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https://www.readbyqxmd.com/read/27914122/design-synthesis-and-structure-activity-relationships-of-bavachinin-analogues-as-peroxisome-proliferator-activated-receptor-%C3%AE-agonists
#1
Guoxin Du, Yuanyuan Zhao, Li Feng, Zhuo Yang, Jiye Shi, Cheng Huang, Bo Li, Fujiang Guo, Weiliang Zhu, Yiming Li
Bavachinin analogues with systematic modifications at the A-, B-, and C-rings were designed, synthesized, and subjected to in vitro bioevaluation as peroxisome proliferator-activated receptor γ (PPAR-γ) agonists. In total, 30 molecules, including flavanone and flavone analogues, were evaluated by reporter gene assays for the PPAR-γ agonist activity. Preliminary structure-activity relationships of PPAR-γ agonist activity of bavachinin analogues were initially summarized and analogues 2b, 3, 4a, 4b, 11c, 11d, and 12b were found with higher PPAR-γ agonist activities compared to bavachinin...
December 3, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27913621/identification-of-hepatic-lysophosphatidylcholine-acyltransferase-3-as-a-novel-target-gene-regulated-by-peroxisome-proliferator-activated-receptor-%C3%AE
#2
Amar Bahadur Singh, Jingwen Liu
Peroxisome proliferator-activated receptor δ (PPARδ) regulates many genes involved in lipid metabolism. Hepatic lysophosphatidylcholine acyltransferase 3 (LPCAT3) has critical functions in triglycerides transport and ER stress response due to its unique ability to catalyze the incorporation of polyunsaturated fatty acids into phospholipids. Previous studies identified liver X receptor as the transcription factor controlling LPCAT3 expression in mouse liver tissue. Here we show that the hepatic LPCAT3 gene is transcriptionally regulated by PPARδ...
December 2, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27912736/citrus-junos-tanaka-peel-ameliorates-hepatic-lipid-accumulation-in-hepg2-cells-and-in-mice-fed-a-high-cholesterol-diet
#3
Eun Ju Shin, Jae Ho Park, Mi Jeong Sung, Min-Yu Chung, Jin-Taek Hwang
BACKGROUND: Citrus junos Tanaka (yuja), a yellow-coloured citrus fruit has traditionally been consumed in Korea, Japan, and China and has been found effective in preventing certain diseases. However, the inhibitory effect of yuja on hepatic lipid accumulation has not been clearly elucidated thus far. METHODS: The inhibitory effect of yuja on hepatic lipid accumulation was investigated in both cell culture and mouse models. We investigated the inhibitory effect of ethanol extract of yuja peel (YE) using HepG2 cells...
December 3, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27911411/preparation-and-in-vivo-use-of-an-activity-based-probe-for-n-acylethanolamine-acid-amidase
#4
Elisa Romeo, Silvia Pontis, Stefano Ponzano, Fabiola Bonezzi, Marco Migliore, Simona Di Martino, Maria Summa, Daniele Piomelli
Activity-based protein profiling (ABPP) is a method for the identification of an enzyme of interest in a complex proteome through the use of a chemical probe that targets the enzyme's active sites. A reporter tag introduced into the probe allows for the detection of the labeled enzyme by in-gel fluorescence scanning, protein blot, fluorescence microscopy, or liquid chromatography-mass spectrometry. Here, we describe the preparation and use of the compound ARN14686, a click chemistry activity-based probe (CC-ABP) that selectively recognizes the enzyme N-acylethanolamine acid amidase (NAAA)...
November 23, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27911087/%C3%AE-amyrin-attenuates-high-fructose-diet-induced-metabolic-syndrome-in-rats
#5
Pankaj Prabhakar, K H Reeta, Subir Kumar Maulik, Amit Kumar Dinda, Yogendra Kumar Gupta
This study investigated the effect of α-amyrin (a pentacyclic triterpene) on high-fructose diet (HFD)-induced metabolic syndrome in rats. Male Wistar rats were randomly distributed into different groups. The control group was fed normal rat chow diet. The HFD group was fed HFD (60%; w/w) for 42 days. Pioglitazone (10 mg/kg, orally, once daily) was used as a standard drug. α-Amyrin was administered in 3 doses (50, 100, and 200 mg/kg, orally, once daily along with HFD). Plasma glucose, total cholesterol, triglycerides, and high-density lipoprotein cholesterol (HDL-C) were estimated...
September 2, 2016: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
https://www.readbyqxmd.com/read/27910744/peroxisome-proliferator-activated-receptor-alpha-ppar%C3%AE-a-key-regulator-of-lipid-metabolism-in-avians
#6
Bahman Navidshad, M Royan
Dietary fatty acids have various effects on cellular metabolism, and many of these effects are carried out through the alteration of the gene expression. Fatty acids upregulate or downregulate the expression of different genes by acting both as agonists or antagonists for nuclear hormone receptors. Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear hormone receptor superfamily. To date, three PPAR subtypes, α, β, and γ, have been recognized. PPARs regulate various target genes with a role in intracellular and extracellular lipid metabolism, mainly those involved in peroxisomal β-oxidation...
2016: Critical Reviews in Eukaryotic Gene Expression
https://www.readbyqxmd.com/read/27909554/high-maysin-corn-silk-extract-reduces-body-weight-and-fat-deposition-in-c57bl-6j-mice-fed-high-fat-diets
#7
Eun Young Lee, Sun Lim Kim, Hyeon Jung Kang, Myung Hwan Kim, Ae Wha Ha, Woo Kyoung Kim
BACKGROUNG/OBJECTIVES: The study was performed to investigate the effects and mechanisms of action of high maysin corn silk extract on body weight and fat deposition in experimental animals. MATERIALS/METHODS: A total of 30 male C57BL/6J mice, 4-weeks-old, were purchased and divided into three groups by weight using a randomized block design. The normal-fat (NF) group received 7% fat (diet weight basis), the high-fat (HF) group received 25% fat and 0.5% cholesterol, and the high-fat corn silk (HFCS) group received high-fat diet and high maysin corn silk extract at 100 mg/kg body weight through daily oral administration...
December 2016: Nutrition Research and Practice
https://www.readbyqxmd.com/read/27906043/exosomes-play-an-important-role-in-the-process-of-psoralen-reverse-multidrug-resistance-of-breast-cancer
#8
Xiaohong Wang, Chengfeng Xu, Yitong Hua, Leitao Sun, Kai Cheng, Zhongming Jia, Yong Han, Jianli Dong, Yuzhen Cui, Zhenlin Yang
BACKGROUND: Release of exosomes have been shown to play critical roles in drug resistance by delivering cargo. Targeting the transfer of exosomes from resistant cells to sensitive cells may be an approach to overcome some cases of drug resistance. METHOD: In this study, we investigated the potential role of exosomes in the process of psoralen reverse multidrug resistance of MCF-7/ADR cells. Exosomes were isolated by differential centrifugation of culture media from MCF-7/ADR cells (ADR/exo) and MCF-7 parental cells (S/exo)...
December 1, 2016: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/27903366/-effects-of-organochloride-pesticides-on-dyslipidemias
#9
W T Shao, A H Gu
Dyslipidemias is one important risk factor associated with chronic diseases. Persistent organic pollutants are resistant to degradation and can be bio-accumulated and magnified through the food chain. Recently, the relation between dyslipidemias and organochlorine pesticides has attracted more attentions. In this review, we explored the distribution of organochloride pesticides in the environment and human body, as well as the possible underlying mechanisms of the association between dyslipidemias and organochloride pesticides, including accumulation and release of organochloride, simulation of estrogen, impact on PPARs, the metabolic fingerprint, and the inflammatory reaction...
November 6, 2016: Zhonghua Yu Fang Yi Xue za Zhi [Chinese Journal of Preventive Medicine]
https://www.readbyqxmd.com/read/27898403/role-of-osteoprotegerin-opg-in-bone-marrow-adipogenesis
#10
Lili Zhang, Mengmeng Liu, Xiaokang Zhou, Yi Liu, Bo Jing, Xiaogang Wang, Qi Zhang, Yao Sun
BACKGROUND/AIMS: Bone marrow adipogenesis is one of the major characteristics of aged bone. Bone marrow mesenchymal stem cells (BMMSCs) prefer to differentiate into adipocytes instead of osteoblasts in the bone marrow cavity in aged hosts. The mechanism of formation and function of adipocytes in aged bone marrow needs further investigation. Osteoprotegerin (OPG) is a member of the tumor necrosis factor receptor (TNFR) super family, and it can inhibit the activities of osteoclasts. We found that adipocyte numbers increased in the bone marrow of Opg knockout mice...
November 30, 2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27897122/bioinformatics-analysis-of-chicken-mirnas-associated-with-monocyte-to-macrophage-differentiation-and-subsequent-ifng-stimulated-activation
#11
Kristopher Jl Irizarry, Adam Chan, Derek Kettle, Steven Kezian, Dominic Ma, Louis Palacios, Qingshun Li, Calvin L Keeler, Yvonne Drechsler
The goal of this project was to characterize the molecular and cellular roles of various gene targets regulated by 8 miRNAs in differentiating macrophages. Among a number of miRNAs that are found to be expressed in avian macrophages, we focused on eight specific miRNAs (miR-1618, miR-1586, miR-1633, miR-1627, miR-1646, miR-1649, miR-1610, miR-1647) associated with macrophage activation through Wnt signaling, ubiquitination, PPAR mediated macrophage function, vesicle mediated cytokine trafficking, and WD40 domain proteins in macrophage differentiation...
November 29, 2016: MicroRNA
https://www.readbyqxmd.com/read/27895698/combinations-of-bio-active-dietary-constituents-affect-human-white-adipocyte-function-in-vitro
#12
Ines Warnke, Johan W E Jocken, Rotraut Schoop, Christine Toepfer, Regina Goralczyk, Joseph Schwager
BACKGROUND: Specific bio-active dietary compounds modulate numerous metabolic processes in adipose tissue (AT), including pre-adipocyte proliferation and differentiation. AT dysfunction, rather than an increased fat mass per se, is strongly associated with the development of insulin resistance and is characterized by impaired adipogenesis, hypertrophic adipocytes, inflammation, and impairments in substrate metabolism. A better understanding of mechanisms underlying AT dysfunction may provide new strategies for the treatment of obesity-associated metabolic diseases...
2016: Nutrition & Metabolism
https://www.readbyqxmd.com/read/27895156/sildenafil-prevents-podocyte-injury-via-ppar-%C3%AE-mediated-trpc6-inhibition
#13
Ramon Sonneveld, Joost G Hoenderop, Andrea M Isidori, Carole Henique, Henry B Dijkman, Jo H Berden, Pierre-Louis Tharaux, Johan van der Vlag, Tom Nijenhuis
Transient receptor potential channel C6 (TRPC6) gain-of-function mutations and increased TRPC6 expression in podocytes induce glomerular injury and proteinuria. Sildenafil reduces TRPC6 expression and activity in nonrenal cell types, although the mechanism is unknown. Peroxisome proliferator-activated receptor γ (PPAR-γ) is a downstream target of sildenafil in the cyclic guanosine monophosphate (cGMP)-activated protein kinase G (PKG) axis. PPAR-γ agonists, like pioglitazone, appear antiproteinuric. We hypothesized that sildenafil inhibits TRPC6 expression in podocytes through PPAR-γ-dependent mechanisms, thereby counteracting podocyte injury and proteinuria...
November 28, 2016: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/27894254/divergent-selection-induced-obesity-alters-the-composition-and-functional-pathways-of-chicken-gut-microbiota
#14
Jinmei Ding, Lele Zhao, Lifeng Wang, Wenjing Zhao, Zhengxiao Zhai, Li Leng, Yuxiang Wang, Chuan He, Yan Zhang, Heping Zhang, Hui Li, He Meng
BACKGROUND: The gastrointestinal tract is populated by a complex and vast microbial network, with a composition that reflects the relationships of the symbiosis, co-metabolism, and co-evolution of these microorganisms with their host. The mechanism that underlies such interactions between the genetics of the host and gut microbiota remains elusive. RESULTS: To understand how genetic variation of the host shapes the gut microbiota and interacts with it to affect the metabolic phenotype of the host, we compared the abundance of microbial taxa and their functional performance between two lines of chickens (fat and lean) that had undergone long-term divergent selection for abdominal fat pad weight, which resulted in a 4...
November 28, 2016: Genetics, Selection, Evolution: GSE
https://www.readbyqxmd.com/read/27893688/identification-of-genes-and-signaling-pathways-associated-with-diabetic-neuropathy-using-a-weighted-correlation-network-analysis-a-consort-study
#15
Ya Li, Weiguo Ma, Chuanqing Xie, Min Zhang, Xiaohong Yin, Fenfen Wang, Jie Xu, Bingyin Shi
BACKGROUND: The molecular mechanisms behind diabetic neuropathy remains to be investigated. METHODS: This is a secondary study on microarray dataset (GSE24290) downloaded from Gene Expression Omnibus (GEO) at the National Center for Biotechnology Information (NCBI), which included 18 nerve tissue samples of progressing diabetic neuropathy (fibers loss ≥500 fibers/mm) and 17 nerve tissue samples of nonprogressing diabetic neuropathy (fibers loss ≤100 fibers/mm)...
November 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27891661/synergistic-effects-of-polydatin-and-vitamin-c-in-inhibiting-cardiotoxicity-induced-by-doxorubicin-in-rats
#16
Hui-Lin Wang, Xiao-Hua Cui, Hai-Lun Yu, Rong Wu, Xu Xu, Jian-Ping Gao
The purpose of this study was to assess the synergistic effect of polydatin and vitamin C on attenuating cardiotoxicity induced by doxorubicin (DOX) in rats. Polydatin could significantly increase the activity of SOD and the heart rate, attenuate myocardial pathological damage, decrease MDA content, slightly increase arterial pressure and GSH-Px activity, reduce intervals of QRS, QT and ST, and lower FFA content. The combination of polydatin and vitamin C could significantly increase arterial pressure and heart rate, decrease QRS interval and slightly reduce ST and QT intervals, significantly attenuate myocardial pathological damage, increase the activities of GSH-Px,T-SOD, Na(+) K(+) -ATPase and Ca(2+) Mg(2+) -ATPase, and elevate PCr and ATP contents, slightly increase ADP and TAN contents and PCr/ATP, and significantly decrease the contents of MDA and FFA, when compared with those in the DOX group...
November 28, 2016: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27890711/the-endogenous-lipid-n-arachidonoyl-glycine-is-hypotensive-and-nitric-oxide-cgmp-dependent-vasorelaxant
#17
Yousuf M Al Suleimani, Ahmed S Al Mahruqi
N-arachidonoyl glycine (NAGLY), is the endogenous lipid that activates the G protein-couple receptor 18 (GPR18) with vasodilatory activity in resistance arteries. This study investigates its hemodynamic effects and mechanisms of vasorelaxation. Hemodynamic effects of NAGLY in rats were assessed using a Biopac system and its vascular responses were assessed using a wire myograph. NAGLY (1 mg/kg) decreased blood pressure by 69.4 ± 5.5% and reduced renal blood flow by 88 ± 12% and the effects were not sensitive to inhibition by O-1918 (3 mg/kg)...
November 24, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27889747/alisol-a-24-acetate-prevents-hepatic-steatosis-and-metabolic-disorders-in-hepg2-cells
#18
Lu Zeng, WaiJiao Tang, JinJin Yin, LiJuan Feng, Yabing Li, Xiaorui Yao, BenJie Zhou
BACKGROUND: Non-alcoholic fatty liver disease (NAFLD) is closely associated with metabolic disorders including hepatic lipid accumulation and inflammation. Alisol A 24-acetate, a triterpene from Alismatis rhizome, has multiple biologic activities such as hypolipidemic, anti-inflammatory and anti-diabetic. Thus we hypothesized that Alisol A 24 -acetate would have effect on NAFLD. The present study was conducted to investigate the therapeutic effects and potential mechanisms of Alisol A 24-acetate against hepatic steatosis in a free fatty acids (FFAs) induced NAFLD cell model...
November 25, 2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27887739/differences-in-the-modulation-of-reactive-species-lipid-bodies-cyclooxygenase-2-5-lipoxygenase-and-ppar-%C3%AE-in-cerebral-malaria-susceptible-and-resistant-mice
#19
Tatiana K S Borges, Érica A R Alves, Henda A R Vasconcelos, Fabiana P Carneiro, André M Nicola, Kelly G Magalhães, Maria Imaculada Muniz-Junqueira
Proinflammatory responses are associated with the severity of cerebral malaria. NO, H2O2, eicosanoid and PPAR-γ are involved in proinflammatory responses, but regulation of these factors is unclear in malaria. This work aimed to compare the expression of eicosanoid-forming-enzymes in cerebral malaria-susceptible CBA and C57BL/6 and -resistant BALB/c mice. Mice were infected with Plasmodium berghei ANKA, and the survival rates and parasitemia curves were assessed. On the sixth day post-infection, cyclooxygenase-2 and 5-lipoxygenase in brain sections were assessed by immunohistochemistry, and, NO, H2O2, lipid bodies, and PPAR-γ expression were assessed in peritoneal macrophages...
November 17, 2016: Immunobiology
https://www.readbyqxmd.com/read/27884680/caloric-restriction-ameliorates-cardiomyopathy-in-animal-model-of-diabetes
#20
Keren Cohen, Maayan Waldman, Nader G Abraham, Michal Laniado-Schwartzman, Danny Gurfield, Dan Aravot, Michael Arad, Edith Hochhauser
BACKGROUND: The db/db mouse is an animal model of diabetes in which leptin receptor activity is deficient resulting accelerated cardiomyopathy when exposed to angiotensin (AT). Toll-like receptors 4 and 2 (TLR4, TLR2) are pattern recognition receptors, that recognize pathogen-associated molecular patterns and exacerbate and release inflammatory cytokines. Fetuin A (Fet A) is a fatty acid carrier which affects inflammation and insulin resistance in obese humans and animals through TLRs...
November 21, 2016: Experimental Cell Research
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