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Ethyl pyruvate

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https://www.readbyqxmd.com/read/28247461/asymmetric-c-alkylation-by-the-s-adenosylmethionine-dependent-methyltransferase-sgvm
#1
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 1, 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
#2
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...
February 25, 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
#3
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
#4
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
https://www.readbyqxmd.com/read/28186988/hmgb1-targeting-by-ethyl-pyruvate-suppresses-malignant-phenotype-of-human-mesothelioma
#5
Laura Pellegrini, Jiaming Xue, David Larson, Sandra Pastorino, Sandro Jube, Kelly H Forest, Zeyana Salim Saad-Jube, Andrea Napolitano, Ian Pagano, Vishal S Negi, Marco E Bianchi, Paul Morris, Harvey I Pass, Giovanni Gaudino, Michele Carbone, Haining Yang
Human malignant mesothelioma (MM) is an aggressive cancer linked to asbestos and erionite exposure. We previously reported that High-Mobility Group Box-1 protein (HMGB1), a prototypic damage-associated molecular pattern, drives MM development and sustains MM progression. Moreover, we demonstrated that targeting HMGB1 inhibited MM cell growth and motility in vitro, reduced tumor growth in vivo, and prolonged survival of MM-bearing mice. Ethyl pyruvate (EP), the ethyl ester of pyruvic acid, has been shown to be an effective HMGB1 inhibitor in inflammation-related diseases and several cancers...
February 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28098908/protective-effects-of-ethyl-pyruvate-on-lipopolysaccharide%C3%A2-induced-acute-lung-injury-through-inhibition-of-autophagy-in-neutrophils
#6
Qingteng Zhu, Hui Wang, Hairong Wang, Yong Luo, Yang Yu, Qirong Du, Aihua Fei, Shuming Pan
Among a number of clinical factors, bacterial infection is one of the most common causes of acute lung injury (ALI), a serious complication that carries a high risk of mortality (~40%). During the process of ALI, intense local and systemic inflammation is elicited, which exacerbates the injury. Neutrophil infiltration into airspace is observed in early stage of ALI, and is required for the full development of ALI through an array of mechanisms, including the release of granule contents and the production of pro‑inflammatory cytokines, due to the overactivation of complement and cytokines...
January 13, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28069436/streptozotocin-causes-neurotoxic-effect-in-cultured-cerebellar-granule-neurons
#7
Elisaveta E Genrikhs, Elena V Stelmashook, Sergey A Golyshev, Olga P Aleksandrova, Nickolay K Isaev
Streptozotocin (STZ) is a glucosamine-nitrosourea compound used for experimental simulation of sporadic Alzheimer's disease at intracerebroventricular administration in vivo. The studies of STZ influence on neurons of central nervous system performed on the primary cultures are practically absent. We have shown the application of STZ (1-5mM) in primary culture for 48h induced strong dose-dependent death in cultured cerebellar granule neurons. This toxic effect was decreased by pyruvate, insulin partially. Using the indicator Fluo-4 AM for measurements of intracellular calcium ions and tetramethylrhodamine ethyl ester (TMRE) for detection of changes of mitochondrial membrane potential in live cells we have shown that 5 h-exposure to STZ induced intensive increase of Fluo-4 and decrease TMRE fluorescence in neurons...
January 6, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28019093/creatine-and-creatine-forms-intended-for-sports-nutrition
#8
REVIEW
Susanne Andres, Rainer Ziegenhagen, Iris Trefflich, Sophie Pevny, Katharina Schultrich, Hans Braun, Wilhelm Schänzer, Karen Ildico Hirsch-Ernst, Bernd Schäfer, Alfonso Lampen
Creatine is a popular ergogenic supplement in sports nutrition. Yet, supplementation of creatine occasionally caused adverse effects such as gastrointestinal complaints, muscle cramps and an increase in body weight. Creatine monohydrate has already been evaluated by different competent authorities and several have come to the conclusion that a daily intake of 3 g creatine per person is unlikely to pose safety concerns, focusing on healthy adults with exclusion of pregnant and breastfeeding women. Possible vulnerable subgroups were also discussed in relation to the safety of creatine...
December 25, 2016: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28012822/hmgb1-rage-axis-promotes-autophagy-and-protects-keratinocytes-from-ultraviolet-radiation-induced-cell-death
#9
Kuanhou Mou, Wei Liu, Dan Han, Pan Li
BACKGROUND: The primary cause of skin cancer is ultraviolet (UV) light from the sun. Keratinocytes are the predominant cell type in the epidermis and form a barrier against environmental damage, especially from UV light irradiation. Autophagy is a self-digestion mechanism for energy homeostasis at critical times during development and as a response to stress. High-mobility group protein 1 (HMGB1) is a highly conserved nuclear protein that is associated with cell autophagy. OBJECTIVE: We investigated the role of HMGB1 in keratinocytes exposed to UV irradiation and its regulation of keratinocyte autophagy...
March 2017: Journal of Dermatological Science
https://www.readbyqxmd.com/read/27995262/ethyl-pyruvate-has-anti-apoptotic-and-myocardial-protective-effects-after-regional-ischaemia-reperfusion-myocardial-damage-in-an-in-vivo-rat-model
#10
Haeng Seon Shim, Jeong Heon Park, Yeon A Kim, Jeong Yeol Han, Miyeong Park, Yun Gyu Song, Joon Soo Kim, Il-Woo Shin
INTRODUCTION: The integration of reactive oxygen species is strongly associated with important pathophysiological mechanisms that mediate myocardial ischaemia/reperfusion (I/R) damage. Pyruvate is an efficacious scavenger of reactive oxygen species and a previous study has shown that ethyl pyruvate (EP) has a myocardial protective effect against regional I/R damage in an in vivo rat model. The purpose of this study was to determine whether the myocardial protective effect of EP is associated with anti-apoptosis...
December 20, 2016: Singapore Medical Journal
https://www.readbyqxmd.com/read/27959427/inhibiting-the-cytoplasmic-location-of-hmgb1-reverses-cisplatin-resistance-in-human-cervical-cancer-cells
#11
Jiyi Xia, Xiaolan Yu, Xueqin Song, Gang Li, Xiguang Mao, Yujiao Zhang
Cervical cancer is the fourth most common malignancy in women worldwide, and resistance to chemotherapy drugs is the biggest obstacle in the treatment of cervical cancers. In the present study, the molecular mechanisms underlying cisplatin resistance in human cervical cancer cells were investigated. When human cervical cancer cells were treated with 10 µg/ml of cisplatin for 24 and 48 h, high mobility group box 1 (HMGB1) protein expression levels significantly increased in a time‑dependent manner. Comparisons between cisplatin‑sensitive HeLa cells and cisplatin‑resistant HeLa/DDP cells revealed higher levels of HMGB1 in HeLa/DDP cells than in HeLa cells...
January 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27919624/metabolic-fate-of-glucose-in-rats-with-traumatic-brain-injury-and-pyruvate-or-glucose-treatments-a-nmr-spectroscopy-study
#12
Katsunori Shijo, Richard L Sutton, Sima S Ghavim, Neil G Harris, Brenda L Bartnik-Olson
Administration of sodium pyruvate (SP; 9.08 μmol/kg, i.p.), ethyl pyruvate (EP; 0.34 μmol/kg, i.p.) or glucose (GLC; 11.1 μmol/kg, i.p.) to rats after unilateral controlled cortical impact (CCI) injury has been reported to reduce neuronal loss and improve cerebral metabolism. In the present study these doses of each fuel or 8% saline (SAL; 5.47 nmoles/kg) were administered immediately and at 1, 3, 6 and 23 h post-CCI. At 24 h all CCI groups and non-treated Sham injury controls were infused with [1,2 (13)C] glucose for 68 min (13)C nuclear magnetic resonance (NMR) spectra were obtained from cortex + hippocampus tissues from left (injured) and right (contralateral) hemispheres...
January 2017: Neurochemistry International
https://www.readbyqxmd.com/read/27916421/protective-potential-of-averrhoa-bilimbi-fruits-in-ameliorating-the-hepatic-key-enzymes-in-streptozotocin-induced-diabetic-rats
#13
Surya B Kurup, Mini S
BACK GROUND: Diabetes is a mutifactorial disease which leads to several complications. Currently available drug regimens for management of diabetes have certain drawbacks. Need for safer and effective medicines from natural sources having potent antidiabetic activity. Averrhoa bilimbi Linn. (Oxalidaceae) is a medicinal plant and is reported to possess hypoglycemic activity. OBJECTIVE: To investigate the antidiabetic potential of Averrhoa bilimbi fruit extract in streptozotocin-induced diabetic rats...
January 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27904077/synthesis-characterization-and-evaluation-of-thiazolidine-derivatives-of-cysteine-for-suppressing-eumelanin-production
#14
Yusuke Amino, Yoshinobu Takino, Megumi Kaneko, Fumie Ookura, Mai Yamamoto, Tatsuki Kashiwagi, Keiji Iwasaki
In the pathway of melanin biosynthesis, cysteine (Cys) is utilized for the synthesis of pheomelanin. Accordingly, Cys is considered to suppress the formation of brown-black eumelanin. Although attempts have been made to utilize Cys and its derivatives as skin-whitening agents, their instability and odor hinders their application as a cosmetic agent. Herein, N-acetyl-2-methylthiazolidine-2,4-dicarboxylic acid ethyl ester (AcCP2Et) was proposed as a candidate for a stable and prolonged-release derivative of Cys to inhibit dopachrome formation after its degradation in melanocytes...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27889435/role-of-hmgb1-translocation-to-neuronal-nucleus-in-rat-model-with-septic-brain-injury
#15
Yafei Li, Xihong Li, Yi Qu, Jichong Huang, Tingting Zhu, Fengyan Zhao, Shiping Li, Dezhi Mu
High-mobility Group Box-1 (HMGB1) is a central late proinflammatory cytokine that triggers the inflammatory response during sepsis. However, whether HMGB1 is involved in the pathogenesis of septic brain damage is unknown. In this study, we investigated the role of HMGB1 in regulating brain injury in a rat model of sepsis. Wistar rats were subjected to cecal ligation and puncture (CLP) to induce septic brain injury. Hematoxylin and eosin staining was used to detect pathological changes in the cortex. The cellular localization of HMGB1 was determined using immunostaining...
November 23, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27882138/impact-of-ethyl-pyruvate-on-adriamycin-induced-cardiomyopathy-in-rats
#16
Menglin Liu, Menglong Wang, Jianfang Liu, Zhen Luo, Lei Shi, Ying Feng, Li Li, Lin Xu, Jun Wan
Ethyl pyruvate (EP), a derivative of pyruvic acid, is known to have protective effects against ischemic cardiomyopathy and other disorders. However, little is known about its role in Adriamycin (ADR)-induced cardiomyopathy. The present study was designed to investigate the impact of EP on ADR-induced cardiomyopathy in an animal model. Sixty male Sprague-Dawley (SD) rats were divided into four groups: Normal control, EP, ADR and ADR + EP groups (n=15/group). Rats in the ADR and ADR + EP groups were treated with ADR (2...
November 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27865166/ethyl-pyruvate-inhibits-the-acetylation-and-release-of-hmgb1-via-effects-on-sirt1-stat-signaling-in-lps-activated-raw264-7-cells-and-peritoneal-macrophages
#17
Young Min Kim, Eun Jung Park, Jung Hwan Kim, Sang Won Park, Hye Jung Kim, Ki Churl Chang
High mobility group box 1 (HMGB1), a cytokine present in the late phase of sepsis, may be a potential target for the treatment of sepsis. For HMGB1 to be actively secreted from macrophages during infections, it must be post-translationally modified. Although ethyl pyruvate (EP), a simple aliphatic ester derived from pyruvic acid, has been shown to inhibit the release of HMGB1 in lipopolysaccharide (LPS)-treated RAW 264.7 cells, the underlying mechanism(s) are not yet clear. We investigated the hypothesis that the upregulation of SIRT1 by EP might promote the deacetylation of HMGB1, which reduces HMGB1 release in LPS-activated macrophages...
December 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27825779/glutamine-is-required-for-red-spotted-grouper-nervous-necrosis-virus-replication-via-replenishing-the-tricarboxylic-acid-cycle
#18
Muhammad Asim, Sanjie Jiang, Lizhu Yi, Wenjie Chen, Lindan Sun, Lijuan Zhao, Muhammad Nasir Khan Khattak, Jiagang Tu, Li Lin
Glutamine, one of the most important nutrients, plays a vital role in carbon metabolic pathway and has been reported to be required for the replication of several human DNA viruses. However, whether glutamine is required for RNA virus replication and the related mechanism remains elusive. Nervous necrosis virus (NNV), a positive-stranded RNA virus, can infect a number of important aquatic species and has caused great economic losses in aquaculture industry worldwide. In this study, the effects of glutamine on red-spotted grouper nervous necrosis virus (RGNNV) replication were investigated...
January 2, 2017: Virus Research
https://www.readbyqxmd.com/read/27816798/the-reactivity-of-lactyl-oxythiamin-implies-the-role-of-the-amino-pyrimidine-in-thiamin-catalyzed-decarboxylation
#19
Yasaman Heidari, Graeme W Howe, Ronald Kluger
It has previously been established that the deprotonated amino substituent of the pyrimidine of thiamin diphosphate (ThDP) acts as an internal base to accept the C2H of the thiazolium in ThDP-dependent enzymes. The amino group has also been implicated in assisting the departure of the aldehydic product formed after loss of CO2 from ketoacid substrates. However, the potential role for the pyrimidine amino group in the key decarboxylation step has not been assessed. Oxythiamin contains a hydroxyl group in place of the pyrimidine amino group in thiamin, providing a basis for comparison of reactivity...
October 31, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27807393/corrigendum-to-ethyl-pyruvate-ameliorates-hepatic-ischemia-reperfusion-injury-by-inhibiting-intrinsic-pathway-of-apoptosis-and-autophagy
#20
Miao Shen, Jie Lu, Weiqi Dai, Fan Wang, Ling Xu, Kan Chen, Lei He, Ping Cheng, Yan Zhang, Chengfen Wang, Dong Wu, Jing Yang, Rong Zhu, Huawei Zhang, Yingqun Zhou, Chuanyong Guo
[This corrects the article DOI: 10.1155/2013/461536.].
2016: Mediators of Inflammation
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