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https://www.readbyqxmd.com/read/29148769/azetidine-and-piperidine-carbamates-as-efficient-covalent-inhibitors-of-monoacylglycerol-lipase
#1
Christopher R Butler, Elizabeth M Beck, Anthony R Harris, Zhen Huang, Laura A McAllister, Christopher W Am Ende, Kimberly F Fennell, Timothy L Foley, Kari R Fonseca, Steven J Hawrylik, Douglas S Johnson, John D Knafels, Scot Mente, Stephen Noell, Jayvardhan Pandit, Tracy B Phillips, Justin R Piro, Bruce N Rogers, Tarek A Samad, Jane Wang, Shuangyi Wan, Michael A Brodney
Monoacylglycerol lipase (MAGL) is the main enzyme responsible for degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the CNS. MAGL catalyzes the conversion of 2-AG to arachidonic acid (AA), a precursor to the pro-inflammatory eicosannoids such as prostaglandins. Herein we describe highly efficient MAGL inhibitors, identified through a parallel medicinal chemistry approach that highlighted the improved efficiency of azetidine and piperidine-derived carbamates. The discovery and optimization of 3-substituted azetidine carbamate irreversible inhibitors of MAGL was aided by the generation of inhibitor-bound MAGL crystal structures...
November 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29147968/effects-of-fasting-on-the-activities-and-mrna-expression-levels-of-lipoprotein-lipase-lpl-hormone-sensitive-lipase-hsl-and-fatty-acid-synthetase-fas-in-spotted-seabass-lateolabrax-maculatus
#2
Hongli Huang, Yu Zhang, Mingyue Cao, Liangyi Xue, Weiliang Shen
To investigate the effects of fasting on lipid metabolism in spotted seabass muscle and liver tissues, we analyzed mRNA levels and enzyme activities of lipoprotein lipase (LPL), hormone-sensitive lipase (HSL) and fatty acid synthetase (FAS), and the relationship among fat content, mRNA level, and enzyme activity during fasting of 35 days. The results showed that expressions of all the three genes were ubiquitous. During the fasting experiment, the hepatosomatic index (HSI) and fat content of muscle and liver tissues significantly decreased before 5 days of fasting (P < 0...
November 16, 2017: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/29146968/heterologous-expression-and-characterization-of-a-new-lipase-from-pseudomonas-fluorescens-pf0-1-and-used-for-biodiesel-production
#3
Wu Liu, Menggang Li, Yunjun Yan
As a kind of important biocatalysts, Pseudomonas lipases are commonly applied in various industrial fields. Pflip1, a new extracellular lipase gene from Pseudomonas. fluorescens Pf0-1, was first cloned and respectively expressed in Escherichia coli BL21(DE3) and Pichia pastoris KM71, the recombinant proteins Pflip1a and Pflip1b were later purified separately. Then Pflip1a was further characterized. The optimum pH of Pflip1a was 8.0 and its optimal temperature was 70 °C. After incubation at 70 °C for 12 h, Pflip1a could retain over 95% of its original activity...
November 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29146375/investigating-the-optimum-conditions-for-minimized-3-chloropropane-1-2-diol-esters-content-and-improved-sensory-attributes-during-savory-beef-flavor-preparation
#4
Qingqing Chai, Khizar Hayat, Eric Karangwa, Emmanuel Duhoranimana, Xiaoming Zhang, Shuqin Xia, Jingyang Yu
In this study, the effects of enzymatic hydrolysis of tallow and addition of sodium chloride (NaCl) were evaluated on the formation of 3-monochloropropane-1,2-diol (3-MCPD) esters and sensory characteristic of beef flavors. The enzymatic hydrolysis condition had significant effects on 3-MCPD mono/di-esters formation during the beef flavor preparation. Considering the safety and sensory characteristics of beef flavors, the optimal enzymatic hydrolysis conditions were selected as: lipase concentration 75U/g tallow, tallow concentration 80% (w/v) and pH 7...
March 15, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29146190/newly-developed-selective-immunoinactivation-assay-revealed-reduction-in-adipose-triglyceride-lipase-activity-in-peripheral-leucocytes-from-patients-with-idiopathic-triglyceride-deposit-cardiomyovasculopathy
#5
Atsuko Takagi, Yasuyuki Ikeda, Kunihisa Kobayashi, Kazuhiro Kobayashi, Yoshihiko Ikeda, Junji Kozawa, Hideyuki Miyauchi, Ming Li, Chikako Hashimoto, Yasuhiro Hara, Satoshi Yamaguchi, Akira Suzuki, Tatsushi Toda, Hironori Nagasaka, Ken-Ichi Hirano
Triglyceride deposit cardiomyovasculopathy (TGCV) is a rare and newly identified disease among patients requiring cardiac transplantation. TGCV is characterized by cardiomyocyte steatosis and triglyceride (TG)-deposit atherosclerosis, resulting from the abnormal intracellular metabolism of TG. TGCV is classified into primary and idiopathic types. Primary TGCV carries ultra-rare genetic mutations in the adipose triglyceride lipase (ATGL), a rate-liming enzyme that hydrolyzes intracellular TG in adipose and non-adipose tissues...
November 13, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29145497/rare-genetic-variants-in-the-endocannabinoid-system-genes-cnr1-and-dagla-are-associated-with-neurological-phenotypes-in-humans
#6
Douglas R Smith, Christine M Stanley, Theodore Foss, Richard G Boles, Kevin McKernan
Rare genetic variants in the core endocannabinoid system genes CNR1, CNR2, DAGLA, MGLL and FAAH were identified in molecular testing data from 6,032 patients with a broad spectrum of neurological disorders. The variants were evaluated for association with phenotypes similar to those observed in the orthologous gene knockouts in mice. Heterozygous rare coding variants in CNR1, which encodes the type 1 cannabinoid receptor (CB1), were found to be significantly associated with pain sensitivity (especially migraine), sleep and memory disorders-alone or in combination with anxiety-compared to a set of controls without such CNR1 variants...
2017: PloS One
https://www.readbyqxmd.com/read/29145154/a-pipeline-for-proteome-scale-identification-and-studies-on-hormone-sensitive-lipases-in-mycobacterium-tuberculosis
#7
Durairaj Sherlin, Sharmila Anishetty
Hormone sensitive lipases (HSLs) play an important role in the survival of M. tuberculosis during dormancy. They help in the utilization of fatty acids from stored lipids. The objective of the current study was to identify all HSLs from the proteome of M. tuberculosis H37Rv. We have developed a novel HSL identification pipeline, based on amino acid sequence homology, presence of conserved motifs and other sequence features deciphered from known HSL dataset. Through this pipeline, we identified 10 proteins as putative HSLs in M...
November 7, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/29144385/preparation-and-characterization-of-cellulose-triacetate-as-support-for-lecitase-ultra-immobilization
#8
Francielle Batista da Silva, Wilson Galvão de Morais Júnior, Cleuzilene Vieira da Silva, Andressa Tironi Vieira, Antônio Carlos Ferreira Batista, Anízio Márcio de Faria, Rosana Maria Nascimento Assunção
The use of polymers as supports for enzyme immobilization is a strategy that enables to remove the enzymes from a chemical reaction and improve their efficiency in catalytic processes. In this work, cellulose triacetate (CTA) was used for physical adsorption of phospholipase Lecitase ultra (LU). CTA is more hydrophobic than cellulose, shows good performance in the lipases immobilization being a good candidate for immobilization of phospholipases. We investigated the immobilization of LU in CTA, the stability of the immobilized enzyme (CTA-LU) and the performance of CTA-LU using soybean oil as a substrate...
November 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29141191/microbial-lipids-and-added-value-metabolites-production-by-yarrowia-lipolytica-from-pork-lard
#9
Marlene Lopes, Andreia S Gomes, Carla M Silva, Isabel Belo
Yarrowia lipolytica is a suitable microbial platform to convert low-value hydrophobic substrates into microbial oils and other important metabolites. In this work, this yeast species was used to simultaneously synthetize ex novo lipids and produce citric acid and lipase from animal fat (pork lard) adding higher value to the low-cost fatty substrate. The effect of pH, lard concentration, arabic gum concentration and oxygen mass transfer rate (OTR) on lipids accumulation on Y. lipolytica batch cultures was assessed by an experimental design based on Taguchi method...
November 12, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/29140549/improving-pancreas-graft-utilization-through-importation
#10
Julia Torabi, Juan P Rocca, Krystina Choinski, Katherine Lorenzen, Camille Yongue, Michelle L Lubetzsky, Melvon E Herbert, Attasit Chokechanachaisakul, Maria Ajaimy, Layla Kamal, Enver Akalin, Milan Kinkhabwala, Jay A Graham
BACKGROUND: We analyze our outcomes utilizing imported allografts as a strategy to shorten wait list time for pancreas transplantation. METHODS: This is an observational retrospective cohort of 26 recipients who received either a locally procured (n=16) or an imported pancreas graft (n=10) at our center between January 2014 and May 2017. Wait list times of this cohort were compared to UNOS Region 9 (New York State and Western Vermont). Hospital financial data was also reviewed to analyze the cost effectiveness of this strategy...
November 15, 2017: Clinical Transplantation
https://www.readbyqxmd.com/read/29140274/an-efficient-approach-for-lipase-catalyzed-synthesis-of-retinyl-laurate-nutraceutical-by-combining-ultrasound-assistance-and-artificial-neural-network-optimization
#11
Shang-Ming Huang, Hsin-Ju Li, Yung-Chuan Liu, Chia-Hung Kuo, Chwen-Jen Shieh
Although retinol is an important nutrient, retinol is highly sensitive to oxidation. At present, some ester forms of retinol are generally used in nutritional supplements because of its stability and bioavailability. However, such esters are commonly synthesized by chemical procedures which are harmful to the environment. Thus, this study utilized a green method using lipase as a catalyst with sonication assistance to produce a retinol derivative named retinyl laurate. Moreover, the process was optimized by an artificial neural network (ANN)...
November 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29139569/lipase-catalyzed-enantioselective-transesterification-of-prochiral-1-1-3-dihydroxypropan-2-yloxy-methyl-5-6-7-8-tetrahydroquinazoline-2-4-1h-3h-dione-in-ionic-liquids
#12
Renata Kołodziejska, Renata Studzińska, Hanna Pawluk
The application of ionic liquids as solvents for transesterification of prochiral pirymidine acyclonucleoside using lipase (EC 3.1.1.3) Amano PS from Burkholderia cepacia (BCL) is reported. The effect of using medium reaction, acyl group donor, and temperature on the activity and enantioselectivity of BCL was studied. From the investigated ionic solvents, the hydrophobic ionic liquid [BMIM]PF6 ] was the preferred medium for enzymatic reactions. However, the best result was obtained in the mixture [BMIM][PF6 ]:TBME (1:1 v/v) at 50°C...
November 15, 2017: Chirality
https://www.readbyqxmd.com/read/29139118/di-2-ethylhexyl-phthalate-dehp-exposure-disturbs-lipid-metabolism-in-juvenile-yellow-catfish-tachysurus-fulvidraco
#13
F X Meng, M Li, M Z Song, L X Yuan, Y F Gong, Y X Qian, G Shi, R X Wang
This study was conducted to determine the mechanism by which di-2-ethylhexyl phthalate (DEHP) exposure influences lipid metabolism of juvenile yellow catfish Tachysurus fulvidraco. Fish were exposed to three DEHP concentrations (0, 0·1 and 0·5 mg l(-1) DEHP) for 8 weeks. Fatty acid synthase (FAS) activity significantly decreased with increasing DEHP concentrations, the highest value was in the Tween control group, whereas the lowest activities of carnitine palmitoyltransferase (CPT) and lipoprotein lipase (LPL) were in this group...
November 15, 2017: Journal of Fish Biology
https://www.readbyqxmd.com/read/29138223/effect-of-maternal-high-fat-diet-on-key-components-of-the-placental-and-hepatic-endocannabinoid-system
#14
Kushal Gandhi, Cun Li, Nadezhda German, Cezary Skobowiat, Maira Carrillo, Raja Reddy Kallem, Eneko Larumbe, Stacy Martinez, Marcel Chuecos, Gary Ventolini, Peter Nathanielsz, Natalia Schlabritz-Loutsevitch
INTRODUCTION: Involvement of endogenous cannabinoids (eCBs) in obesity is well-characterized. However, information regarding eCB physiology in obesity associated with pregnancy is sparse. METHODS: From at least 9 months before conception, non-pregnant baboons (Papio spp.) were fed a diet of either 45% fat (HFD; n=11) or 12% fat or a control diet (CTR; n=11), and dietary intervention continued through pregnancy. Maternal and fetal venous plasma samples were evaluated using liquid chromatography-mass spectrometry to quantify anandamide (AEA) and 2-arachidonoyl glycerol (2-AG)...
November 14, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29137992/ir-spectroscopy-analysis-of-pancreatic-lipase-related-protein-2-interaction-with-phospholipids-3-monitoring-dppc-lipolysis-in-mixed-micelles
#15
Eduardo Mateos-Diaz, Priscila Sutto-Ortiz, Moulay Sahaka, Jorge A Rodriguez, Frédéric Carrière
Usual methods for the continuous assay of lipolytic enzyme activities are mainly based on the titration of free fatty acids, surface pressure monitoring or spectrophotometry using substrates labeled with specific probes. These approaches only give a partial information on the chemistry of the lipolysis reaction and additional end-point analyses are often required to quantify both residual substrate and lipolysis products. We used transmission infrared (IR) spectroscopy to monitor simultaneously the hydrolysis of phospholipids by guinea pig pancreatic lipase-related protein 2 (GPLRP2) and the release of lipolysis products...
November 11, 2017: Chemistry and Physics of Lipids
https://www.readbyqxmd.com/read/29137734/ultrasound-irradiation-promoted-enzymatic-alcoholysis-for-synthesis-of-monoglyceryl-phenolic-acids-in-a-solvent-free-system
#16
Chunfang Xu, Haiping Zhang, Jie Shi, Mingming Zheng, Xia Xiang, Fenghong Huang, Junyong Xiao
Monoglyceryl phenolic acids (MPAs) were known as the natural hydrophilic antioxidants which could be used in different fields such as food, pharmaceutical, cosmetic etc. A novel enzymatic route of MPAs synthesis by the alcoholysis of phenolic acid ethyl esters with glycerol under ultrasound irradiation in solvent free system was developed. Optimization of reaction parameters shows that a high conversion of above 97.4% can be obtained under the following conditions: phenolic acid ethyl esters to glycerol molar ratio of 1:10, with 6% catalyst (Novozym 435), at 60°C and 200rpm, with ultrasound input of 250W, at 20kHz frequency...
March 2018: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/29136214/effects-of-dietary-supplemental-bile-acids-on-performance-carcass-characteristics-serum-lipid-metabolites-and-intestinal-enzyme-activities-of-broiler-chickens
#17
Wenqing Lai, Weigang Huang, Bing Dong, Aizhi Cao, Wenjuan Zhang, Juntao Li, Hui Wu, Liying Zhang
The objective of the present study was to evaluate the effect of bile acids derived from swine on the growth performance, carcass traits, serum lipid metabolites and intestinal enzyme activities in broiler chickens. Four hundred thirty-two 1-day-old Arbor Acres male broilers were randomly assigned to 4 treatments with 6 replicates of 18 chicks each for 42 d. The experimental treatments received a corn-soybean basal diet containing lard and were as follows: 0 (control), 40 mg, 60 mg, and 80 mg bile acids/kg of diet...
November 9, 2017: Poultry Science
https://www.readbyqxmd.com/read/29135689/vldl-triglyceride-accumulation-in-skeletal-muscle-and-adipose-tissue-in-type-2-diabetes
#18
Esben Søndergaard, Søren Nielsen
PURPOSE OF REVIEW: Insulin resistance is closely linked to accumulation of lipid outside adipose tissue (ectopic fat storage). VLDL particles transport lipids from the liver to peripheral tissues. However, whether abnormalities in VLDL-triglyceride storage in muscle and adipose tissue exist in type 2 diabetes has previously been unknown, primarily because of methodological difficulties. Here, we review recent research on VLDL-triglyceride storage. RECENT FINDINGS: In a recent study, men with type 2 diabetes had increased skeletal muscle VLDL-triglyceride storage compared to weight-matched nondiabetic men, potentially leading to intramyocellular triglyceride accumulation...
November 11, 2017: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/29135023/effects-of-different-pretreatments-to-fresh-fruit-on-chemical-and-thermal-characteristics-of-crude-palm-oil
#19
Minmin Tang, Qiuyu Xia, Brendan J Holland, Hui Wang, Yufeng Zhang, Rui Li, Hongxing Cao
This study selected 5 methods, including boiling, hot air drying, high-pressurized steam, freezing, and microwave radiation to pretreat fresh oil palm fruit before solvent extraction of the oil. Using fresh fruit as a control, the pretreatment methods were compared for the effects on the activity of the 2 main enzymes in the fruit and some physicochemical properties of the crude palm oil. The results indicated, although all the 5 pretreatments could inactivate lipase and peroxidase in the treated flesh significantly (P < 0...
November 14, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/29133865/cold-acclimation-causes-fiber-type-specific-responses-in-glucose-and-fat-metabolism-in-rat-skeletal-muscles
#20
Diane M Sepa-Kishi, Yass Sotoudeh-Nia, Ayesha Iqbal, George Bikopoulos, Rolando B Ceddia
This study investigated fiber type-specific metabolic responses and the molecular mechanisms that regulate glucose and fat metabolism in oxidative and glycolytic muscles upon cold acclimation. Male Wistar rats were exposed to cold (4 °C) for 7 days, and then glycogen synthesis and content, glucose and palmitate oxidation, and the molecular mechanisms underlying these metabolic pathways were assessed in soleus (Sol), extensor digitorum longus (EDL), and epitrochlearis (Epit) muscles. Cold acclimation increased glycogen synthesis, glycogen content, glucose oxidation, and reduced glycogen synthase (GS) phosphorylation only in Sol muscles...
November 13, 2017: Scientific Reports
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