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https://www.readbyqxmd.com/read/27906635/a-specific-inhibitor-of-lactate-dehydrogenase-overcame-the-resistance-toward-gemcitabine-in-hypoxic-mesothelioma-cells-and-modulated-the-expression-of-the-human-equilibrative-transporter-1
#1
Elisa Giovannetti, Leticia G Leon, Valentina E Gómez, Paolo A Zucali, Filippo Minutolo, Godefridus J Peters
Malignant pleural mesothelioma (MPM) is a very hypoxic malignancy, and hypoxia has been associated with resistance towards gemcitabine. The muscle-isoform of lactate dehydrogenase (LDH-A) constitutes a major checkpoint for the switch to anaerobic glycolysis. Therefore we investigated the combination of a new LDH-A inhibitor (NHI-1) with gemcitabine in MPM cell lines. Under hypoxia (O2 tension of 1%) the cell growth inhibitory effects of gemcitabine, were reduced, as demonstrated by a 5- to 10-fold increase in IC50s...
December 2016: Nucleosides, Nucleotides & Nucleic Acids
https://www.readbyqxmd.com/read/27894810/na-ca-2-exchanger-1-inhibition-abolishes-ischemic-tolerance-induced-by-ischemic-preconditioning-in-different-cardiac-models
#2
Pasqualina Castaldo, Maria Loredana Macrì, Vincenzo Lariccia, Alessandra Matteucci, Marta Maiolino, Santo Gratteri, Salvatore Amoroso, Simona Magi
Ca(2+)-handling disturbances play an important role in the genesis of myocardial ischemia/reperfusion (I/R) injury. Ischemic preconditioning (IPC) is a powerful strategy to induce tolerance against subsequent ischemic episodes. IPC signaling pathways may be triggered by Ca(2+) ion. Since Na(+)/Ca(2+) exchanger 1 (NCX1) participates in modulating intracellular Ca(2+) homeostasis, here we further defined its role in I/R and investigated its potential involvement in IPC-induced cardioprotection. In isolated ventricular cardiomyocytes, perfused rat heart and H9c2 cardiomyoblasts, I/R produced a significant cell injury, assessed by measuring extracellular lactate dehydrogenase (LDH) and, for the whole heart, also by estimating myocardial infarct size area...
November 25, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27889750/metformin-protects-neurons-against-oxygen-glucose-deprivation-reoxygenation-induced-injury-by-down-regulating-mad2b
#3
Xianfang Meng, Guangpin Chu, Zhihua Yang, Ping Qiu, Yue Hu, Xiaohe Chen, Wenpeng Peng, Chen Ye, Fang-Fang He, Chun Zhang
BACKGROUND/AIMS: Metformin, the common medication for type II diabetes, has protective effects on cerebral ischemia. However, the molecular mechanisms are far from clear. Mitotic arrest deficient 2-like protein 2 (MAD2B), an inhibitor of the anaphase-promoting complex (APC), is widely expressed in hippocampal and cortical neurons and plays an important role in mediating high glucose-induced neurotoxicity. The present study investigated whether metformin modifies the expression of MAD2B and to exert its neuroprotective effects in primary cultured cortical neurons during oxygen-glucose deprivation/reoxygenation (OGD/R), a widely used in vitro model of ischemia/reperfusion...
November 11, 2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27864013/factors-predictive-of-response-disease-progression-and-overall-survival-after-dabrafenib-and-trametinib-combination-treatment-a-pooled-analysis-of-individual-patient-data-from-randomised-trials
#4
Georgina V Long, Jean-Jacques Grob, Paul Nathan, Antoni Ribas, Caroline Robert, Dirk Schadendorf, Stephen R Lane, Carmen Mak, Philippe Legenne, Keith T Flaherty, Michael A Davies
BACKGROUND: Dabrafenib plus trametinib treatment provides significant benefits over BRAF-inhibitor monotherapy in patients with BRAF(V600E)-mutant or BRAF(V600K)-mutant advanced melanoma; however, in many patients the disease progresses, leading to death. With many treatment options available, understanding clinical factors that predict long-term response and survival for treatments is important for optimisation of patient management. We aimed to identify clinical factors associated with long-term response and survival using pooled data from randomised trials of dabrafenib plus trametinib in patients with metastatic BRAF-mutant melanoma...
November 15, 2016: Lancet Oncology
https://www.readbyqxmd.com/read/27861613/non-serotonergic-neurotoxicity-by-mdma-ecstasy-in-neurons-derived-from-mouse-p19-embryonal-carcinoma-cells
#5
Dina Popova, Andréas Forsblad, Sanaz Hashemian, Stig O P Jacobsson
3,4-methylenedioxymethamphetamine (MDMA; ecstasy) is a commonly abused recreational drug that causes neurotoxic effects in both humans and animals. The mechanism behind MDMA-induced neurotoxicity is suggested to be species-dependent and needs to be further investigated on the cellular level. In this study, the effects of MDMA in neuronally differentiated P19 mouse embryonal carcinoma cells have been examined. MDMA produces a concentration-, time- and temperature-dependent toxicity in differentiated P19 neurons, as measured by intracellular MTT reduction and extracellular LDH activity assays...
2016: PloS One
https://www.readbyqxmd.com/read/27858860/antagonistic-effects-of-endostatin-vascular-endothelial-growth-inhibitor-chimeric-recombinant-adenovirus-on-homocysteine-induced-vascular-endothelial-cells-injury-in-vitro-and-in-vivo
#6
Zhen-Tian Cui, Jian-Ping Liu, Jian-Min Yao
BACKGROUND: The study is inclined to investigate the antagonistic effects of endostatin-vascular endothelial growth inhibitor chimeric recombinant adenovirus (Ad-hENDO-VEGI) on homocysteine (Hcy)-induced vascular endothelial cells (VECs) injury in vitro and in vivo. METHODS: Human VECs cell line ECV304 was selected and infected with Ad-hENDO-VEGI. The LDH leakage, SOD activity, and MDA levels were measured by the automatic biochemical analyzer. Cell survival rate was counted by Trypanblau dying...
November 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27856430/glycolysis-and-oxidative-phosphorylation-are-essential-for-purinergic-receptor-mediated-angiogenic-responses-in-vasa-vasorum-endothelial-cells
#7
Martin Lapel, Philip Weston, Derek Strassheim, Vijaya Karoor, Nana Burns, Taras Lyubchenko, Petr Paucek, Kurt R Stenmark, Evgenia V Gerasimovskaya
Angiogenesis is an energy demanding process, however, the role of cellular energy pathways and their regulation by extracellular stimuli, especially extracellular nucleotides, remain largely unexplored. Using metabolic inhibitors of glycolysis (2-deoxyglucose, 2-DG) and oxidative phosphorylation (oligomycin, rotenone, and FCCP) we demonstrate that glycolysis and OXPHOS are both essential for angiogenic responses of vasa vasorum endothelial cell (VVEC). Treatment with P2R agonists, ATP and MeSADP, but not P1 receptor agonist, adenosine, increased glycolytic activity in VVEC (measured by extracellular acidification rate and lactate production)...
November 16, 2016: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/27853287/pyroptosis-of-salmonella-typhimurium-infected-macrophages-was-suppressed-and-elimination-of-intracellular-bacteria-from-macrophages-was-promoted-by-blocking-qsec
#8
Zhi Li, Qing Zheng, Xiaoyan Xue, Xin Shi, Ying Zhou, Fei Da, Di Qu, Zheng Hou, Xiaoxing Luo
QseC is a membrane-bound histidine sensor kinase found in Gram-negative pathogens and is involved in the regulation of bacterial virulence. LED209, a QseC-specific inhibitor, significantly inhibits the virulence of several pathogens and partially protects infected mice from death by blocking QseC. However, the mechanism of its antibacterial effects remains unclear. In this experiment, a Salmonella Typhimurium (S. Typhimurium) and macrophage co-culture system was utilized to investigate possible mechanisms underlying the antimicrobial effects of the QseC inhibitor...
November 17, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27830023/over-expression-of-heat-shock-protein-70-protects-mice-against-lung-ischemia-reperfusion-injury-through-sirt1-ampk-enos-pathway
#9
Shumei Liu, Junping Xu, Chunfang Fang, Chunjing Shi, Xin Zhang, Bo Yu, Yantong Yin
Lung ischemia/reperfusion injury (LIRI) usually occurs during in lung transplantation and extracorporeal circulation operation and may develop into pulmonary infections, acute rejection and bronchiolitis obliterans syndrome. Recent studies have discovered the protective effect of heat shock protein 70 (HSP70) on various types of injuries. In the present study, we firstly explore the role of over-expressed HSP70 on the protection against LIRI. Lung Wet/Dry (W/D) ratio, biomarkers in the bronchoalveolar lavage fluid (BALF), lung histological changes and apoptosis markers, oxidative products and proinflammatory cytokines in the lung tissues were analyzed...
2016: American Journal of Translational Research
https://www.readbyqxmd.com/read/27827510/synthesis-of-natural-urolithin-m6-a-galloflavin-mimetic-as-a-potential-inhibitor-of-lactate-dehydrogenase-a
#10
Sebastiano Rupiani, Laura Guidotti, Marcella Manerba, Lorenza Di Ianni, Elisa Giacomini, Federico Falchi, Giuseppina Di Stefano, Marinella Roberti, Maurizio Recanatini
Glycolysis is the main route for energy production in tumors. LDH-A is a key enzyme of this process and its inhibition represents an attractive strategy to hamper cancer cell metabolism. Galloflavin is a reliable LDH-A inhibitor as previously identified by us; however, its poor physicochemical properties and chemical tractability render it unsuitable for further development. Therefore, a rational design was undertaken with the aim to reproduce the pharmacophore of galloflavin on simpler, potentially more soluble and synthetic accessible scaffolds...
November 9, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27826898/collective-cell-migration-of-thyroid-carcinoma-cells-a-beneficial-ability-to-override-unfavourable-substrates
#11
Liudmila Lobastova, Dominik Kraus, Alexander Glassmann, Dilaware Khan, Christian Steinhäuser, Christina Wolff, Nadine Veit, Jochen Winter, Rainer Probstmeier
PURPOSE: Tumor cell invasion and metastasis are life threatening events. Invasive tumor cells tend to migrate as collective sheets. In the present in vitro study we aimed to (i) assess whether collective tumor cells gain benefits in their migratory potential compared to single cells and (ii) to identify its putative underlying molecular mechanisms. METHODS: The migratory potential of single and collective carcinoma cells was assessed using video time lapse microscopy and cell migration assays in the absence and presence of seven potential gap junction inhibitors or the Rac1 inhibitor Z62954982...
November 8, 2016: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/27809355/aliskiren-protects-against-myocardial-ischemia-reperfusion-injury-via-an-endothelial-nitric-oxide-synthase-dependent-manner
#12
Yu Chen, Guoliang Meng, Wenli Bai, Yan Ma, Liping Xie, Naila Altaf, Yanning Qian, Yi Han, Yong Ji
Aliskiren, a direct renin inhibitor, was shown potent ability to attenuate hypertension. Our previous research has found that aliskiren protected against myocardial ischemia-reperfusion (I/R) injury and enhanced phosphorylation of endothelial nitric oxide synthase (eNOS) in spontaneously hypertensive rats. However, whether the cardioprotective effect of aliskiren against myocardial I/R injury was eNOS-dependent is unknown. In the present study, 12-week-old male eNOS knockout (eNOS(-/-) ) and wild-type C57BL/6J mice (WT) were orally administrated with the dose of 50 mg/kg/day of aliskiren...
November 3, 2016: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/27808425/e-cigarette-vapor-induces-an-apoptotic-response-in-human-gingival-epithelial-cells-through-the-caspase-3-pathway
#13
Mahmoud Rouabhia, Hyun Jin Park, Abdelhabib Semlali, Andrew Zakrzewski, Witold Chmielewski, Jamila Chakir
Electronic cigarettes represent an increasingly significant proportion of today's consumable tobacco products. E-cigarettes contain several chemicals which may promote oral diseases. The aim of this study was to investigate the effect of e-cigarette vapor on human gingival epithelial cells. Results show that e-cigarette vapor altered the morphology of cells from small cuboidal form to large undefined shapes. Both single and multiple exposures to e-cigarette vapor led to a bulky morphology with large faint nuclei and an enlarged cytoplasm...
November 3, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27802437/valproic-acid-promotes-human-glioma-u87-cells-apoptosis-and-inhibits-glycogen-synthase-kinase-3%C3%AE-through-erk-akt-signaling
#14
Chi Zhang, Songlin Liu, Xianrui Yuan, Zhongliang Hu, Haoyu Li, Ming Wu, Jian Yuan, Zijin Zhao, Jun Su, Xiangyu Wang, Yiwei Liao, Qing Liu
BACKGROUND: Valproic acid (VPA), an established antiepileptic drug, was assessed for antitumor activity, including its effects on glioblastoma, but its role has not been determined. METHODS: In the present study, we investigated VPA-induced apoptosis effects on human U87 cells by cell viability, lactate dehydrogenase (LDH) release, TUNEL/Hoechst staining and flow cytometric in vitro, then we further explored the underlying molecular mechanisms using the selective antagonists PD98059, LY294002 and SB216763...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27799463/estrogen-receptors-and-esterol-dependent-neuroprotective-actions-a-pilot-study
#15
Ekaterine Tskitishvili, Christel Pequeux, Carine Munaut, Renaud Viellevoye, Michelle Nisolle, Agnes Noel, Jean-Michel Foidart
Estetrol (E4) has strong antioxidative, neuro- and angiogenic effects in neural system resulting in attenuation of neonatal hypoxic-ischemic encephalopathy. We aimed to define the role of estrogen receptors in E4-dependent actions in neuronal cell cultures and prove the promyelinating effect of E4. In vitro the antioxidative and cell survival/proliferating effects of E4 on H202-induced oxidative stress in primary hippocampal cell cultures were studied by using different combinations of specific inhibitors for ERα (MPP dihydrochloride), ERβ (PHTTP), GPR30 (G15) and palmytoilation (2-BR)...
October 31, 2016: Journal of Endocrinology
https://www.readbyqxmd.com/read/27794544/hsp70-expression-induced-by-co-enzyme-q10-protected-chicken-myocardial-cells-from-damage-and-apoptosis-under-in-vitro-heat-stress
#16
J Xu, S Tang, E Song, B Yin, D Wu, E Bao
The aim of this study was to investigate whether induction of Hsp70 expression by co-enzyme Q10 (Q10) treatment protects chicken primary myocardial cells (CPMCs) from damage and apoptosis in response to heat stress for 5 hours. Analysis of the expression and distribution of Hsp70 and the levels of the damage-related enzymes creatine kinase-MB (CK-MB) and lactate dehydrogenase (LDH), as well as pathological analysis showed that co-enzyme Q10 alleviated the damage caused to CPMCs during heat stress. Further, analysis of cell apoptosis and the expression of cleaved caspase-3 indicated that co-enzyme Q10 did have an anti-apoptotic role during heat stress...
October 28, 2016: Poultry Science
https://www.readbyqxmd.com/read/27786573/effect-and-mechanism-of-calpains-on-pediatric-lobar-pneumonia
#17
Genquan Yin, Qiang Zeng, Haijin Zhao, Peiqiong Wu, Shaoxi Cai, Li Deng, Wenhui Jiang
BACKGROUND: Lobar pneumonia, one of the community-acquired pneumonia (CAP), is a common pediatric low respiratory tract infection. Calpains are Ca(2+)-activated cysteine proteases whose activation mechanism is elusive. The present study was undertaken to detect the role and mechanism of calpains in pediatric lobar pneumonia. MATERIAL AND METHODS: The human acute lung infection model (ALIM) was constructed and infected by Streptococcus. Enzyme-linked immunosorbent assay (ELISA) was used to measure interleukin (IL)-6, IL-8 and tumor necrosis factor (TNF)-α...
October 27, 2016: Bioengineered
https://www.readbyqxmd.com/read/27785949/apremilast-reversed-carfilzomib-induced-cardiotoxicity-through-inhibition-of-oxidative-stress-nf-%C3%AE%C2%BAb-and-mapk-signaling-in-rats
#18
Faisal Imam, Naif O Al-Harbi, Mohammad Matar Al-Harbi, Mushtaq Ahmad Ansari, Mashal M Almutairi, Musaad Alshammari, Talal Saad Almukhlafi, Mohd Nazam Ansari, Khaldoon Aljerian, Sheikh Fayaz Ahmad
Carfilzomib (CFZ), is a potent, selective second generation proteasome inhibitor, used for the treatment of multiple myeloma. The aim of the present study was to investigate the possible protective effect of apremilast (AP) on the CFZ -induced cardiotoxicity. Rats were randomly divided into four groups: Group 1, served as the control group, received normal saline. Group 2, served as the toxic group, received CFZ (4 mg/kg, intraperitoneally [i.p.]). Groups 3 and 4, served as treatment groups, and received CFZ with concomitant oral administration of AP in doses of 10 and 20 mg/kg/day, respectively...
October 27, 2016: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/27777967/nod-like-receptor-protein-3-inflammasome-priming-and-activation-in-barrett-s-epithelial-cells
#19
Yuji Nadatani, Xiaofang Huo, Xi Zhang, Chunhua Yu, Edaire Cheng, Qiuyang Zhang, Kerry B Dunbar, Arianne Theiss, Thai H Pham, David H Wang, Toshio Watanabe, Yasuhiro Fujiwara, Tetsuo Arakawa, Stuart J Spechler, Rhonda F Souza
BACKGROUND & AIMS: Microbial molecular products incite intestinal inflammation by activating Toll-like receptors (TLRs) and inflammasomes of the innate immune system. This system's contribution to esophageal inflammation is not known. Gram-negative bacteria, which dominate the esophageal microbiome in reflux esophagitis, produce lipopolysaccharide (LPS), a TLR4 ligand. TLR4 signaling produces pro-interleukin (IL)1β, pro-IL18, and NOD-like receptor protein 3 (NLRP3), which prime the NLRP3 inflammasome...
July 2016: Cellular and Molecular Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/27769022/tadalafil-reduces-airway-hyperactivity-and-protects-against-lung-and-respiratory-airways-dysfunction-in-a-rat-model-of-silicosis
#20
Rania R Abdelaziz, Wagdi F Elkashef, Eman Said
Silicosis is a crippling respiratory disorder characterized by massive lung inflammation and fibrosis. The current study provides evidence on the protective potential of tadalafil; a specific phosphodiesterase-5 (PDE-5) inhibitor against experimentally-induced pulmonary silicosis in rats. Silicosis was induced by intranasal instillation of crystalline silica (50mg/rat). Halofuginone hydrobromide; a standard collagen-1 synthesis inhibitor was selected as a reference anti-fibrotic. Daily oral administration of tadalafil (1mg/kg) for 8weeks significantly ameliorated silica-induced pulmonary damage...
October 18, 2016: International Immunopharmacology
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