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Ethyl pyruvate

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
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
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
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
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
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
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
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
Suha Turkmen, Ozgen Cekic Gonenc, Yunus Karaca, Ahmet Mentese, Selim Demir, Ercument Beyhun, Aynur Sahin, Abdulkadir Gunduz, Esin Yulug, Suleyman Turedi
INTRODUCTION: Reperfusion therapies play an important role in early-period treatment for patients presenting to the emergency department due to stroke. However, the ischemia-reperfusion injury that may occur with reperfusion must then be considered. The purpose of this study was to determine the effectiveness of N-acetylcysteine (NAC) and ethyl pyruvate in preventing ischemia-reperfusion injury. METHOD: This study is a randomized, controlled experimental study. In group 1, rats' left main carotid arteries were clamped...
September 2016: American Journal of Emergency Medicine
Dong-Woo Lim, Hyuck Kim, Ju-Yeon Park, Jai-Eun Kim, Jin-Young Moon, Sun-Dong Park, Won-Hwan Park
BACKGROUND: Medicinal herb-derived drug development has become important in the relief of liver pathology. Amomun cardamomum is traditionally used therapeutically in Korea to treat various human ailments including dyspepsia, hiccupping, and vomiting. We investigated to assess the protective effect of A. cardamomum on carbon tetrachloride (CCl4)-induced liver damage through antioxidant activity in hepatic tissues of Sprague-Dawley rats. METHODS: Antioxidant properties of different fractions from A...
2016: BMC Complementary and Alternative Medicine
Ali Akbar Mozafari, Rasoul Shahrooz, Abbas Ahmadi, Hassan Malekinjad, Karim Mardani
The aim of the present study was to assess the protective effect of ethyl pyruvate (EP) on sperm quality parameters, testosterone level and malondialdehyde (MDA) in phenylhydrazine (PHZ) treated mice. For this purpose, 32 NMRI mice with the age range of 8 to 10 weeks, weight average 26.0 ± 2.0 g, were randomly divided into four equal groups. The control group (1) received normal saline (0. 1 mL per day) by intraperitoneal injection (IP). Group 2 (PHZ group) was treated with initial dose of PHZ (8 mg 100 g(-1), IP) followed by 6 mg 100 g(-1) , IP every 48 hr...
2016: Veterinary Research Forum
Zahra Bakhtiary, Rasoul Shahrooz, Abbas Ahmadi, Farhad Soltanalinejad
BACKGROUND: Cyclophosphamide (CP) is a chemotherapy drug which causes deleterious effects on testicular tissue and increases free radicals in the body. The aim of this study is to investigate the protective effects of ethyl pyruvate (EP) on testicular improvement in CP treated animals. MATERIALS AND METHODS: In this experimental study, 15 male mice (6-8 weeks) were divided into 3 groups. The control group received normal saline (0.1 ml/day), intraperitoneal (IP), CP group received CP (15 mg/kg/week, IP), and the CP+EP group received EP (40 mg/kg/day, IP) plus CP...
April 2016: International Journal of Fertility & Sterility
Turkmen Suha, Mutlu Asli, Sahin Aynur, Karaca Yunus, Mentese Ahmet, Demir Selim, Yulug Esin, Tatli Ozgur, Neziha Senem Ari, Turedi Süleyman
OBJECTIVES: This study was planned as a histopathologic evaluation of the effectiveness of ethyl pyruvate (EP) and N-acetylcysteine (NAC) in reducing electric burn-related organ damage in an experimental model. METHODS: Four groups of 7 female Wister rats were established. The first was a sham group, the second an electrical burn control group receiving 600 V, the third group received NAC therapy of 20 mg/kg 1 hour after 600 V electrical burn, and the fourth group received 50 mg/kg EP 1 hour after 600 V electrical burn...
July 2016: American Journal of Emergency Medicine
Rong Fang, Xiaojun Zheng, Mei Zhang
BACKGROUND: Previous studies have demonstrated the neuroprotective effects of ethyl pyruvate in central nervous system (CNS) diseases. However, whether ethyl pyruvate attenuates early brain injury after subarachnoid hemorrhage (SAH) remains unknown. This study was conducted to investigate the potential effects of ethyl pyruvate on early brain injury induced by SAH and explore the underlying mechanisms. METHODS: Eighty-eight male Sprague-Dawley rats were used. An SAH model was induced by endovascular perforation...
June 2016: Acta Neurochirurgica
Nobuhiro Moro, Sima S Ghavim, Neil G Harris, David A Hovda, Richard L Sutton
Experimental traumatic brain injury (TBI) is known to produce an acute increase in cerebral glucose utilization, followed rapidly by a generalized cerebral metabolic depression. The current studies determined effects of single or multiple treatments with sodium pyruvate (SP; 1000mg/kg, i.p.) or ethyl pyruvate (EP; 40mg/kg, i.p.) on cerebral glucose metabolism and neuronal injury in rats with unilateral controlled cortical impact (CCI) injury. In Experiment 1 a single treatment was given immediately after CCI...
July 1, 2016: Brain Research
Ying Yu, Yong Yu, Ming Liu, Peng Yu, Guijian Liu, Yuxi Liu, Yangang Su, Hong Jiang, Ruizhen Chen
Inflammation plays important roles in the pathogenesis of coxsackievirus B3 (CVB3)-induced acute viral myocarditis (AVMC). Ethyl pyruvate (EP) has been shown to be an anti-inflammatory agent. High mobility group box 1 (HMGB1)/receptor for advanced glycation end product (RAGE)/nuclear factor (NF)-ΚB pathway has close relation with inflammatory responses. Here, we investigated the effects of EP on CVB3-induced AVMC and potential mechanisms. The mice with AVMC were treated with EP (40 or 80 mg/kg/day) from day 5 to day 7 post-infection...
2016: SpringerPlus
Tarik Artis, A Seda Artis, Ergin Arslan, Fatih Mutlu, Abdurrahman Akay, Kemal Deniz
OBJECTIVE: Postoperative adhesions are among the major causes of morbidity and mortality following abdominal surgery. As an antioxidant and antiinflamatory agent, the potential effect of ethyl pyruvate on adhesion prevention has not been clearly studied. We aimed to investigate the possible anti-adhesive effect of ethyl pyruvate compared with an effective barrier membrane, Seprafilm, in a rat cecal abrasion model. MATERIALS AND METHODS: Male Wistar albino rats separated into three adhesion model groups (n = 8, each) with applications of different agents during surgery: control (intraperitoneal normal saline), Seprafilm group (intraperitoneal Seprafilm), and Ethyl pyruvate group (40 mg/kg intraperitoneal ethyl pyruvate)...
October 2016: Journal of Investigative Surgery: the Official Journal of the Academy of Surgical Research
Mei Huang, Sabina Paglialunga, Julia M-K Wong, Monica Hoang, Renjitha Pillai, Jamie W Joseph
Type 2 diabetes is associated with impaired nutrient-regulated anaplerosis and insulin secretion in pancreatic β-cells. One key anaplerotic substrate that may be involved in regulating insulin release is α-ketoglutarate (αKG). Since prolyl hydroxylase domain proteins (PHDs) can metabolize cytosolic αKG, we sought to explore the role of this enzyme in the regulation of β-cell function. The oxygen-sensing PHDs regulate the stability of hypoxia-inducible factor 1α (HIF1α) as well as other proline-containing proteins by catalyzing the hydroxylation of proline residues...
March 2016: Physiological Reports
Hongjun Kang, Zhi Mao, Yan Zhao, Ting Yin, Qing Song, Liang Pan, Xin Hu, Jie Hu, Feihu Zhou
BACKGROUND: Ethyl pyruvate (EP) is a derivative of pyruvic acid that has been demonstrated to be a potential scavenger of reactive oxygen species as well as an anti-inflammatory agent. In this study, we investigated the protective effects of EP and its role in regulating the energy metabolism in the livers of cecal-ligation-and-puncture-induced septic mice. METHODS: The animals were treated intraperitoneally with 0.2 mL of Ringer's lactate solution or an equivalent volume of Ringer's lactate solution containing EP immediately after cecal ligation and puncture...
2016: Therapeutics and Clinical Risk Management
Yon-Suk Kim, Eun-Kyung Kim, Jin-Woo Hwang, Il-Bok Seo, Jae-Hyuk Jang, Sangkeun Son, Jae-Hyun Jeong, Sang-Ho Moon, Byong-Tae Jeon, Pyo-Jam Park
The ethanolic extract of Trapa japonica pericarp (TJP) and its various fractions were evaluated for their antioxidant potential. The ethyl acetate fraction (EF) from TJP exhibited significant antioxidant and protective effects against tert-butylhydroperoxide (t-BHP)-induced oxidative damage in vitro and in vivo. In vitro experimental results showed that the EF suppressed t-BHP-induced damage in Chang cells by inhibiting reactive oxygen species generation and regulating the mitochondrial membrane potential. Furthermore, western blot analysis showed that the EF effectively inhibited t-BHP-induced apoptosis by suppressing caspase-3, caspase-7, caspase-8, and caspase-9...
March 2016: Food & Function
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