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N-acyl or cannabinoid or NAPE

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https://www.readbyqxmd.com/read/29053249/holistic-lipidomics-of-the-human-gut-phenotype-using-validated-ultra-high-performance-liquid-chromatography-coupled-to-hybrid-orbitrap-mass-spectrometry
#1
Lieven Van Meulebroek, Ellen De Paepe, Vicky Vercruysse, Beata Pomian, Simon Bos, Bruno Lapauw, Lynn Vanhaecke
As lipids are assigned a plethora of biological functions, it is evident that a dysregulated lipid metabolism signifies a key element in many pathological conditions. With this rationale, this study presents a validated lipidomics platform to map the fecal lipidome, which integrates unique information about the host-gut microbiome interactions, gastrointestinal functionality, and dietary pattern. This particular method accomplished coverage across all eight lipid categories; the fatty acyls, glycerolipids, phosphoglycerolipids, polyketides, prenols, saccharolipids, sphingolipids, and sterols...
October 20, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29051736/novel-peripherally-restricted-cannabinoid-1-receptor-selective-antagonist-txx-522-with-prominent-weight-loss-efficacy-in-diet-induced-obese-mice
#2
Wei Chen, Fengchun Shui, Cheng Liu, Xinbo Zhou, Wei Li, Zhibing Zheng, Wei Fu, Lili Wang
The clinical development of the first generation of globally active cannabinoid 1 receptor (CB1R) antagonists was suspended because of their adverse neuropsychiatric effects. Selective blockade of peripheral CB1Rs has the potential to provide a viable strategy for the treatment of severe obesity while avoiding these central nervous system side effects. In the current study, a novel compound (TXX-522) was rationally designed based on the parent nucleus of a classical CB1R-selective antagonist/inverse agonist, rimonabant (SR141716A)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29051094/modification-of-proteins-and-polysaccharides-using-dodecenyl-succinic-anhydride-synthesis-properties-and-applications-a-review
#3
REVIEW
Nirali N Shah, Niharika Soni, Rekha S Singhal
Proteins and polysaccharides are among the biopolymers produced by living organisms for their structural integrity, protection, physiological functions or as reserve energy. These biopolymers are extracted from their natural matrices by humans to fulfil basic as well as convenience needs. The inquisitive human nature, ever-growing demands and resources at disposal have led to copious research in the field of biopolymer modifications. The availability of reactive sites on these biopolymers make them suitable substrates for esterification, etherification, oxidation, epoxidation, N-acylation, alkylation, etc...
October 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29049116/basic-translational-development-of-forthcoming-opioid-and-nonopioid-targeted-pain-therapeutics
#4
Nebojsa Nick Knezevic, Ajay Yekkirala, Tony L Yaksh
Opioids represent an efficacious therapeutic modality for some, but not all pain states. Singular reliance on opioid therapy for pain management has limitations, and abuse potential has deleterious consequences for patient and society. Our understanding of pain biology has yielded insights and opportunities for alternatives to conventional opioid agonists. The aim is to have efficacious therapies, with acceptable side effect profiles and minimal abuse potential, which is to say an absence of reinforcing activity in the absence of a pain state...
November 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29049102/unraveling-the-mystery-of-thc-cannabinoids-and-neuropathic-pain
#5
Naveen Nathan
No abstract text is available yet for this article.
November 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29048877/stereoselective-synthesis-of-benzo-e-1-4-oxazino-4-3-a-1-4-diazepine-6-12-diones-with-two-diversity-positions
#6
Petra Kralova, Michal Malon, Miroslav Soural
Herein, we report a fully stereoselective synthesis of tetrahydro-6H-benzo[e][1,4]oxazino[4,3-a][1,4]diazepine-6,12(11H)-diones from polymer-supported Fmoc-Ser(tBu)-OH. After the simple solid-phase synthesis of N-alkylated-N-acylated intermediates using various 2-nitrobenzoic acids and bromoketones, the key intermediates were obtained via trifluoroacetic acid (TFA)-mediated cleavage from the resin in the presence of triethylsilane (TES), which led to stereoselective reduction and yielded a specific configuration of the newly formed C3 chiral center...
October 19, 2017: ACS Combinatorial Science
https://www.readbyqxmd.com/read/29048715/one-pot-four-segment-ligation-realized-by-selenoester-and-its-application-to-the-synthesis-of-superoxide-dismutase
#7
Hironobu Hojo, Toshiki Takei, Tomoshige Andoh, Toshifumi Takao
The synthesis of the peptide selenoester was efficiently carried out by the 9-fluorenylmethoxycarbonyl method using the N-alkylcysteine at the C-terminus of the peptide as the N-to-S acyl shift device. The selenoester highly selectively reacted with the terminal amino group of the peptide aryl thioester in the presence of N, N-diisopropylethylamine and dipyridyldisulfide, maintaining the aryl thioester intact. Combining with the silver ion promoted and silver ion free thioester activation method, the one-pot four-segment ligation was realized...
October 19, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/29048366/lipase-catalyzed-transesterification-of-egg-yolk-phophatidylcholine-with-concentrate-of-n-3-polyunsaturated-fatty-acids-from-cod-liver-oil
#8
Anna Chojnacka, Witold Gładkowski, Aleksandra Grudniewska
Phospholipids containing PUFAs are important vehicles for their delivering to the targeted tissues. In our research project we established enzymatic methods for the enrichment of natural egg-yolk PC with n-3 PUFAs. Instead of synthetic PUFA ethyl esters, the new strategy was developed using polyunsaturated fatty acids enriched fraction (PUFA-EF) from cod liver oil as the natural acyl donors. PUFA-EF was produced by urea-complexation and contained 86.9% PUFA including 8.5% stearidonic acid (SDA; 18:4(n-3)), 26...
October 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29047318/spontaneous-spinal-epidural-hemorrhage-following-disseminated-intravascular-coagulation-resulting-in-paraplegia-a-case-report
#9
Nazia Dildar, Saeed Bin Ayaz, Muhammad Omer Aamir, Nadeem Ahmad
CONTEXT: Spontaneous spinal epidural hemorrhage (SSEH) mostly presents as low back pain with or without a radiculopathy, and rarely with paraplegia or tetraplegia depending on the site and severity of spinal cord compression. We present here a case who had anemia and developed paraplegia following disseminated intravascular coagulation (DIC) due to a transfusion reaction. FINDINGS: A 65-year-old lady presented with sudden onset chest pain radiating to nape of the neck followed by loss of sensations and power in legs few hours after a blood transfusion...
October 19, 2017: Journal of Spinal Cord Medicine
https://www.readbyqxmd.com/read/29046744/clinical-and-epidemiological-characteristics-of-patients-with-acute-drug-intoxication-admitted-to-icu
#10
Jose Orsini, Nanda Din, Ershad Elahi, Anthony Gomez, Salil Rajayer, Ryan Malik, Elie Jean
Background: Drug overdose continues to be the most common cause of acute poisoning worldwide. There has been a substantial increase in drug overdose incidence and prevalence over the past decade, probably as a result of the emergence of new synthetic designer drugs. The purpose of this study is to describe the clinical and epidemiological characteristics of patients with acute drug intoxication admitted to the Intensive Care Unit (ICU). Methods: A single center, prospective, observational study was conducted among all adult patients with clinical signs suggestive of acute drug intoxication admitted from the Emergency Department (ED) to ICU during a 6-month period (September to March)...
October 2017: Journal of Community Hospital Internal Medicine Perspectives
https://www.readbyqxmd.com/read/29046638/blockade-of-cannabinoid-cb1-receptors-in-the-dorsal-periaqueductal-gray-unmasks-the-antinociceptive-effect-of-local-injections-of-anandamide-in-mice
#11
Diego C Mascarenhas, Karina S Gomes, Tatiani Sorregotti, Ricardo L Nunes-de-Souza
Divergent results in pain management account for the growing number of studies aiming at elucidating the pharmacology of the endocannabinoid/endovanilloid anandamide (AEA) within several pain-related brain structures. For instance, the stimulation of both Transient Receptor Potential Vanilloid type 1 (TRPV1) and Cannabinoid type 1 (CB1) receptors led to paradoxical effects on nociception. Here, we attempted to propose a clear and reproducible methodology to achieve the antinociceptive effect of exogenous AEA within the dorsal periaqueductal gray (dPAG) of mice exposed to the tail-flick test...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29045576/activation-of-cannabinoid-receptor-1-is-involved-in-protection-against-mitochondrial-dysfunction-and-cerebral-ischaemic-tolerance-induced-by-isoflurane-preconditioning
#12
M Cai, Q Yang, G Li, S Sun, Y Chen, L Tian, H Dong
Background: Isoflurane preconditioning (IPC) induces cerebral ischaemic tolerance, but the mechanism remains poorly understood. The aim of this study was to determine changes in mitochondrial function in the brain after IPC, and whether the cannabinoid receptor 1 (CB1R) could be involved in the mechanism of mitochondrial protection mediated by IPC. Methods: Adult male Sprague-Dawley rats were pretreated with isoflurane 2% for 1 h day-1, for 5 days consecutively, and then subjected to 120 min right middle cerebral artery occlusion...
October 13, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29045301/cannabinoid-hyperemesis-syndrome-chs-a-parisian-case-series
#13
Maude Marillier, Anne Batisse, Yves Edel, An-Hung Nguyen, Cécile Chevallier, Grégory Pfau, Philippe Podevin, Samira Djezzar
No abstract text is available yet for this article.
October 17, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29044015/-argentina-enacts-first-law-on-medical-use-of-the-cannabis-plant-history-and-perspectives
#14
Eduardo L De Vito
In the last few years, great expectations have risen in the society concerning the eventual therapeutic usefulness of compounds derived from the cannabis plant. It is well known that these compounds are being used in treating certain health conditions, either through medical prescription or self-administration. Extreme opinions range from believing that it is a harmful and dangerous drug to sustaining that it is a panacea. However, the sheer existence of an endocannabinoid system in the brain compels us to study its dimensions and derivations thoroughly...
2017: Medicina
https://www.readbyqxmd.com/read/29042214/synthetic-cannabinoid-am2201-induces-seizures-involvement-of-cannabinoid-cb1-receptors-and-glutamatergic-transmission
#15
Masahiko Funada, Mika Takebayashi-Ohsawa
Abuse of synthetic cannabinoids is a serious social problem worldwide. Intentional ingestion of synthetic cannabinoids can cause severe toxicity, including seizures. Here we investigated the effects of acute administration of synthetic cannabinoids on the induction of epileptic seizures by monitoring electroencephalographic activity in freely moving mice. The synthetic cannabinoid, AM2201, induced abnormal, high-amplitude (>2-fold baseline amplitude), sharp-wave activity. The abnormal spike-wave discharges were accompanied by epileptiform behavior: rigid posture, tail extension, rearing with forepaws extended, jumping, and intermittent tonic-clonic jerking movements...
October 14, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29040803/synthesis-and-characterization-of-fatty-acid-grafted-chitosan-polymer-and-their-nanomicelles-for-non-viral-gene-delivery-applications
#16
Divya Sharma, Jagdish Singh
The aim of this study was to synthesize and characterize fatty acid-grafted-chitosan (fatty acid-g-CS) polymer and their nanomicelles for using as carriers for gene delivery. CS was hydrophobically modified using saturated fatty acids of increasing fatty acyl chain length. Carbodiimide along with N-hydroxysuccinimide was used for coupling carboxyl group of fatty acids with amine groups of CS. Proton nuclear magnetic resonance and Fourier transform-infrared spectroscopy were used to quantify fatty acyl substitution onto CS backbone...
October 17, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29039866/n-acylsuccinimides-twist-controlled-acyl-transfer-reagents-in-suzuki-miyaura-cross-coupling-by-n-c-amide-bond-activation
#17
Yuki Osumi, Chengwei Liu, Michal Szostak
The palladium-catalyzed Suzuki-Miyaura cross-coupling of N-acylsuccinimides as versatile acyl-transfer reagents via selective amide N-C bond cleavage is reported. The method is user-friendly since it employs commercially-available, air-stable reagents and catalysts. The cross-coupling is enabled by half-twist of the amide bond in N-acylsuccinimides. These highly effective, crystalline acyl-transfer reagents present major advantages over perpendicularly twisted N-acylglutarimides, including low price of the succinimide activating ring, selective metal insertion under redox neutral conditions and high stability of the amide bond towards reaction conditions...
October 17, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29039791/synthesis-of-chiral-tfa-protected-%C3%AE-amino-aryl-ketone-derivatives-with-friedel-crafts-acylation-of-%C3%AE-amino-acid-n-hydroxysuccinimide-ester
#18
Zetryana Puteri Tachrim, Kazuhiro Oida, Haruka Ikemoto, Fumina Ohashi, Natsumi Kurokawa, Kento Hayashi, Mami Shikanai, Yasuko Sakihama, Yasuyuki Hashidoko, Makoto Hashimoto
Chiral N-protected α-amino aryl-ketones are one of the useful precursors used in the synthesis of various biologically active compounds and can be constructed via Friedel-Crafts acylation of N-protected α-amino acids. One of the drawbacks of this reaction is the utilization of toxic, corrosive and moisture-sensitive acylating reagents. In peptide construction via amide bond formation, N-hydroxysuccinimide ester (OSu), which has high storage stability, can react rapidly with amino components and produces fewer side reactions, including racemization...
October 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29039165/-screening-for-fatty-acid-oxidation-disorders-of-newborns-in-zhejiang-province-prevalence-outcome-and-follow-up
#19
Jing Zheng, Yu Zhang, Fang Hong, Jianbin Yang, Fan Tong, Huaqing Mao, Xiaolei Huang, Xuelian Zhou, Rulai Yang, Zhengyan Zhao, Xinwen Huang
OBJECTIVE: To screen fatty acid oxidation disorders (FAOD) in newborns in Zhejiang province. METHODS: A total of 1 861 262 newborns were screened for FAOD in Neonatal Screening Center of Zhejiang Province during January 2009 and December 2016. The blood samples from newborns were screened by tandem mass spectrometry, and diagnosis of FAOD was confirmed by urine organic acid measurement combined with genetic analysis. The prognosis and follow-up of patients with FAOD were also evaluated...
May 25, 2017: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/29038772/revealing-the-genomic-differences-between-two-subgroups-in-lactobacillus-gasseri
#20
Ipputa Tada, Yasuhiro Tanizawa, Akihito Endo, Masanori Tohno, Masanori Arita
Being an autochthonous species in humans, Lactobacillus gasseri is widely used as a probiotic for fermented products. We thoroughly compared the gene contents of 75 L. gasseri genomes and identified two intraspecific groups by the average nucleotide identity (ANI) threshold of 94%. Group I, with 48 strains, possessed 53 group-specific genes including the gassericin T cluster (9 genes) and N-acyl homoserine lactone lactonase. Group II, with 27 strains, including the type strain ATCC 33323, possessed group-specific genes with plasmid- or phage-related annotations...
2017: Bioscience of Microbiota, Food and Health
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