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Ethyl pyruvate

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https://www.readbyqxmd.com/read/28894846/trypsinogen-activation-peptide-induces-hmgb1-release-from-rat-pancreatic-acinar-cells
#1
Guoliang Wang, Yan Liu, Danhua Dui, Liang Bai, Yao Liu, Fei Tian, Wei Wei
BACKGROUND: The development of acute pancreatitis (AP) is associated with intracellular events in pancreatic cells, as well as with early and late inflammatory responses; however, their underlying mechanisms remain unclear. This study investigated trypsinogen activation peptide (TAP)-induced release of high mobility group box-l (HMGB1) from pancreatic acinar cells and how ethyl pyruvate (EP) affects this release. METHODOLOGY: Pancreatic acinar cells from Sprague Dawley rats were divided into control, TAP (administered TAP), and EP (administered TAP and EP) groups...
2017: Open Medicine (Warsaw, Poland)
https://www.readbyqxmd.com/read/28885840/chemical-synthesis-of-rp-and-sp-16-o-17-o-18-o-phosphoenol-pyruvate
#2
Petra Malová Križková, Susanne Prechelmacher, Alexander Roller, Friedrich Hammerschmidt
Enzymes and chirality are intimately associated. For their mechanisms to be studied, chiral substrates are needed as probes. Here, we report a concise synthesis of (RP)- and (SP)-[(16)O,(17)O,(18)O]phosphoenol pyruvate starting from enantiomerically pure (R)-2-chloro-1-phenylethanol, which was transformed into (18)O-labeled 3-methyl-1-phenylbutane-1,3-diol. The diol was reacted with tris(dimethylamino)phosphane and consecutively with H2(17)O to yield a mixture of cyclic H-phosphonates labeled with (17)O and (18)O...
September 8, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28863323/ethyl-pyruvate-reverses-development-of-pseudomonas-aeruginosa-pneumonia-during-sepsis-induced-immunosuppression
#3
Wei Chen, Jie Lian, Jing-Jing Ye, Qing-Fei Mo, Jie Qin, Guang-Liang Hong, Long-Wang Chen, Shao-Ce Zhi, Guang-Ju Zhao, Zhong-Qiu Lu
Sepsis is characterized by an innate immune response and the following immune dysfunction which can increase the emergence of secondary infections. Ethyl pyruvate (EP) has multiple immunoregulation functions in several serious illnesses, such as burn injury, severe sepsis and acute respiratory syndrome. However, little data was shown the effect of EP administration on immunosuppression post-CLP and the following secondary infection. The cecal ligation and puncture (CLP) followed by the induction of Pseudomonas aeruginosa (PA) was used as a clinically relevant two-hit model of sepsis...
August 29, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28858979/mir-195-modulates-oxidative-stress-induced-apoptosis-and-mitochondrial-energy-production-in-human-trophoblasts-via-flavin-adenine-dinucleotide-dependent-oxidoreductase-domain-containing-protein-1-and-pyruvate-dehydrogenase-phosphatase-regulatory-subunit
#4
Hao Wang, Lanmei Zhang, Xuejiang Guo, Yang Bai, Yu-Xia Li, Jiahao Sha, Chun Peng, Yan-Ling Wang, Ming Liu
OBJECTIVE: Preeclampsia is a severe pregnancy-specific syndrome defined as newly onset hypertension and proteinuria. Abnormal placental development has been generally accepted as the initial cause of the disorder. Recently, miR-195 was identified as one of the downregulated small RNAs in preeclamptic placentas. METHODS: The potential targets of miR-195 in human trophoblast cells were screened by isobaric tags for relative and absolute quantification-based mass spectrum analysis...
August 30, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28836378/ethyl-pyruvate-does-not-require-microglia-for-mediating-neuroprotection-after-excitotoxic-injury
#5
Philipp Pieroh, Daniel-Christoph Wagner, Chalid Ghadban, Gerd Birkenmeier, Faramarz Dehghani
AIMS: Ethyl pyruvate (EP) mediates protective effects after neuronal injury. Besides a direct conservation of damaged neurons, the modulation of indigenous glial cells has been suggested as one important mechanism for EP-related neuroprotection. However, the specific contribution of glial cells is still unknown. METHODS: Organotypic hippocampal slice cultures (OHSC) were excitotoxically lesioned by 50 μmol/L N-methyl-D-aspartate (NMDA, for 4 hours) or left untreated...
August 23, 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28755135/macrophage-derived-hmgb1-as-a-pain-mediator-in-the-early-stage-of-acute-pancreatitis-in-mice-targeting-rage-and-cxcl12-cxcr4-axis
#6
Yuhei Irie, Maho Tsubota, Hiroyasu Ishikura, Fumiko Sekiguchi, Yuka Terada, Toshifumi Tsujiuchi, Keyue Liu, Masahiro Nishibori, Atsufumi Kawabata
Extracellular high mobility group box 1 (HMGB1) activates the receptor for advanced glycation end products (RAGE) or Toll-like receptor 4 (TLR4) and forms a heterocomplex with CXCL12 that strongly activates CXCR4, promoting inflammatory and pain signals. In the present study, we investigated the role of HMGB1 in pancreatic pain accompanying cerulein-induced acute pancreatitis in mice. Abdominal referred hyperalgesia accompanying acute pancreatitis occurred within 1 h after 6 hourly injections of cerulein. The anti-HMGB1 neutralizing antibody or recombinant human soluble thrombomodulin (rhsTM), known to inactivate HMGB1, abolished the cerulein-induced referred hyperalgesia, but not pancreatitis itself...
July 28, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28645008/effect-of-microrna-129-5p-targeting-hmgb1-rage-signaling-pathway-on-revascularization-in-a-collagenase-induced-intracerebral-hemorrhage-rat-model
#7
Xin-Long Ma, Shu-Ya Li, Feng Shang
BACKGROUND: This study aimed at exploring the effect of microRNA-129-5p (miR-129-5p) targeting high mobility group box-1 (HMGB1)-receptor for advanced glycation end-products (RAGE) signaling pathway on the revascularization in a collagenase-induced intracerebral hemorrhage (ICH) rat model. METHODS: OX26-pGFAP-IL, an immunoliposome expressing miR-129-5p was constructed. The collagenase-induced ICH rat models were successfully established by 96 Sprague Dawley (SD) rats, which were categorized into the sham group, ICH group, miR-129-5p group, negative control (NC) group, ethyl pyruvate (EP, an inhibitor of HMGB1) group and N-benzyl-4-chloro-N-cyclohe-xylbenzamide (FPS-ZM1, a RAGE receptor antagonist) group...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28606778/hmgb1-promotes-neurovascular-remodeling-via-rage-in-the-late-phase-of-subarachnoid-hemorrhage
#8
Xiaodi Tian, Liang Sun, Dongxia Feng, Qing Sun, Yang Dou, Chenglin Liu, Feng Zhou, Haiying Li, Haitao Shen, Zhong Wang, Gang Chen
High-mobility group box1 (HMGB1) is a nuclear protein widely expressed in the central nervous system. Extracellular HMGB1 serves as a proinflammatory cytokine and contributes to brain injury during the acute stage post-stroke. Recently, increasing evidence has demonstrated beneficial effects of HMGB1 in some types of brain injury, but little is known about its effects during the late phase of subarachnoid hemorrhage (SAH). This study was designed to explore the potential roles and mechanisms of HMGB1 and its receptor, receptor for advanced glycation end-products (Rage), on brain recovery in the late stage of experimental SAH...
June 9, 2017: Brain Research
https://www.readbyqxmd.com/read/28601590/hepatoprotective-effects-of-ethyl-pyruvate-against-ccl4-induced-hepatic-fibrosis-via-inhibition-of-tlr4-nf-%C3%AE%C2%BAb-signaling-and-up-regulation-of-mmps-timps-ratio
#9
Mingxiao Zhang, Xiaosong Hu, Shuai Li, Chen Lu, Juan Li, Yonghua Zong, Wenqian Qi, Huijun Yang
BACKGROUND AND AIM: Liver fibrosis is a worldwide clinical issue. It has been well established that liver fibrosis is characterized of excessive extracellular matrix (ECM) deposition in chronically damaged livers. Accumulating evidences have suggested that ethyl pyruvate (EP) is a potential useful agent for preventing from hepatic injury. The aim of this study was to evaluate the protective effects of the EP against liver fibrosis induced by carbon tetrachloride (CCl4) in rats. METHOD: Rats were randomly divided into control group, CCl4 group and CCl4+EP group, which with and without EP administration...
June 7, 2017: Clinics and Research in Hepatology and Gastroenterology
https://www.readbyqxmd.com/read/28576319/chloroformate-derivatization-for-tracing-the-fate-of-amino-acids-in-cells-and-tissues-by-multiple-stable-isotope-resolved-metabolomics-msirm
#10
Ye Yang, Teresa W-M Fan, Andrew N Lane, Richard M Higashi
Amino acids have crucial roles in central metabolism, both anabolic and catabolic. To elucidate these roles, steady-state concentrations of amino acids alone are insufficient, as each amino acid participates in multiple pathways and functions in a complex network, which can also be compartmentalized. Stable Isotope-Resolved Metabolomics (SIRM) is an approach that uses atom-resolved tracking of metabolites through biochemical transformations in cells, tissues, or whole organisms. Using different elemental stable isotopes to label multiple metabolite precursors makes it possible to resolve simultaneously the utilization of these precursors in a single experiment...
July 11, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28570981/ethyl-pyruvate-alleviates-radiation-induced-lung-injury-in-mice
#11
Baoqing Chen, Feifei Na, Hui Yang, Rui Li, Mengqian Li, Xiaowen Sun, Binbin Hu, Guodong Huang, Jie Lan, He Xu, Ruizhan Tong, Xianming Mo, Jianxin Xue, You Lu
OBJECTIVE: Radiation-induced lung injury (RILI) is a common complication of thoracic cancer radiation therapy. Ethyl pyruvate (EP) was reported to have an ameliorating effect on a variety of systemic inflammation reactions, including acute lung injury. However, the protective effect of EP on RILI has not been explored. MATERIALS/METHODS: RILI was induced by a single thoracic irradiation of 16Gy X-rays in C57BL/6 mice. Mice were divided into four groups: control, radiation, 100mg/kg EP, and 200mg/kg dexamethasone...
August 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28538193/ethyl-pyruvate-protects-pc12-cells-from-oxygen-glucose-deprivation-a-potential-role-in-ischemic-cerebrovascular-disease
#12
Wenbo Li, Jiyu Lou, Liping Wei, Hongying Bai, Yaohui Zhang, Yuqing He
The protective potential of ethyl pyruvate (EP) on neuron has been investigated previously. This study was intended to investigate the effects of EP on the severity of oxygen-glucose deprivation (OGD)-induced injury in neural-like PC12 cells. PC12 cells were exposed to OGD condition with or without EP treatment. Then, cell viability, apoptosis, and the expressions of neurotrophic factors were detected. Further, Sprague-Dawley rats were intravenously administered with 5mg/kg EP for 14 days post-middle cerebral artery occlusion (MCAO)...
August 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28505390/correlation-between-chiral-modifier-adsorption-and-enantioselectivity-in-hydrogenation-catalysis
#13
Yufei Ni, Alexander D Gordon, Florisa Tanicala, Francisco Zaera
Infrared absorption spectroscopy performed in situ at the solid-liquid interface revealed that the adsorption on platinum supported catalysts of 1-(1-naphthyl)-ethylamine, which is used as a chiral modifier in hydrogenation catalysis, occurs through the amine group, not the aromatic ring as is widely believed. Comparisons were performed against a set of related modifier compounds with targeted substitutions to help identify the key moiety involved in the adsorption. It was determined that neither naphthalene-based modifiers without amine groups nor those with tertiary amine moieties are capable of adsorbing on the metal surface to any significant extent...
June 26, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28428710/cma-down-regulates-p53-expression-through-degradation-of-hmgb1-protein-to-inhibit-irradiation-triggered-apoptosis-in-hepatocellular-carcinoma
#14
Jing-Hua Wu, Jia-Pei Guo, Jun Shi, Hui Wang, Lei-Lei Li, Bin Guo, Dian-Xing Liu, Qing Cao, Zhi-Yong Yuan
AIM: To investigate the mechanism of chaperone-mediated autophagy (CMA)-induced resistance to irradiation-triggered apoptosis through regulation of the p53 protein in hepatocellular carcinoma (HCC). METHODS: Firstly, we detected expression of lysosome-associated membrane protein 2a (Lamp-2a), which is the key protein of CMA, by western blot in HepG2 and SMMC7721 cells after irradiation. We further used shRNA Lamp-2a HCC cells to verify the radioresistance induced by CMA...
April 7, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28427942/inhibitory-effects-of-ethyl-pyruvate-on-platelet-aggregation-and-phosphatidylserine-exposure
#15
Wenjin Li, Xinyu Yang, Minyuan Peng, Can Li, Guangfu Mu, Fangping Chen
Ethyl pyruvate (EP) is a stable lipophilic pyruvate derivative. Studies demonstrated that EP shows potent anti-oxidation, anti-inflammatory and anti-coagulant effects. Inflammation and coagulation are closely interacted with platelet activation. However, it is unclear whether EP has anti-platelet effects. Therefore, we investigated the anti-platelet effect of EP in this study in vitro. We found that EP inhibited agonists induced platelets aggregation, ATP release and adhesion to collagen. Flow cytometric analysis revealed that EP inhibited agonist induced platelets PAC-1 binding, as well as P-selectin and CD40L expression...
June 3, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28425958/reactions-of-5-indolizyl-lithium-compounds-with-some-bielectrophiles
#16
Sergey A Rzhevskii, Victor B Rybakov, Victor N Khrustalev, Eugene V Babaev
Abstract: Indolizyl-5-lithium anions react with succinic and phtalic anhidrides giving 1,4-keto acids, with oxallyl chloride giving 1,2-diketone, and with ethyl pyruvate giving 1,2-hydroxyacid. However, with α-halocarbonyl compounds, they react in different ways, forming the products of selective bromination at C-5 (with α-bromo ketones and esters of α-bromo acids) and 5-chloroacetyl indolizines.
April 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28247461/asymmetric-c-alkylation-by-the-s-adenosylmethionine-dependent-methyltransferase-sgvm
#17
Christina Sommer-Kamann, Alexander Fries, Silja Mordhorst, Jennifer N Andexer, Michael Müller
S-Adenosylmethionine-dependent methyltransferases (MTs) play a decisive role in the biosynthesis of natural products and in epigenetic processes. MTs catalyze the methylation of heteroatoms and even of carbon atoms, which, in many cases, is a challenging reaction in conventional synthesis. However, C-MTs are often highly substrate-specific. Herein, we show that SgvM from Streptomyces griseoviridis features an extended substrate scope with respect to the nucleophile as well as the electrophile. Aside from its physiological substrate 4-methyl-2-oxovalerate, SgvM catalyzes the (di)methylation of pyruvate, 2-oxobutyrate, 2-oxovalerate, and phenylpyruvate at the β-carbon atom...
March 27, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28236213/ethyl-pyruvate-attenuates-early-brain-injury-following-subarachnoid-hemorrhage-in-the-endovascular-perforation-rabbit-model-possibly-via-anti-inflammation-and-inhibition-of-jnk-signaling-pathway
#18
Tao Lv, Yi-Feng Miao, Yi-Chao Jin, Shao-Feng Yang, Hui Wu, Jiong Dai, Xiao-Hua Zhang
Early brain injury (EBI) following subarachnoid hemorrhage (SAH) is the main cause to poor outcomes of SAH patients, and early inflammation plays an important role in the acute pathophysiological events. It has been demonstrated that ethyl pyruvate (EP) has anti-inflammatory and neuroprotective effects in various critical diseases, however, the role of EP on EBI following SAH remains to be elucidated. Our study aimed to evaluate the effects of EP on EBI following SAH in the endovascular perforation rabbit model...
April 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28231326/expression-of-glyoxalase-i-is-reduced-in-cirrhotic-livers-a-possible-mechanism-in-the-development-of-cirrhosis
#19
Marcus Hollenbach, Antje Thonig, Sabine Pohl, Cristina Ripoll, Maurice Michel, Alexander Zipprich
BACKGROUND: High concentrations of methylglyoxal (MGO) cause cytotoxiticy via formation of advanced glycation endproducts (AGEs) and inflammation. MGO is detoxificated enzymatically by glyoxalase-I (Glo-I). The aim of this study was to analyze the role of Glo-I during the development of cirrhosis. METHODS: In primary hepatocytes, hepatic stellate cells (pHSC) and sinusoidal endothelial cells (pLSEC) from rats with early (CCl4 8wk) and advanced cirrhosis (CCl4 12wk) expression and activity of Glo-I were determined and compared to control...
2017: PloS One
https://www.readbyqxmd.com/read/28220827/anti-inflammatory-and-anti-excitoxic-effects-of-diethyl-oxopropanamide-an-ethyl-pyruvate-bioisoster-exert-robust-neuroprotective-effects-in-the-postischemic-brain
#20
Hye-Kyung Lee, Il-Doo Kim, Seung-Woo Kim, Hahnbie Lee, Ju-Young Park, Sung-Hwa Yoon, Ja-Kyeong Lee
Ethyl pyruvate (EP) is a simple aliphatic ester of pyruvic acid and has been shown to have robust neuroprotective effects via its anti-inflammatory, anti-oxidative, and anti-apoptotic functions. In an effort to develop novel EP derivatives with greater protective potencies than EP, we generated four EP isosteres, among them the neuroprotective potency of N,N-diethyl-2-oxopropanamide (DEOPA), in which the ethoxy group of EP was replaced with diethylamine, was far greater than that of EP. When DEOPA was administered intravenously (5 mg/kg) to rat middle cerebral artery occlusion (MCAO) model at 6 hrs post-surgery, it suppressed infarct formation, ameliorated neurological and sensory/motor deficits, and inhibited microglial activation and neutrophil infiltrations in the postischemic brain more effectively than EP...
February 21, 2017: Scientific Reports
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