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https://www.readbyqxmd.com/read/29299197/inhibition-of-5-lipoxygenase-inhibitor-zileuton-in-high-fat-diet-induced-nonalcoholic-fatty-liver-disease-progression-model
#1
Kuifen Ma, Yihe Chen, Xingguang Liang, Jing Miao, Qingwei Zhao
Objectives: Arachidonic Acid/5-lipoxygenase (AA/5-LOX) pathway connects lipid metabolism and proinflammatory cytokine, which are both related to the development and progression of nonalcoholic fatty liver disease (NAFLD). Therefore, the present study was designed to investigate the role of AA/5-LOX pathway in progression of NAFLD, and the effect of zileuton, an inhibitor of 5-LOX, in this model. Materials and Methods: Animal model for progression of NAFLD was established via feeding high saturated fat diet (HFD)...
November 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29298996/the-phosphatidylinositide-3-kinase-pi3k-signaling-pathway-is-a-determinant-of-zileuton-response-in-adults-with-asthma
#2
Amber Dahlin, Weiliang Qiu, Augusto A Litonjua, John J Lima, Mayumi Tamari, Michiaki Kubo, Charles G Irvin, Stephen P Peters, Ann C Wu, Scott T Weiss, Kelan G Tantisira
Variable responsiveness to zileuton, a leukotriene antagonist used to treat asthma, may be due in part to genetic variation. While individual SNPs were previously associated with zileuton-related lung function changes, specific quantitative trait loci (QTLs) and biological pathways that may contribute have not been identified. In this study, we investigated the hypothesis that genetic variation within biological pathways is associated with zileuton response. We performed an integrative QTL mapping and pathway enrichment study to investigate data from a GWAS of zileuton response, in addition to mRNA expression profiles and leukotriene production data from lymphoblastoid cell lines (LCLs) (derived from asthmatics) that were treated with zileuton or ethanol (control)...
January 3, 2018: Pharmacogenomics Journal
https://www.readbyqxmd.com/read/29290980/up-regulation-of-5-lipoxygenase-by-inhibition-of-cathepsin-g-enhances-trail-induced-apoptosis-through-down-regulation-of-survivin
#3
Seon Min Woo, Kyoung-Jin Min, Seung Un Seo, Shin Kim, Jong-Wook Park, Dae Kyu Song, Hyun-Shik Lee, Sang Hyun Kim, Taeg Kyu Kwon
Cathepsin G is a serine protease secreted from activated neutrophils, it has important roles in inflammation and immune response. Moreover, cathepsin G promotes tumor cell-cell adhesion and migration in cancer cells. In this study, we investigated whether inhibition of cathepsin G could sensitize TRAIL-mediated apoptosis in cancer cells. An inhibitor of cathepsin G [Cathepsin G inhibitor I (Cat GI); CAS 429676-93-7] markedly induced TRAIL-mediated apoptosis in human renal carcinoma (Caki, ACHN, and A498), lung cancer (A549) and cervical cancer (Hela) cells...
December 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/29289887/novel-click-modifiable-thioquinazolinones-as-anti-inflammatory-agents-design-synthesis-biological-evaluation-and-docking-study
#4
Ghandoura Moussa, Rana Alaaeddine, Lynn M Alaeddine, Rasha Nassra, Ahmed S F Belal, Azza Ismail, Ahmed F El-Yazbi, Yasser S Abdel-Ghany, Aly Hazzaa
Click chemistry was used to synthesize a new series of thioquinazolinone molecules equipped with propargyl moiety,1,2,3-triazolyl and isoxazolyl rings. Our design was based on merging pharmacophores previously reported to exhibit COX-2 inhibitory activities to a thioquinazolinone-privileged scaffold. The synthesized compounds were subjected to in vitro cyclooxygenase COX-1/COX-2 and 15-LOX inhibition assays. Compounds 2c, 3b, 3h, 3j, and 3k showed COX-2 inhibition with IC50 (μM) 0.18, 0.19, 0.11, 0.16 and 0...
December 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29248523/emerging-therapies-for-atopic-dermatitis-the-prostaglandin-leukotriene-pathway
#5
Daniel A Yanes, Joy L Mosser-Goldfarb
The role of leukotrienes and prostaglandins in development of atopy has been prototypically established in studies of asthma pathogenesis. Likewise, both in vitro and in vivo studies of atopic dermatitis have demonstrated that these molecules maintain important pathophysiologic roles. Thus, it follows that targeted therapies against these molecules may be promising in management of atopic dermatitis. Montelukast has had questionable efficacy in patients with atopic dermatitis, while small pilots using zileuton did have some clinically significant improvement...
December 14, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29174741/antidepressant-like-effect-of-zileuton-is-accompanied-by-hippocampal-neuroinflammation-reduction-and-creb-bdnf-upregulation-in-lipopolysaccharide-challenged-mice
#6
Dan-Dan Li, Hang Xie, Yi-Feng Du, Yan Long, Miranda N Reed, Mei Hu, Vishnu Suppiramaniam, Hao Hong, Su-Su Tang
BACKGROUND: Recent studies demonstrated beneficial effects of zileuton, a 5-lipoxygenase (5LO) inhibitor, on some brain diseases in animal models, but the role of zileuton in the depression remains unknown. METHODS: We investigated the effects of zileuton on depressive behaviors using tail suspension test (TST), forced swimming test (FST) and novelty-suppressed feeding test (NSFT) in mice injected with lipopolysaccharide (LPS). The 5LO level, activation of microglia, NF-κB p65, TNF-α, IL-1β, brain-derived neurotrophic factor (BDNF), and c-AMP response element-binding protein (CREB) were determined in the mouse hippocampus...
November 13, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29133059/recent-advances-in-the-search-for-novel-5-lipoxygenase-inhibitors-for-the-treatment-of-asthma
#7
Ferdinando Bruno, Giuseppe Spaziano, Angela Liparulo, Fiorentina Roviezzo, Seyed Mohammed Nabavi, Antoni Sureda, Rosanna Filosa, Bruno D'Agostino
The products of 5-lipoxygenase are synthesized and released in the airway when an asthmatic reaction occurs. 5-lipoxygenase via arachidonic acid metabolism produces leukotrienes that mediate bronchoconstriction and inflammatory modifications essential in the pathophysiology of asthma. Until to now, only one approved 5-LO inhibitor, zileuton, can be found as a potential therapy for asthma. With the increasing number of indications for anti-leukotriene (anti-LT) drugs, the development of 5-LO inhibitor agents becomes increasingly important...
October 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29076063/neuropsychiatric-events-associated-with-leukotriene-modifying-agents-a-systematic-review
#8
REVIEW
Sharon W Y Law, Angel Y S Wong, Shweta Anand, Ian C K Wong, Esther W Chan
INTRODUCTION: Leukotriene-modifying agents (LTMAs) including montelukast, zafirlukast, and zileuton are approved by the US Food and Drug Administration (FDA) for the treatment of asthma and allergic rhinitis. Various neuropsychiatric events (NEs) have been reported; however, the evidence of the association is conflicting. This systematic review investigates the association between NEs and LTMAs by assessing the relevant published literature. METHODS: PubMed, EMBASE, MEDLINE, and Cochrane Library were searched using keywords...
October 26, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/29074417/multiple-mechanisms-underlying-neuroprotection-by-secretory-phospholipase-a2-preconditioning-in-a-surgically-induced-brain-injury-rat-model
#9
Yuechun Wang, Prativa Sherchan, Lei Huang, Onat Akyol, Devin W McBride, John H Zhang
BACKGROUND: Intra-operative bleeding, post-operative brain edema and neuroinflammation are major complications in patients with surgical brain injury (SBI). Phospholipase A2 (PLA2) is the upstream enzyme which initiates the PLA2, 5-lipoxygenase (5-LOX) and leukotriene B4 (LTB4) inflammatory pathway. We hypothesized PLA2preconditioning (PPC) prior to SBI can activate endogenous anti-inflammatory responses to protect against SBI. This study evaluated if PPC can ameliorate neurosurgical complications and elucidated PPC-mediated possible protective mechanisms in a rat SBI model...
October 24, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28947611/inhibition-of-5-lipoxygenase-alleviates-graft-versus-host-disease
#10
Barbara Maximino Rezende, Rayssa Maciel Athayde, William Antônio Gonçalves, Carolina Braga Resende, Priscila Teles de Tolêdo Bernardes, Denise Alves Perez, Lísia Esper, Alesandra Côrte Reis, Milene Alvarenga Rachid, Marina Gomes Miranda E Castor, Thiago Mattar Cunha, Fabiana Simão Machado, Mauro Martins Teixeira, Vanessa Pinho
Leukotriene B4 (LTB4), a proinflammatory mediator produced by the enzyme 5-lipoxygenase (5-LO), is associated with the development of many inflammatory diseases. In this study, we evaluated the participation of the 5-LO/LTB4 axis in graft-versus-host disease (GVHD) pathogenesis by transplanting 5-LO-deficient leukocytes and investigated the effect of pharmacologic 5-LO inhibition by zileuton and LTB4 inhibition by CP-105,696. Mice that received allogeneic transplant showed an increase in nuclear 5-LO expression in splenocytes, indicating enzyme activation after GVHD...
November 6, 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/28865292/pyrazole-hydrazone-derivatives-as-anti-inflammatory-agents-design-synthesis-biological-evaluation-cox-1-2-5-lox-inhibition-and-docking-study
#11
Mohamed A Abdelgawad, Madlen B Labib, Mahmoud Abdel-Latif
A new series of pyrazole-hydrazone derivatives 4a-i were designed and synthesized, their chemical structures were confirmed by IR, (1)H NMR, (13)C NMR, MS spectral data and elemental analysis. IC50 values for all prepared compounds to inhibit COX-1, COX-2 and 5-LOX enzymes were determined in vitro. Compounds 4a (IC50=0.67μM) and 4b (IC50=0.58μM) showed better COX-2 inhibitory activity than celecoxib (IC50=0.87μM) with selectivity index (SI=8.41, 10.55 in sequent) relative to celecoxib (SI=8.85). Also, compound 4a and 4b exhibited superior inhibitory activity against 5-LOX (IC50=1...
October 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28860177/effect-of-zileuton-on-osteoporotic-bone-and-its-healing-expression-of-bone-and-brain-genes-in-rats
#12
Dominik Saul, Milena Ninkovic, Marina Komrakova, Lorenz Wolff, Turab Gasimov, Björn Menger, Daniel Bernd Hoffmann, Veit Rohde, Stephan Sehmisch
Estrogen deficiency and aging are associated with osteoporosis, impaired bone healing and lower cognitive performance. Close functional and physical connections occur between bone and the central nervous system. An anti-inflammatory drug, zileuton, is known to have a positive effect on bone and ischemic brain. We studied the effect of zileuton on bone, its healing and on the genes for bone-brain cross-talks. Three-month-old Sprague-Dawley rats were ovariectomized or left untreated. After 8 weeks, bilateral metaphyseal tibia osteotomy with plate osteosynthesis was performed in all rats...
August 31, 2017: Journal of Applied Physiology
https://www.readbyqxmd.com/read/28720504/synthesis-of-novel-hybrids-of-pyrazole-and-coumarin-as-dual-inhibitors-of-cox-2-and-5-lox
#13
Fa-Qian Shen, Zhong-Chang Wang, Song-Yu Wu, Shen-Zhen Ren, Ruo-Jun Man, Bao-Zhong Wang, Hai-Liang Zhu
In our previous study, we designed a series of pyrazole derivatives as novel COX-2 inhibitors. In order to obtain novel dual inhibitors of COX-2 and 5-LOX, herein we designed and synthesized 20 compounds by hybridizing pyrazole with substituted coumarin who was reported to exhibit 5-LOX inhibition to select potent compounds using adequate biological trials sequentially including selective inhibition of COX-2 and 5-LOX, anti-proliferation in vitro, cells apoptosis and cell cycle. Among them, the most potent compound 11g (IC50=0...
August 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28713783/streptococcus-pyogenes-phospholipase-a2-induces-the-expression-of-adhesion-molecules-on-human-umbilical-vein-endothelial-cells-and-aorta-of-mice
#14
Masataka Oda, Hisanori Domon, Mie Kurosawa, Toshihito Isono, Tomoki Maekawa, Masaya Yamaguchi, Shigetada Kawabata, Yutaka Terao
The Streptococcus pyogenes phospholipase A2 (SlaA) gene is highly conserved in the M3 serotype of group A S. pyogenes, which often involves hypervirulent clones. However, the role of SlaA in S. pyogenes pathogenesis is unclear. Herein, we report that SlaA induces the expression of intercellular adhesion molecule 1 (ICAM1) and vascular cell adhesion molecule 1 (VCAM1) via the arachidonic acid signaling cascade. Notably, recombinant SlaA induced ICAM1 and VCAM1 expression in human umbilical vein endothelial cells (HUVECs), resulting in enhanced adhesion of human monocytic leukemia (THP-1) cells...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28710425/naja-sputatrix-venom-preconditioning-attenuates-neuroinflammation-in-a-rat-model-of-surgical-brain-injury-via-pla2-5-lox-ltb4-cascade-activation
#15
Yuechun Wang, Prativa Sherchan, Lei Huang, Onat Akyol, Devin W McBride, John H Zhang
Inflammatory preconditioning is a mechanism in which exposure to small doses of inflammatory stimuli prepares the body against future massive insult by activating endogenous protective responses. Phospholipase A2/5-lipoxygenase/leukotriene-B4 (PLA2/5-LOX/LTB4) axis is an important inflammatory signaling pathway. Naja sputatrix (Malayan spitting cobra) venom contains 15% secretory PLA2 of its dry weight. We investigated if Naja sputatrix venom preconditioning (VPC) reduces surgical brain injury (SBI)-induced neuroinflammation via activating PLA2/5-LOX/LTB4 cascade using a partial frontal lobe resection SBI rat model...
July 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28694473/5-lo-inhibition-ameliorates-palmitic-acid-induced-er-stress-oxidative-stress-and-insulin-resistance-via-ampk-activation-in-murine-myotubes
#16
Hyun Jeong Kwak, Hye-Eun Choi, Hyae Gyeong Cheon
Leukotriene B4 (LTB4) production via the 5-lipoxygenase (5-LO) pathway contributes to the development of insulin resistance in adipose and hepatic tissues, but the role of LTB4 in skeletal muscle is relatively unknown. Here, the authors investigated the role of LTB4 in C2C12 myotubes in palmitic acid (PA)-induced ER stress, inflammation and insulin resistance. PA (750 μM) evoked lipotoxicity (ER stress, oxidative stress, inflammation and insulin resistance) in association with LTB4 production. 5-LO inhibition reduced all the lipotoxic effects induced by PA...
July 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28680195/new-hydroxycinnamic-acid-esters-as-novel-5-lipoxygenase-inhibitors-that-affect-leukotriene-biosynthesis
#17
Luc H Boudreau, Grégoire Lassalle-Claux, Marc Cormier, Sébastien Blanchard, Marco S Doucet, Marc E Surette, Mohamed Touaibia
Leukotrienes are inflammatory mediators that actively participate in the inflammatory response and host defense against pathogens. However, leukotrienes also participate in chronic inflammatory diseases. 5-lipoxygenase is a key enzyme in the biosynthesis of leukotrienes and is thus a validated therapeutic target. As of today, zileuton remains the only clinically approved 5-lipoxygenase inhibitor; however, its use has been limited due to severe side effects in some patients. Hence, the search for a better 5-lipoxygenase inhibitor continues...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28669741/design-synthesis-and-biological-evaluation-of-some-novel-indolizine-derivatives-as-dual-cyclooxygenase-and-lipoxygenase-inhibitor-for-anti-inflammatory-activity
#18
Sushant K Shrivastava, Pavan Srivastava, Robin Bandresh, Prabhash Nath Tripathi, Avanish Tripathi
Some novel indolizine derivatives were synthesized by bioisosteric modification of imidazo[1,2-a]pyridine for anti-inflammatory activity. The physicochemical characterization and structure of compounds were elucidated by state of the art spectroscopic technique. Induced fit docking was performed for initial screening to elucidate the interactions with corresponding amino acids of cyclooxygenase (COX-1, COX-2) and lipoxygenase (LOX) enzymes. The target compounds 53-60 were then evaluated against in vivo carrageenan and arachidonic acid induced rat paw edema models for anti-inflammatory activity...
August 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28623130/leukotriene-signaling-via-alox5-and-cysteinyl-leukotriene-receptor-1-is-dispensable-for-in%C3%A2-vitro-growth-of-cd34-cd38-stem-and-progenitor-cells-in-chronic-myeloid-leukemia
#19
Monika Dolinska, Alexandre Piccini, Wan Man Wong, Eleni Gelali, Anne-Sofie Johansson, Johannis Klang, Pingnan Xiao, Elham Yektaei-Karin, Ulla Olsson Strömberg, Satu Mustjoki, Leif Stenke, Marja Ekblom, Hong Qian
Tyrosine kinase inhibitors targeting the BCR-ABL oncoprotein in chronic myeloid leukemia (CML) are remarkably effective inducing deep molecular remission in most patients. However, they are less effective to eradicate the leukemic stem cells (LSC), resulting in disease persistence. Therefore, there is great need to develop novel therapeutic strategies to specifically target the LSC. In an experimental mouse CML model system, the leukotriene pathway, and specifically, the expression ALOX5, encoding 5-lipoxygenase (5-LO), has been reported as a critical regulator of the LSC...
August 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28512667/involvement-of-leukotriene-b4-released-from-keratinocytes-in-itch-associated-response-to-intradermal-interleukin-31-in-mice
#20
Tsugunobu Andoh, Ayako Harada, Yasushi Kuraishi
A recent study suggests that interleukin-31 (IL-31) exerts its effect via indirect mechanisms rather than through direct stimulation of cutaneous nerves. However, the underlying peripheral mechanisms of IL-31-induced itch in the skin remain unclear. Therefore, the present study investigated the peripheral mechanisms underlying IL-31-induced itch in mice. IL-31-induced itch-related response was inhibited by anti-allergic drugs (tranilast and azelastine), but not by an H1 histamine receptor antagonist (terfenadine)...
August 31, 2017: Acta Dermato-venereologica
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