The tetra-para-guanidinoethyl-calix[4]arene, its distally-disubstituted ether derivatives involving 2,2'-bithiazolyl- or 2,2'-bipyridyl-methyl groups, as well as the para-guanidinoethylphenol and its analogous derivatives have been synthesized, fully characterized and evaluated as antibacterial agents towards both gram positive and gram negative reference bacteria. The simple phenolic species showed lower activity than their calixarene analogues, confirming the hypothesis that a synergistic effect should result from the spatial organization of guanidinium and heterocycles on a macrocyclic scaffold. Introduction of the bithiazole and bipyridine substituents enhanced the activity of simple phenol derivatives, reaching, for the two Staphylococcus aureus strains in particular, the values obtained for their calixarenic parents. MTT viability assays were carried out to determine selectivity indexes.
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http://dx.doi.org/10.1016/j.bmc.2009.06.040 | DOI Listing |
Biol Pharm Bull
December 2024
Department of Radiation Biosciences, Graduate School of Pharmaceutical Sciences, Tokyo University of Science.
Excessive inflammatory responses to viral infections, known as cytokine storms, are caused by overactivation of endolysosomal Toll-like receptors (TLRs) (TLR3, TLR7, TLR8, and TLR9) and can be lethal, but no specific treatment is available. Some quinoline derivatives with antiviral activity were tried during the recent coronavirus disease 2019 (COVID-19) pandemic, but showed serious toxicity, and their efficacy for treating viral cytokine storms was not established. Here, in order to discover a low-toxicity quinoline derivative as a candidate for controlling virally induced inflammation, we synthesized a series of derivatives of amodiaquine (ADQ), a quinoline approved as an antimalarial, and tested their effects on TLRs-mediated production of inflammatory cytokines and cell viability in vitro.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Department of Food Engineering, Istanbul Technical University, 34469 Maslak, Istanbul, Türkiye. Electronic address:
Black carrot pomace (BCP) is a by-product of colorant production, containing various valuable components with the health promoting effects. In this study, for the first time, BCP was incorporated into a starch-based extruded snack formulation using wheat semolina and corn starch. Total phenolic content, total antioxidant capacity, phenolics, and anthocyanins after processing and in vitro gastrointestinal digestion were investigated, and physical and textural properties of the snack products were determined.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
December 2024
Zhejiang Sci-Tech University, Hangzhou 310018, China. Electronic address:
Excited-state intramolecular proton transfer (ESIPT) reactions are one of the fundamental energy transformation reactions in catalysis and biological process. The combining ESIPT with the twisted intramolecular charge transfer (TICT) brings the richness of optical, photoelectronic performances to certain functional compounds. Delineating the mechanism of ESIPT + TICT reactions and further understanding why a specific functional group dominates are fundamentally crucial for the design and application of the functionally photoelectric materials.
View Article and Find Full Text PDFEcotoxicol Environ Saf
December 2024
College of Natural Resources and Environment, Northwest A&F University, Yangling, Shaanxi 712100, China; Key Laboratory of Plant Nutrition and the Agri-environment in Northwest China, Ministry of Agriculture and Rural Affairs, Yangling, Shaanxi 712100, China. Electronic address:
Dissolved organic matter (DOM) released by straw returning for decomposition interacts with selenium (Se) in soil, which affects the speciation distribution of Se and its bioavailability. However, the relative mechanisms involved are slightly understood. This study investigated the effects of straw-derived DOM on two levels of exogenous selenite (low-Se and high-Se treatments) in two types of soil with distinct pH.
View Article and Find Full Text PDFBMC Res Notes
December 2024
Department of Vegetable Life Science, Graduate School of Medicine, Hirosaki University, 5 Zaifu-cho, Hirosaki, 036-8562, Aomori, Japan.
Objective: Various plants have been reported to contain compounds that promote the transcriptional activity of Nuclear factor erythroid 2-related factor 2 (Nrf2) to induce a set of xenobiotic detoxifying enzymes, such as NAD(P)H-quinone acceptor oxidoreductase 1 (NQO1), via the antioxidant response element (ARE). While conventional methods for evaluating Nrf2 induction potency include measurement of NQO1 activity, an ARE luciferase reporter assay was recently developed to specifically assess Nrf2 induction potency of compounds of interest. In this study, we compared the abilities of these two assays to evaluate and determine Nrf2 induction potency of plant-derived compounds.
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