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Innate immunity response of zafirlukast treated-tilapia during foreign body inflammation
Dev Comp Immunol. 2023 Dec 11:105112. doi: 10.1016/j.dci.2023.105112. Online ahead of print.ABSTRACTThere is limited knowledge regarding the blockade of cysteinyl leukotriene receptors (CysLTRs) and their effects in teleost fish. The present study investigated the effects of Zafirlukast, antagonist of CysLTR1 receptor, on the foreign body inflammatory reaction in Nile tilapia (Oreochromis niloticus). Zafirlukast-treated tilapia demonstrated a decrease in the formation of multinucleated foreign body giant cells and Langhans cells on the round glass coverslips implanted in the subcutaneous tissue, along with a significant re...
Source: Developmental and Comparative Immunology - December 13, 2023 Category: Allergy & Immunology Authors: Susana Luporini de Oliveira Camila Carlino da Costa Mayumi Fernanda Aracati Leticia Franchin Rodrigues Gabriel Conde Alessandra Cristina de Moraes Annelise Carla Camplesi Thais Heloisa Vaz Farias Ives Charlie Silva Luiz Arthur Malta Pereira Marco Antonio Source Type: research

Structured solubility behaviour in fed simulated intestinal fluids
This study has utilised nine bioequivalent simulated fed intestinal media recipes that cover over 90% of the compositional variability of sampled fed human intestinal fluid. The solubility of 24 drugs (Acidic; furosemide, ibuprofen, indomethacin, mefenamic acid, naproxen, phenytoin, piroxicam, valsartan, zafirlukast: Basic; aprepitant, atazanavir, bromocriptine, carvedilol, dipyridamole, posaconazole, tadalafil: Neutral; acyclovir, carbamazepine, felodipine, fenofibrate, griseofulvin, itraconazole, paracetamol, probucol) has been assessed to determine if structured solubility behaviour is present. The measured solubility b...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 27, 2023 Category: Drugs & Pharmacology Authors: Maria In ês Silva Ibrahim Khadra Kate Pyper Gavin W Halbert Source Type: research

Zafirlukast protects against hepatic ischemia-reperfusion injury in rats via modulating Bcl-2/Bax and NF- κB/SMAD-4 pathways
This study aimed to evaluate the protective effect of zafirlukast (ZFK) on IR-induced hepatic injury and investigate its relevant protective mechanism. Thirty-two male Wistar albino rats were randomly allocated to four groups: sham, IRI, ZFK, and ZFK + IR groups. ZFK was administered orally in a dose of 80 mg/kg/day for 10 consecutive days. Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBL) levels, and gamma glutamyl transferase (GGT) activity were estimated. Liver tissues were used to assess oxidative stress biomarkers including malondialdehyde (MDA), myeloperoxidase (MPO), nitri...
Source: International Immunopharmacology - July 7, 2023 Category: Allergy & Immunology Authors: Heba M Mahmoud Deiaa E Elsayed Abouzed Amira M Abo-Youssef Ramadan A M Hemeida Source Type: research

Molecules, Vol. 28, Pages 2989: Repurposing FIASMAs against Acid Sphingomyelinase for COVID-19: A Computational Molecular Docking and Dynamic Simulation Approach
The objective was to inhibit acid sphingomyelinase activity in order to prevent the cells from SARS-CoV-2 infection. Previous studies have reported functional inhibitors against ASM (FIASMAs). These inhibitors can be exploited to block the entry of SARS-CoV-2 into the cells. To achieve our objective, a drug library containing 257 functional inhibitors of ASM was constructed. Computational molecular docking was applied to dock the library against the target protein (PDB: 5I81). The potential binding site of the target protein was identified through structural alignment with the known binding pocket of a protein with a simil...
Source: Molecules - March 27, 2023 Category: Chemistry Authors: Aliza Naz Sumbul Asif Khairiah Mubarak Alwutayd Sara Sarfaraz Sumra Wajid Abbasi Asim Abbasi Abdulkareem M. Alenazi Mohamed E. Hasan Tags: Article Source Type: research

Comparison of Cromolyn Sodium, Montelukast, and Zafirlukast Prophylaxis for Capsular Contracture
This study investigated the effects of cromolyn sodium, montelukast, and zafirlukast on capsular contracture in a rat model. Methods: Thirty female Wistar albino rats were randomly divided into five groups: control, sham, cromolyn sodium, montelukast, and zafirlukast. Intraperitoneal injections were administered daily to the sham (1 ml per day), cromolyn sodium (10 mg/kg per day), montelukast (10 mg/kg per day), and zafirlukast (1.25 mg/kg per day) groups 1 month before surgery. Miniature breast implants were then placed on the backs of the rats in each group. Injections were continued for the next 3 months. The rat...
Source: Plastic and Reconstructive Surgery - October 29, 2022 Category: Cosmetic Surgery Tags: Experimental Source Type: research

[ASAP] Selective Inhibition of the Periodontal Pathogen < named-content content-type="genus-species" xlink:type="simple" > Porphyromonas gingivalis < /named-content > by Third-Generation Zafirlukast Derivatives
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.2c01471 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - October 23, 2022 Category: Chemistry Authors: Kaitlind C. Howard and Sylvie Garneau-Tsodikova Source Type: research

Cysteinyl-maresin 3 inhibits IL-13 induced airway hyperresponsiveness through alternative activation of the CysLT < sub > 1 < /sub > receptor
CONCLUSIONS: MCTR3, but not LTD4, decreased the IL-13-induced airway hyperresponsiveness by activation of the CysLT1 receptor. The distinct actions of the two lipid mediators on the CysLT1 receptor suggest an alternative signalling pathway appearing under inflammatory conditions, where this new action of MCTR3 implicates potential to inhibit airway hyperresponsiveness in asthma.PMID:36116518 | DOI:10.1016/j.ejphar.2022.175257 (Source: European Journal of Pharmacology)
Source: European Journal of Pharmacology - September 18, 2022 Category: Drugs & Pharmacology Authors: Jesper S äfholm Willem Abma Lora G Bankova Joshua A Boyce Mamdoh Al-Ameri Ann-Charlotte Orre Craig E Wheelock Sven-Erik Dahl én Mikael Adner Source Type: research

A Disproportionality Analysis of Drug –Drug Interactions of Tizanidine and CYP1A2 Inhibitors from the FDA Adverse Event Reporting System (FAERS)
ConclusionsReports involving tizanidine and a CYP1A2 inhibitor have higher odds of reporting hypotension. This study suggests that concurrent use of tizanidine with CYP1A2 inhibitors may lead to serious health consequences associated with low blood pressure such as falls and fractures. (Source: Drug Safety)
Source: Drug Safety - July 14, 2022 Category: Drugs & Pharmacology Source Type: research