"目录号: HY-14164
Metabolic Enzyme/Protease-
Zileuton 是一种有效的，选择性的5-lipoxygenase抑制剂，具有抗炎的作用。
5-Lipoxygenase
相关产品
U-73122-ML355-Zileuton sodium-Enazadrem-LY 178002-Malotilate-RWJ 63556-S-2474-CMI-392-CMI977-PGS-IN-1-RS4317-S-(+)-Marmesin-U66858-
生物活性
Description
Zileuton is a potent and selective inhibitor of5-lipoxygenase, exhibiting inflammatory activities.
In Vitro
In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer[2].
In Vivo
In zileuton (5 mg/kg, p.o.) treated I/R rat, the effect of zileuton to decrease NF-κB expression does not change significantly in the presence of COX inhibitors, and the group reveals significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreases apoptotic index significantly. Zileuton has no significant effect on increased serum TNF-α levels in I/R group[1]. Zileuton (1,200 mg/kg) inhibits the polyp formation in APCΔ468colon and small intestine. Zileuton treatment inhibits the proliferation rates of non epithelial cells in polyps, and increases the apoptosis rates in polyps in rat. There is significant increase in the number of apoptotic cells in the Zileuton-treated cells both in small intestine and in the colon. The reduced proliferation rate may significantly contribute to the reduction of polyposis in both the small intestine and colon of Zileuton-fed APCΔ468mice[3].
Clinical Trial
NCT01136941
Children's Hospital Medical Center, Cincinnati
Sickle Cell Disease
September 2010
Phase 1
NCT01130688
University of Massachusetts, Worcester
Chronic Myelogenous Leukemia
January 2010
Phase 1
NCT02047149
University of Massachusetts, Worcester-Bristol-Myers Squibb
Chronic Myelogenous Leukemia
January 2014
Phase 1
NCT00575861
Gelb, Arthur F., M.D.
Asthma
September 2005
Phase 4
NCT00486343
Critical Therapeutics
Asthma
July 2007
Phase 4
NCT02348203
National Cancer Institute (NCI)
Pulmonary Nodules-Tobacco Use Disorder
January 13, 2016
Phase 2
NCT00262405
University of Michigan-National Institutes of Health (NIH)
Idiopathic Pulmonary Fibrosis
January 2001
Phase 2
NCT00534625
Critical Therapeutics
Asthma
September 2007
Phase 2
NCT00493974
University of Minnesota - Clinical and Translational Science Institute-National Heart, Lung, and Blood Institute (NHLBI)
Pulmonary Disease, Chronic Obstructive
March 2007
Phase 3
NCT00056004
Barbara Ann Karmanos Cancer Institute-National Cancer Institute (NCI)
Head and Neck Cancer-Lung Cancer
June 2003
Phase 2
NCT01021215
National Cancer Institute (NCI)
Tobacco Use Disorder
May 2010
Phase 1-Phase 2
NCT00098358
Critical Therapeutics
Acne Vulgaris
November 2004
Phase 2
NCT00299065
Critical Therapeutics
Asthma
January 2006
Phase 1-Phase 2
NCT01805687
Cornerstone Therapeutics Inc.
Asthma
March 2013
Phase 4
NCT00070486
Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)
Lung Cancer
December 2003
Phase 2
NCT01174056
Washington University School of Medicine-Doris Duke Charitable Foundation
Lung Inflammation
July 2011
Early Phase 1
NCT00467831
National Human Genome Research Institute (NHGRI)-National Institutes of Health Clinical Center (CC)
Hermansky-Pudlak Syndrome (HPS)-Pulmonary Fibrosis-Oculocutaneous Albinism-Platelet Storage Pool Deficiency-Metabolic Disease
April 2007
Phase 1-Phase 2
NCT00723021
Pfizer
Asthma
July 2008
Phase 2
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References
[1].Abueid L, et al. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2016 Nov 10.
[2].Kuvibidila S, et al. Hydroxyurea and Zileuton Differentially Modulate Cell Proliferation and Interleukin-2 Secretion by Murine Spleen Cells: Possible Implication on the Immune Function and Risk of Pain Crisis in Patients with Sickle Cell Disease. Ochsner
[3].Gounaris E, et al. Zileuton, 5-lipoxygenase inhibitor, acts as a chemopreventive agent in intestinal polyposis, by modulating polyp and systemic inflammation. PLoS One. 2015 Mar 6;10(3):e0121402.