalamic GPR120 and GPR40 as targets for the treatment of obesity. METHODS: Male Swiss (6-weeks old), were fed with a high fat diet (HFD, 60% of kcal from fat) for 4 weeks...
April 26, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28446062/metabolite-sensing-g-protein-coupled-receptors-facilitators-of-diet-related-immune-regulation
#18
Jian K Tan, Craig McKenzie, Eliana Mariño, Laurence Macia, Charles R Mackay
Nutrition and the gut microbiome regulate many systems, including the immune, metabolic, and nervous systems. We propose that the host responds to deficiency (or sufficiency) of dietary and bacterial metabolites in a dynamic way, to optimize responses and survival. A family of G protein-coupled receptors (GPCRs) termed the metabolite-sensing GPCRs bind to various metabolites and transmit signals that are important for proper immune and metabolic functions. Members of this family include GPR43, GPR41, GPR109A, GPR120, GPR40, GPR84, GPR35, and GPR91...
April 26, 2017: Annual Review of Immunology
https://www.readbyqxmd.com/read/28435531/discovery-of-the-first-environment-sensitive-fluorescent-probe-for-gpr120-ffa4-imaging
#19
Jiaxiang Liu, Chengsen Tian, Tianyu Jiang, Yuqi Gao, Yubin Zhou, Minyong Li, Lupei Du
GPR120, which is activated by long-chain free fatty acids (FFAs), has been recognized as a new attractive target for the treatment of type 2 diabetes and metabolic disease. The visualization and location of GPR120 in native cells can provide powerful information for guiding the physiological and pathological studies of GPR120. We report herein the first potent fluorescent probes that sensitively detect GPR120. We designed and synthesized a series of novel environment-sensitive probes with suitable fluorescence property, high biological activity on the GPR120, and acceptable cytotoxicity...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28374589/indazole-6-phenylcyclopropylcarboxylic-acids-as-selective-gpr120-agonists-with-in-vivo-efficacy
#20
William McCoull, Andrew Bailey, Peter Barton, Alan M Birch, Alastair J H Brown, Hayley S Butler, Scott Boyd, Roger J Butlin, Ben Chappell, Paul Clarkson, Shelley Collins, Robert M D Davies, Anne Ertan, Clare D Hammond, Jane L Holmes, Carol Lenaghan, Anita Midha, Pablo Morentin-Gutierrez, Jane E Moore, Piotr Raubo, Graeme Robb
GPR120 agonists have therapeutic potential for the treatment of diabetes, but few selective agonists have been reported. We identified an indazole-6-phenylcyclopropylcarboxylic acid series of GPR120 agonists and conducted SAR studies to optimize GPR120 potency. Furthermore, we identified a (S,S)-cyclopropylcarboxylic acid structural motif which gave selectivity against GPR40. Good oral exposure was obtained with some compounds displaying unexpected high CNS penetration. Increased MDCK efflux was utilized to identify compounds such as 33 with lower CNS penetration, and activity in oral glucose tolerance studies was demonstrated...
April 13, 2017: Journal of Medicinal Chemistry
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