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UGT1A1 and UGT1A3 activity and inhibition in human liver and intestinal microsomes and a recombinant UGT system under similar assay conditions using selective substrates and inhibitors
Xenobiotica. 2021 Oct 26:1-15. doi: 10.1080/00498254.2021.1998732. Online ahead of print.ABSTRACT1. In vitro enzyme kinetics and inhibition data was compared for UGT1A1 and UGT1A3 isoforms under similar assay conditions using human liver microsomes (HLM), human intestinal microsomes (HIM) and recombinant UGT (rUGT) enzyme systems.2. UGT1A1 catalyzed β-estradiol 3-β-D-glucuronide formation showed allosteric sigmoidal kinetics in all enzyme systems; while UGT1A3 catalyzed CDCA 24-acyl-β-D-glucuronide formation exhibited Michaelis-Menten kinetics in HLM, substrate inhibition kinetics in HIM and rUGT systems. Corresponding ...
Source: Xenobiotica - October 26, 2021 Category: Research Authors: T V Radhakrishna Mullapudi Punna Rao Ravi Ganapathi Thipparapu Source Type: research

Small scale in vitro method to determine a bioequivalent equilibrium solubility range for fasted human intestinal fluid
This study demonstrates that it is possible to assess the fasted intestinal equilibrium solubility envelope using a small number of bioequivalent media recipes obtained from a multi-dimensional analysis of fasted HIF. The derivation of the nine bioequivalent SIF media coupled with the lower measured solubility range indicate that the solubility results are more likely to reflect the fasted intestinal solubility envelope than previous DoE studies and highlight that intestinal solubility is a range and not a single value.PMID:34419602 | DOI:10.1016/j.ejpb.2021.08.002 (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 22, 2021 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Ibrahim Khadra Kate Pyper Gavin W Halbert Source Type: research

Zafirlukast promotes mitochondrial respiration by stimulating mitochondrial biogenesis in human bronchial epithelial cells
AbstractLung diseases, including asthma, pose a serious global health issue. Loss of mitochondrial function and decreased mitochondrial biogenesis play pivotal roles in the initiation and progression of chronic lung diseases. Thus, maintaining mitochondrial function and homeostasis is an important treatment goal. Zafirlukast is a CysLTR1 antagonist that is widely used as an adjuvant treatment for asthma. In the present study, we investigated the effects of zafirlukast in vitro using human bronchial epithelial cells (BECs). We performed measurements of oxygen consumption and bioenergetics and found that zafirlukast increase...
Source: Journal of Molecular Histology - May 11, 2021 Category: Laboratory Medicine Source Type: research

Zafirlukast prevented ox-LDL-induced formation of foam cells.
Abstract Atherosclerosis (AS), a common arterial disease, is one of the main pathological roots of cardiovascular disease. The formation and accumulation of foam cells is an important event in early AS. An imbalance between cholesterol uptake and efflux is the primary cause of foam cell formation. Although research has focused on preventing the formation of foam cells, a safe and effective therapy has to be found. Zafirlukast is a widely useful type 1 cysteinyl leukotriene receptor (CysLT1R) antagonist with a good safety profile. Zafirlukast is the most used for the treatment of asthma and allergic rhiniti...
Source: Toxicology and Applied Pharmacology - October 20, 2020 Category: Toxicology Authors: Song Q, Hu Z, Xie X, Cai H Tags: Toxicol Appl Pharmacol Source Type: research

Comparison of the Effects of Acellular Dermal Matrix and Montelukast on Radiation-Induced Peri-implant Capsular Formation in Rabbits
Conclusions Acellular dermal matrix and montelukast have a prophylactic effect for CC even when the breast is irradiated. There was no significant difference between ADM and montelukast in preventing capsular formation. The difference is that ADM will only have the effect of covering the capsular formation with ADM and montelukast can cause systemic effects or complications. (Source: Annals of Plastic Surgery)
Source: Annals of Plastic Surgery - August 14, 2020 Category: Cosmetic Surgery Tags: Research Source Type: research

Quantitative single-molecule imaging of TNFR1 reveals zafirlukast as antagonist of TNFR1 clustering and TNF α-induced NF-ĸB signaling.
Quantitative single-molecule imaging of TNFR1 reveals zafirlukast as antagonist of TNFR1 clustering and TNFα-induced NF-ĸB signaling. J Leukoc Biol. 2020 May 13;: Authors: Weinelt N, Karathanasis C, Smith S, Medler J, Malkusch S, Fulda S, Wajant H, Heilemann M, van Wijk SJL Abstract TNFR 1 is a crucial regulator of NF-ĸB-mediated proinflammatory cell survival responses and programmed cell death (PCD). Deregulation of TNFα- and TNFR1-controlled NF-ĸB signaling underlies major diseases, like cancer, inflammation, and autoimmune diseases. Therefore, although being routinely used...
Source: Journal of Leukocyte Biology - May 12, 2020 Category: Hematology Authors: Weinelt N, Karathanasis C, Smith S, Medler J, Malkusch S, Fulda S, Wajant H, Heilemann M, van Wijk SJL Tags: J Leukoc Biol Source Type: research

Identification of Cysteinyl-leukotriene-receptor 1 antagonists as ligands for the bile acid receptor GPBAR1.
Abstract The cysteinyl leukotrienes (CysLTs), i.e. LTC4, LTD4 and LTE4, are a family of proinflammatory agents synthesized from the arachidonic acid. In target cells, these lipid mediators bind to the cysteinyl leukotriene receptors (CysLTR), a family of seven transmembrane G-protein coupled receptors. The CysLT1R is a validated target for treatment of pulmonary diseases and several selective antagonists for this receptor, including montelukast, zafirlukast and pranlukast, have shown effective in the management of asthma. Nevertheless, others CysLT1R antagonists, such as the alpha-pentyl-3-[2-quinolinylmet...
Source: Biochemical Pharmacology - April 20, 2020 Category: Drugs & Pharmacology Authors: Biagioli M, Carino A, Marchianò S, Roselli R, Di Giorgio C, Bordoni M, Fiorucci C, Sepe V, Conflitti P, Limongelli V, Distrutti E, Baldoni M, Zampella A, Fiorucci S Tags: Biochem Pharmacol Source Type: research

In Brief: Neuropsychiatric Events with Montelukast
Date: May 4, 2020 Issue #: 1597Summary: The FDA is requiring stronger warnings in the labeling of the leukotriene receptor antagonist montelukast (Singulair, and generics) about the risk of suicidal behavior and other serious neuropsychiatric events associated with its use. (Source: The Medical Letter)
Source: The Medical Letter - April 14, 2020 Category: Drugs & Pharmacology Authors: admin Tags: Accolate Allergic rhinitis Allergies Antihistamines Asthma corticosteroids Drug Safety Montelukast Singulair Zafirlukast Zileuton Zyflo Source Type: research