Zafirlukast Is a Dual Modulator of Human Soluble Epoxide Hydrolase and Peroxisome Proliferator-Activated Receptor γ
Tamara G öbel, Olaf Diehl, Jan Heering, Daniel Merk, Carlo Angioni, Sandra K. Wittmann, Estel.la Buscato, Ramona Kottke, Lilia Weizel, Tim Schader, Thorsten J. Maier, Gerd Geisslinger, Manfred Schubert-Zsilavecz, Dieter Steinhilber, Ewgenij Proschak, Astrid S. Kahnt (Source: Frontiers in Pharmacology)
Source: Frontiers in Pharmacology - March 20, 2019 Category: Drugs & Pharmacology Source Type: research
Zafirlukast attenuates advanced glycation end-products (AGEs)-induced degradation of articular extracellular matrix (ECM).
Abstract
Zafirlukast, a leukotriene receptor antagonist, has been shown to exert a wide range of effects including anti-asthmatic, anti-inflammatory and oral anti-bacterial. Osteoarthritis is one of the most prevalent age-related public health burdens in the modern world. In the present study, we applied zafirlukast in the treatment of human primary chondrocytes and found that it exerts potent anti-osteoarthritic effects. Zafirlukast inhibited AGEs-induced degradation of the articular extracellular matrix by suppressing expression of MMPs, ADAMTS, NOX-4, generation of ROS, and activation of NF-κB via the ...
Source: International Immunopharmacology - January 3, 2019 Category: Allergy & Immunology Authors: Lei C, Wu S, Wen C, Li Y, Liu N, Huang J, Li L, Fu M, Liu J Tags: Int Immunopharmacol Source Type: research
Cysteinyl leukotriene receptor type 1 (CysLT1R) antagonist zafirlukast protects against TNF-α-induced endothelial inflammation
In this study, we found that zafirlukast possesses beneficial protective effects on endothelial cells from TNF-α-induced inflammatory response and injury. Our results indicate that TNF-α treatment induces CysLT1R expression. The addition of zafirlukast to culture media suppressed TNF-α-induced expression of endothelial vascular adhesion molecules, such as ICAM-1, VCAM-1, and induction of cytokines, including IL-1β, IL-6, and IL-8. Zafirlukast also ameliorated production of reactive oxygen species (ROS) and adhesion of monocytes to endothelial cells induced by TNF-α. Mechanistically, we demonstrate that zafirlukast sup...
Source: Biomedicine and Pharmacotherapy - December 28, 2018 Category: Drugs & Pharmacology Source Type: research
Cysteinyl leukotriene receptor type 1 (CysLT1R) antagonist zafirlukast protects against TNF- α-induced endothelial inflammation.
In this study, we found that zafirlukast possesses beneficial protective effects on endothelial cells from TNF-α-induced inflammatory response and injury. Our results indicate that TNF-α treatment induces CysLT1R expression. The addition of zafirlukast to culture media suppressed TNF-α-induced expression of endothelial vascular adhesion molecules, such as ICAM-1, VCAM-1, and induction of cytokines, including IL-1β, IL-6, and IL-8. Zafirlukast also ameliorated production of reactive oxygen species (ROS) and adhesion of monocytes to endothelial cells induced by TNF-α. Mechanistically, we demonstrate that zafirlukast sup...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - December 27, 2018 Category: Drugs & Pharmacology Authors: Zhou X, Cai J, Liu W, Wu X, Gao C Tags: Biomed Pharmacother Source Type: research
Tiotropium provides greater improvements in FEV1 than leukotriene receptor antagonists as add-on to ICS in adults with asthma: a systematic review
Conclusion: This systematic literature review suggests that tiotropium provides greater improvements in FEV1 than montelukast or zafirlukast as an add-on to ICS in adults with asthma. (Source: European Respiratory Journal)
Source: European Respiratory Journal - November 19, 2018 Category: Respiratory Medicine Authors: Kaplan, A., Fitzgerald, J. M., El Azzi, G., Engel, M., Buhl, R. Tags: Airway pharmacology and treatment Source Type: research
Breathing new life into West Nile virus therapeutics; discovery and study of zafirlukast as an NS2B-NS3 protease inhibitor.
Abstract
The West Nile virus (WNV) has spread throughout the world causing neuroinvasive diseases with no treatments available. The viral NS2B-NS3 protease is essential for WNV survival and replication in host cells and is a promising drug target. Through an enzymatic screen of the National Institute of Health clinical compound library, we report the discovery of zafirlukast, an FDA approved treatment for asthma, as an inhibitor for the WNV NS2B-NS3 protease. Zafirlukast was determined to inhibit the protease through a mixed mode mechanism with an IC50 value of 32 μM. A structure activity relationship s...
Source: European Journal of Medicinal Chemistry - August 31, 2018 Category: Chemistry Authors: Martinez AA, Espinosa BA, Adamek RN, Thomas BA, Chau J, Gonzalez E, Keppetipola N, Salzameda NT Tags: Eur J Med Chem Source Type: research
[ASAP] Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.8b00458 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Simone Schierle, Cathrin Flauaus, Pascal Heitel, Sabine Willems, Jurema Schmidt, Astrid Kaiser, Lilia Weizel, Tamara Goebel, Astrid S. Kahnt, Gerd Geisslinger, Dieter Steinhilber, Mario Wurglics, G. Enrico Rovati, Achim Schmidtko, Ewgenij Proschak, Daniel Source Type: research
Zafirlukast promotes insulin secretion by increasing calcium influx through L ‐type calcium channels
Journal of Cellular Physiology, EarlyView. (Source: Journal of Cellular Physiology)
Source: Journal of Cellular Physiology - May 24, 2018 Category: Cytology Authors: Hyeon ‐Jeong Hwang
,
Kyoung‐Su Park
,
Jang Hyun Choi
,
Lucio Cocco
,
Hyun‐Jun Jang
,
Pann‐Ghill Suh Source Type: research
Cysteinyl Leukotriene Receptor Antagonists Induce Apoptosis and Inhibit Proliferation of Human Glioblastoma Cells by Down-regulating B-cell Lymphoma 2 and Inducing Cell Cycle Arrest.
Abstract
Glioblastoma is the most aggressive type of brain cancer with the highest proliferation, invasion and migration. Montelukast and zafirlukast, two widely used leukotriene receptor antagonists (LTRAs) for asthma treatment, inhibited invasion and migration of glioblastoma cell lines. Montelukast induces apoptosis and inhibites cell proliferation of various cancer cells. Herein, apoptotic and antiproliferative effects of montelukast and zafirlukast were investigated in two glioblastoma cell lines, A172 and U-87 MG. Both LTRAs induced apoptosis and inhibited cell proliferation of glioblastoma cells in ...
Source: Canadian Journal of Physiology and Pharmacology - May 4, 2018 Category: Drugs & Pharmacology Authors: Piromkraipak P, Parakaw T, Phuagkhaopong S, Srihirun S, Chongthammakun S, Chaithirayanon K, Vivithanaporn P Tags: Can J Physiol Pharmacol Source Type: research
Montelukast inhibits hypoxia inducible factor-1 α translation in prostate cancer cells.
In conclusion, we identify montelukast may be used as a novel agent for the treatment of prostate cancer by decreasing HIF-1α protein translation.
PMID: 29708817 [PubMed - as supplied by publisher] (Source: Cancer Biology and Therapy)
Source: Cancer Biology and Therapy - April 30, 2018 Category: Cancer & Oncology Authors: Tang C, Lei H, Zhang J, Liu M, Jin, Luo H, Xu H, Wu Y Tags: Cancer Biol Ther Source Type: research
Zafirlukast and vincamine ameliorate tamoxifen-induced oxidative stress and inflammation: Role of the JNK/ERK pathway
This study investigated the hepatoprotective effects of both zafirlukast and vincamine and their possible role in the treatment of tamoxifen-induced liver injury in rats. Materials and methods Female Wistar rats were divided into five groups (10 rats each). Groups I and II received 1% Tween 80 and served as normal and tamoxifen controls, respectively. Groups III, IV and V were treated with zafirlukast (80 mg/kg), vincamine (10 mg/kg) and a combination of zafirlukast (80 mg/kg) and vincamine (10 mg/kg), respectively for 10 successive days. Tamoxifen was given orally to all groups, except for 1st group, in the dose ...
Source: Life Sciences - April 5, 2018 Category: Biology Source Type: research
Leukotriene Receptor Antagonists Inhibit Mitogenic Activity in Triple Negative Breast Cancer Cells
Authors: Suknuntha K, Yubolphan R, Krueaprasertkul K, Srihirun S, Sibmooh N, Vivithanaporn P
Abstract
Despite a discovery of hormonal pathways regulating breast cancer, a definitive cure for the disease requires further
identification of alternative targets that provide a hormone-independent support. Apart from their role in inflammatory
diseases, cysteinyl leukotriene (CysLT) receptor antagonists (LTRAs) decrease the risk of lung cancer in asthma patients
and inhibit tumor progression in several malignancies. In the present study, we evaluate the effects of two chemically
different, clinically relevant LT...
Source: Asian Pacific Journal of Cancer Prevention - March 29, 2018 Category: Cancer & Oncology Tags: Asian Pac J Cancer Prev Source Type: research
Property Prediction and Pharmacokinetic Evaluation of Mixed Stoichiometry Cocrystals of Zafirlukast, a Drug Delivery Case Study
CrystEngComm, 2018, Accepted Manuscript DOI: 10.1039/C7CE02059G, CommunicationPhilip Anthony Corner, David Berry, James Francis McCabe, Rafael Barbas, Rafel Prohens, Hongwen Du, Hongyu Zhou, Antonio Llinas Cocrystals have been identified as a method for ensuring the delivery of poorly soluble drugs. Development of cocrystal phases presents many challenges, with the in vivo drug delivery benefits difficult... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - CrystEngComm latest articles)
Source: RSC - CrystEngComm latest articles - January 16, 2018 Category: Chemistry Authors: Philip Anthony Corner Source Type: research
Encapsulation and release of zafirlukast from electrospun polyisobutylene-based thermoplastic elastomeric fiber mat
Publication date: Available online 6 November 2017 Source:European Polymer Journal Author(s): Judit E. Puskas, Aditya Jindal, Kyle Nedic, Matthew T. Luebbers, James R. Baker, Andrew McClain, Bruno Paiva dos Santos, Melissa Camassola, Wayne Jennings, Richard L. Einsporn, Nic D. Leipzig This paper reports the discovery that free-standing rubbery fiber mats can be electrospun from polyisobutylene-based thermoplastic elastomer/poly(ethylene glycol) mixtures from a THF-toluene solution. Direct contact and elution cytotoxic assays of these mats showed no cytotoxic response. Electrospinning the polymers mixed with Za...
Source: European Polymer Journal - November 7, 2017 Category: Chemistry Source Type: research
Neuropsychiatric Events Associated with Leukotriene-Modifying Agents: A Systematic Review
ConclusionMany pharmacovigilance studies have been conducted to determine the association between NEs and LTMAs, but there is limited evidence from observational studies. High-quality epidemiological studies should be conducted to evaluate the association and quantify the risk, not only in children, but also in adults. (Source: Drug Safety)
Source: Drug Safety - October 26, 2017 Category: Drugs & Pharmacology Source Type: research
