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Molecules, Vol. 28, Pages 1174: 3-Arylidene-2-oxindoles as Potent NRH:Quinone Oxidoreductase 2 Inhibitors
v
Sergey E. Sosonyuk
The enzyme NRH:quinone oxidoreductase 2 (NQO2) plays an important role in the pathogenesis of various diseases such as neurodegenerative disorders, malaria, glaucoma, COVID-19 and cancer. NQO2 expression is known to be increased in some cancer cell lines. Since 3-arylidene-2-oxindoles are widely used in the design of new anticancer drugs, such as kinase inhibitors, it was interesting to study whether such structures have additional activity towards NQO2. Herein, we report the synthesis and study of 3-arylidene-2-oxindoles as novel NRH:quinone oxidoreductase inhibitors. It was demonstrated that ox...
Source: Molecules - January 25, 2023 Category: Chemistry Authors: Natalia A. Lozinskaya Elena N. Bezsonova Meriam Dubar Daria D. Melekhina Daniil R. Bazanov Alexander S. Bunev Olga B. Grigor ’eva Vladlen G. Klochkov Elena V. Sokolova Denis A. Babkov Alexander A. Spasov Sergey E. Sosonyuk Tags: Article Source Type: research
Microneedles in diagnostic, treatment and theranostics: An advancement in minimally-invasive delivery system
Biomed Microdevices. 2021 Dec 8;24(1):4. doi: 10.1007/s10544-021-00604-w.ABSTRACTMicroneedle (MN) technology plays an important role in biomedical engineering for their less intrusive access to the skin due to minimally or painless penetration, enhancement of drug permeability, improvement of detectability of biomolecules in the epidermal and dermal layers with therapeutic efficacy and safety. Furthermore, MNs possess some major disadvantages like difficulty in scale-up technique, variation in drug delivery pattern with respect to external environment of skin, blockage of arrays due to dermal tissues, induction of inflamma...
Source: Biomedical Microdevices - December 8, 2021 Category: Biomedical Engineering Authors: Ragini Amarnani Pravin Shende Source Type: research
What Are Some Indications for Using Dexamethasone?
Discussion
Corticosteroids are a group of drugs which can be naturally or synthetically produced. Naturally occurring substances are produced in the adrenal gland, and are protein-bound (primarily corticosteroid-binding globulin and albumin). In the target tissues, they may need to be converted to an active substance. They are then reduced, oxidized, hydroxylated or conjugated as measures to inactivate them. Synthetic steroids have less protein binding and depending on their structure are more or less resistant to inactivation. Prednisone is the glucocorticoid most often used for treatment, especially as it has a short hal...
Source: PediatricEducation.org - June 7, 2021 Category: Pediatrics Authors: Pediatric Education Tags: Uncategorized Source Type: news
An Unusual Diagnosis for Abdominal Pain
BY ARJUN BHARADWAJ; MARGARET GAVOR, MBChB, MPH; & KHALID MALIK, MDA 65-year-old man presented to the emergency department complaining of sudden-onset left-sided abdominal pain followed by a “seizure.” His abdominal pain started a few hours prior to presentation, was sharp in nature, and radiated to his back and umbilicus. The pain waxed and waned, worsened when he walked or sat up, and at its worst was a 10/10. He took a laxative and two antacids, but received no relief.Each “seizure” episode lasted about 30 seconds and occurred every five minutes. He said he felt drained after each event but never lost cons...
Source: The Case Files - October 24, 2018 Category: Emergency Medicine Tags: Blog Posts Source Type: research
Investigating the antiplasmodial activity of primary sulfonamide compounds identified in open source malaria data
In this study 31 PS compounds sourced from the GlaxoSmithKline (GSK) Tres Cantos antimalarial set (TCAMS) were investigated for their ability to selectively inhibit the in vitro growth of Plasmodium falciparum asexual stage malaria parasites. Of these, 14 compounds were found to have submicromolar activity (IC50 0.16–0.89 μM) and a modest selectivity index (SI) for the parasite versus human cells (SI > 12 to >43). As the PS moiety is known to inhibit carbonic anhydrase (CA) enzymes from many organisms, the PS compounds were assessed for recombinant P. falciparum CA (PfCA) mediated inhibition of CO2 hyd...
Source: International Journal for Parasitology: Drugs and Drug Resistance - January 12, 2017 Category: Parasitology Source Type: research
Polycaprolactone thin-film drug delivery systems: Empirical and predictive models for device design.
CONCLUSION: The proposed empirical models can be used to design polycaprolactone thin-film devices for target geometries and release rates. Empirical parameters can be predicted based on drug properties. Together, these models provide tools for preliminary evaluation and design of controlled-release delivery systems.
PMID: 26354259 [PubMed - in process]
Source: Biol Sci Space - September 12, 2015 Category: Science Authors: Schlesinger E, Ciaccio N, Desai TA Tags: Mater Sci Eng C Mater Biol Appl Source Type: research
