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https://www.readbyqxmd.com/read/29126901/omega-3-polyunsaturated-fatty-acids-protect-human-hepatoma-cells-from-developing-steatosis-through-ffa4-gpr120
#1
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...
November 7, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29113108/polymorphisms-in-ffar4-gpr120-gene-modulate-insulin-levels-and-sensitivity-after-fish-oil-supplementation
#2
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
https://www.readbyqxmd.com/read/29080746/oral-lipase-activities-and-fat-taste-receptors-for-fat-taste-sensing-in-chickens
#3
Yuko Kawabata, Fuminori Kawabata, Shotaro Nishimura, Shoji Tabata
It has been reported that a functional fat-taste receptor, GPR120, is present in chicken oral tissues, and that chickens can detect fat taste in a behavioral test. However, although triglycerides need to be digested to free fatty acids to be recognized by fat-taste receptors such as GPR120, it remains unknown whether lipase activities exist in chicken oral tissues. To examine this question, we first cloned another fat-taste receptor candidate gene, CD36, from the chicken palate. Then, using RT-PCR, we determined that GPR120 and CD36 were broadly expressed in chicken oral and gastrointestinal tissues...
October 25, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28980737/gpr120-is-not-required-for-%C3%AF-3-pufas-induced-cell-growth-inhibition-and-apoptosis-in-breast-cancer-cells
#4
Shenglong Zhu, Xiaowei Jiang, Siyuan Jiang, Guangxiao Lin, Jianping Gong, Wei Chen, Zhao He, Yong Q Chen
Intake of ω-3 PUFAs reduces the frequency of breast cancer, and GPR120 receptor transduces ω-3 PUFAs signaling to increase insulin sensitivity in mice, but whether GPR120 mediates ω-3 PUFAs signaling to inhibit breast carcinogenesis is currently unknown. In the present study, we found that GPR120 is highly expressed in human breast cancerous tissues but not adjacent normal tissue. Knockdown of GPR120 by siRNA in breast cancer cells significantly reduced cell growth, and dramatically increased ω-3 FFA-induced cell growth inhibition and apoptosis...
October 5, 2017: Cell Biology International
https://www.readbyqxmd.com/read/28947942/discovery-of-an-isothiazole-based-phenylpropanoic-acid-gpr120-agonist-as-a-development-candidate-for-type-2-diabetes
#5
Xuqing Zhang, Chaozhong Cai, Zhihua Sui, Mark Macielag, Yuanping Wang, Wen Yan, Arthur Suckow, Hong Hua, Austin Bell, Peter Haug, Wilma Clapper, Celia Jenkinson, Joseph Gunnet, James Leonard, William V Murray
We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure-activity relationship studies led to the discovery of a potent GPR120 agonist 4x, which displayed good EC50 values in both calcium and β-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile. Moreover, it demonstrated in vivo antidiabetic activity in C57BL/6 DIO mice. Studies in WT and knockout DIO mice showed that it improved glucose handling during an OGTT via GPR120...
September 14, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28887275/ffa4-gpr120-as-a-fatty-acid-sensor-involved-in-appetite-control-insulin-sensitivity-and-inflammation-regulation
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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 hr, 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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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