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Ethyl pyruvate

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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
#1
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...
December 2, 2016: 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
#2
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...
December 1, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27904077/synthesis-characterization-and-evaluation-of-thiazolidine-derivatives-of-cysteine-for-suppressing-eumelanin-production
#3
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
#4
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
#5
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
#6
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...
November 16, 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
#7
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
#8
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
#9
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
https://www.readbyqxmd.com/read/27800513/preconditioning-with-ethyl-3-4-dihydroxybenzoate-augments-aerobic-respiration-in-rat-skeletal-muscle
#10
Charu Nimker, Deependra Pratap Singh, Deepika Saraswat, Anju Bansal
Muscle respiratory capacity decides the amount of exertion one's skeletal muscle can undergo, and endurance exercise is believed to increase it. There are also certain preconditioning methods by which muscle respiratory and exercise performance can be enhanced. In this study, preconditioning with ethyl 3,4-dihydroxybenzoate (EDHB), a prolyl hydroxylase domain enzyme inhibitor, has been investigated to determine its effect on aerobic metabolism and bioenergetics in skeletal muscle, thus facilitating boost in physical performance in a rat model...
2016: Hypoxia
https://www.readbyqxmd.com/read/27779688/-retracted-inhibitory-effects-of-ethyl-pyruvate-administration-on-human-gastric-cancer-growth-via-regulation-of-the-hmgb1-rage-and-akt-pathways-in%C3%A2-vitro-and-in%C3%A2-vivo
#11
Jing Zhang, Jin-Shui Zhu, Zhou Zhou, Wei-Xiong Chen, Ni-Wei Chen
Following the publication of this article, an interested reader drew to the attention of the Editorial Board that the above article appeared to contain a series of Figures that featured duplicated data. Following an internal investigation, the Editorial Board reached the conclusion that the allegations of the reader were well-founded. Specifically, the GAPDH bands shown in Figs. 2 and 3 are identical with those in Figs. 4C and 5D, with the exception that the images have been reversed. Furthermore, certain data in Fig...
October 19, 2016: Oncology Reports
https://www.readbyqxmd.com/read/27776698/ethyl-pyruvate-modulates-delayed-paralysis-following-thoracic-aortic-ischemia-reperfusion-in-mice
#12
Bao-Ngoc Nguyen, Hassan Albadawi, Rahmi Oklu, Robert S Crawford, Mitchell P Fink, Richard P Cambria, Michael T Watkins
OBJECTIVE: Delayed paralysis is an unpredictable problem for patients undergoing complex repair of the thoracic/thoracoabdominal aorta. These experiments were designed to determine whether ethyl pyruvate (EP), a potent anti-inflammatory and antioxidant agent, might ameliorate delayed paralysis following thoracic aortic ischemia reperfusion (TAR). METHODS: C57BL6 mice were subjected to 5 minutes of thoracic aortic ischemia followed by reperfusion for up to 48 hours...
November 2016: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/27689918/treatment-response-of-ethyl-pyruvate-in-a-mouse-model-of-chronic-obstructive-pulmonary-disease-studied-by-hyperpolarized-129-xe-mri
#13
Atsuomi Kimura, Yukiko Yamauchi, Shota Hodono, Neil James Stewart, Osamu Hosokawa, Yu Hagiwara, Hirohiko Imai, Hideaki Fujiwara
PURPOSE: The purpose of this work was to investigate disease progression and treatment response in a murine model of chronic obstructive pulmonary disease (COPD) using a preclinical hyperpolarized (129) Xe (HPXe) magnetic resonance imaging (MRI) strategy. METHODS: COPD phenotypes were induced in 32 mice by 10 weeks of exposure to cigarette smoke (CS) and lipopolysaccharide (LPS). Efficacy of ethyl pyruvate (EP), an anti-inflammatory drug, was investigated by administering EP to 16 of the 32 mice after 6 weeks of CS and LPS exposure...
September 30, 2016: Magnetic Resonance in Medicine: Official Journal of the Society of Magnetic Resonance in Medicine
https://www.readbyqxmd.com/read/27624523/synthesis-molecular-modeling-and-sar-study-of-novel-pyrazolo-5-1-f-1-6-naphthyridines-as-cb2-receptor-antagonists-inverse-agonists
#14
Antonio Dore, Battistina Asproni, Alessia Scampuddu, Stefania Gessi, Gabriele Murineddu, Elena Cichero, Paola Fossa, Stefania Merighi, Serena Bencivenni, Gérard A Pinna
Pyrazolo[5,1-f][1,6]naphthyridine-carboxamide derivatives were synthesized and evaluated for the affinity at CB1 and CB2 receptors. Based on the AgOTf and proline-cocatalyzed multicomponent methodology, the ethyl 5-(p-tolyl)pyrazolo[5,1-f][1,6]naphthyridine-2-carboxylate (12) and ethyl 5-(2,4-dichlorophenyl)pyrazolo[5,1-f][1,6]naphthyridine-2-carboxylate (13) intermediates were synthesized from the appropriate o-alkynylaldehydes, p-toluenesulfonyl hydrazide and ethyl pyruvate. Most of the novel compounds feature a p-tolyl (8a-i) or a 2,4-dichlorophenyl (8j) motif at the C5-position of the tricyclic pyrazolo[5,1-f][1,6]naphthyridine scaffold...
November 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27579985/ethyl-pyruvate-combats-human-leukemia-cells-but-spares-normal-blood-cells
#15
Gerd Birkenmeier, Nasr Y A Hemdan, Susanne Kurz, Marina Bigl, Philipp Pieroh, Tewodros Debebe, Martin Buchold, Rene Thieme, Gunnar Wichmann, Faramarz Dehghani
Ethyl pyruvate, a known ROS scavenger and anti-inflammatory drug was found to combat leukemia cells. Tumor cell killing was achieved by concerted action of necrosis/apoptosis induction, ATP depletion, and inhibition of glycolytic and para-glycolytic enzymes. Ethyl lactate was less harmful to leukemia cells but was found to arrest cell cycle in the G0/G1 phase. Both, ethyl pyruvate and ethyl lactate were identified as new inhibitors of GSK-3β. Despite the strong effect of ethyl pyruvate on leukemia cells, human cognate blood cells were only marginally affected...
2016: PloS One
https://www.readbyqxmd.com/read/27567422/effects-of-insulin-combined-with-ethyl-pyruvate-on-inflammatory-response-and-oxidative-stress-in-multiple-organ-dysfunction-syndrome-rats-with-severe-burns
#16
Zhanke Wang, Rongjian Chen, Zhongzhen Zhu, Xiaoyun Zhang, Shiliang Wang
BACKGROUND: Inflammation response and oxidative stress promote the occurrence and development of multiple-organ dysfunction syndrome (MODS). METHODS: Eighty MODS rats with third-degree burns were divided randomly into 4 groups: insulin, ethyl pyruvate (EP), insulin combined with EP, and control. Blood levels of glucose, alanine aminotransferase (ALT), creatine (CRE), creatine kinase (CK), tumor necrosis factor α (TNF-α), high-mobility group box 1 (HMGB-1), malondialdehyde (MDA), and total antioxidant capacity (TAC) before as well as 1, 3, 5, and 7 days after burns were measured...
August 9, 2016: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/27554159/application-of-high-pressure-processing-for-controlling-clostridium-tyrobutyricum-and-late-blowing-defect-on-semi-hard-cheese
#17
Marta Ávila, Natalia Gómez-Torres, David Delgado, Pilar Gaya, Sonia Garde
In this study we evaluated the application of different high pressure (HP) treatments (200-500 MPa at 14 °C for 10 min) to industrial sized semi-hard cheeses on day 7, with the aim of controlling two Clostridium tyrobutyricum strains causing butyric acid fermentation and cheese late blowing defect (LBD). Clostridium metabolism and LBD appearance in cheeses were monitored by sensory (cheese swelling, cracks/splits, off-odours) and instrumental analyses (organic acids by HPLC and volatile compounds by SPME/GC-MS) after 60 days...
December 2016: Food Microbiology
https://www.readbyqxmd.com/read/27441057/attenuation-of-methotrexate-induced-embryotoxicity-and-oxidative-stress-by-ethyl-pyruvate
#18
Gholamreza Najafi, Elham Atashfaraz, Farah Farokhi
BACKGROUND: Methotrexate (MTX), as an anti-folate agent, is widely used in the treatment of rheumatic disorders and malignant tumors, however it damages reproductive sys- tem in mice. The aim of this research was to study the effects of ethyl pyruvate (EP) on embryo development and oxidative stress changes in the testis of mice treated with MTX. MATERIALS AND METHODS: In this experimental study, thirty-two adult male Naval Medical Research Institute mice, with average weight of 26 ± 2 g, were divided into four groups...
July 2016: International Journal of Fertility & Sterility
https://www.readbyqxmd.com/read/27354791/intratracheal-instillation-of-ethyl-pyruvate-nanoparticles-prevents-the-development-of-shunt-flow-induced-pulmonary-arterial-hypertension-in-a-rat-model
#19
Kai Liu, Xiquan Zhang, Guangqing Cao, Yongjun Liu, Chuanzhen Liu, Hourong Sun, Xinyan Pang
PURPOSE: To investigate whether inhalation of ethyl pyruvate (EP) encapsulated with poly(ethylene glycol)-block-lactide/glycolide copolymer nanoparticles (EP-NPs) can prevent the development of shunt-flow-induced hyperkinetic pulmonary arterial hypertension (PAH) in a rat model. MATERIALS AND METHODS: Rats were separated into five groups: blank (ie, no treatment after shunt flow), normal control (ie, no shunt flow or treatment), EP-NP instillation, EP-only instillation, and vehicle...
2016: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/27353589/molecular-docking-and-simulation-studies-of-gustatory-receptor-of-aedes-aegypti-a-potent-drug-target-to-distract-host-seeking-behaviour-in-mosquitoes
#20
Krishna Kant Gupta, Guneswar Sethi, Manikandan Jayaraman
BACKGROUND & OBJECTIVES: It is well reported that exhaled CO 2 and skin odour from human being assist female mosquitoes to locate human host. Basically, the receptors for this activity are expressed in cpA neurons. In both Aedes aegypti and Anopheles gambiae, this CO 2-sensitive olfactory neuron detects myriad number of chemicals present in human skin. Therefore, manipulation of gustatory receptors housing these neurons may serve as important targets for behavioural intervention. The study was aimed towards virtual screening of small molecules in the analyzed conserved active site residues of gustatory receptor and molecular dynamics simulation study of optimum protein-ligand complex to identify a suitable lead molecule for distracting host-seeking behaviour of mosquitoes...
April 2016: Journal of Vector Borne Diseases
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