Search results for "ANTIFUNGAL"
showing 10 items of 348 documents
Zinc oxide nanoparticles for therapeutic purposes in cancer medicine.
2020
The importance of zinc as a trace metal in the human body has long been overlooked. We now gradually discover that the impact of zinc on the health of our body might be as far-reaching as that of iron. Concurrently, nanomaterials containing zinc, in particular zinc oxide nanoparticles (ZnO NPs), are becoming increasingly attractive as innovative agents for medical applications. Zinc oxide is characterized by a good biocompatibility which allows the exploitation of its antibacterial, antifungal, antiviral, and anti-cancer qualities in a therapeutic setting. This perspective outlines the current state of knowledge concerning the interaction of zinc oxide nanoparticles with eukaryotic cells an…
DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.
2019
Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, …
Novel isoquinoline derivatives as antimicrobial agents.
2013
The wide variety of potent biological activities of natural and synthetic isoquinoline alkaloids encouraged us to develop novel antimicrobial isoquinoline compounds. We synthesized a variety of differently functionalized 1-pentyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines (THIQs), including dihydroisoquinolinium salts (2 and 5), methyl pentanoate-THIQ (6), 1-pentanol-THIQ (7), ester derivatives (8-15) and carbamate derivatives (16-23). We employed classic intramolecular Bischler-Napieralski cyclodehydration to generate the isoquinoline core. All the structures were characterized by nuclear magnetic resonance and mass spectrometry. The bactericide and fungicide activities were evaluated f…
Candida biofilms on implanted biomaterials: a clinically significant problem.
2006
In recent years there has been an increasing appreciation that microbial biofilms are ubiquitous, which has resulted in a number of studies on infectious diseases from a biofilm perspective. Biofilms are defined as structured microbial communities that are attached to a surface and encased in a matrix of exopolymeric material. A wide range of biomaterials used in clinical practice have been shown to support colonization and biofilm formation by Candida spp., and the increase in Candida infections in the last decades has almost paralleled the increase and widespread use of a broad range of medical implant devices, mainly in populations with impaired host defenses. Formation of Candida biofil…
Marine biodiversity as source of new drugs
2013
Life in the oceans has an extraordinary biodiversity, including most of plant and animal taxa. Ecological pressures, including competition for space, the fouling of the surface, predation, and successful reproduction have led to the evolution of secondary metabolites and proteins with various biological activities (Cammarata et al. 2011; Maisano et al. 2013). Therefore, marine biodiversity is an exceptional reservoir of natural products, with different structural features from those of terrestrial natural products (Ireland et al. 1988). Only less than 1% of the natural products isolated from marine organisms have been examined for pharmacological activities (Fusetani 2000). These molecules …
The soluble dietary fiber inulin can influence the bioaccessibility of enniatins.
2012
Enniatins (ENs) are bioactive compounds produced by the secondary metabolism of several Fusarium strains and are known to have various biological activities, such as acting as enzyme inhibitors, antifungal antibacterial agents, and immunomodulatory substances. This study investigated the bioaccessibility of the ENs in wheat crispy breads produced with three different inulin concentrations (1, 5 and 10%). The mean bioaccessibility data of the four ENs (A, A(1), B and B(1)) ranged from 68.67% to 84.67 in the experiments carried out without inulin, whereas the data ranged from 51.00 to 74.00% in the experiments carried out with the wheat crispy bread produced with 5 and 10% of the inulin.
Comparison of MALDI-TOF mass spectra with microsatellite length polymorphisms inCandida albicans
2015
Candida albicans is the most frequent yeast involved in human infections. Its population structure can be divided into several genetic clades, some of which have been associated with antifungal susceptibility. Therefore, detecting and monitoring fungal clones in a routine laboratory setting would be a major epidemiological advance. Matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectra results are now widely used as bar codes to identify microorganisms in clinical microbiology laboratories. This study aimed at testing MALDI-TOF mass spectra bar codes to identify clades among a set of C. albicans isolates. Accordingly, 102 clinical strains were genotyped using 10…
Bioactivity of essential oils in phytopathogenic and post-harvest fungi control
2017
[EN] Commercial thyme and lavender essential oils were analysed by GC/MS. Sixty-six compounds accounting for 98.6¿99.6% of total essential oil were identified. Thymol (52.14 ± 0.21%), followed by pcymene (32.24 ± 0.16%), carvacrol (3.71 ± 0.01%) and ¿-terpinene (3.34 ± 0.02%), were the main compounds in thyme essential oil, while large amounts of oxygenated monoterpenes linalool acetate (37.07 ± 0.24%) and linalool (30.16 ± 0.06%) were found in lavender one. In vitro antifungal activity of the essential oils was evaluated at 200 and 300 ¿g/mL against 10 phytopathogenic and post-harvest fungi, which significantly affect agriculture. Micelial growth inhibition was calculated for each tested f…
Studies on puupehenone-metabolites of a Dysidea sp.: structure and biological activity
2007
[EN] Puupchenone (1) and a series of its congeners (2-6) have been isolated from a Dysidea sponge. The unprecedented 20-acetoxyhater-unnadienone (2) exhibiting a five-membered contracted ring, has been characterized. In addition, stereochemical assignment of two previously reported acetone adducts of puupehenone (5 and 6) has been made. Finally, the inhibition of mitochondrial respiratory chain as well as antibacterial and antifungal activities of all compounds has been evaluated. (c) 2006 Elsevier Ltd. All rights reserved.
ChemInform Abstract: New Highly Asymmetric Henry Reaction Catalyzed by CuIIand a C1-Symmetric Aminopyridine Ligand, and Its Application to the Synthe…
2008
A new catalytic asymmetric Henry reaction has been developed that uses a C(1)-symmetric chiral aminopyridine ligand derived from camphor and picolylamine. A variety of aromatic, heteroaromatic, aliphatic, and unsaturated aldehydes react with nitromethane and other nitroalkanes in the presence of DIPEA (1.0 equiv), Cu(OAc)(2)*H(2)O (5 mol %), and an aminopyridine ligand (5 mol %) to give the expected products in high yields (up to 99 %), moderate-to-good diastereoselectivites (up to 82:18), and excellent enantioselectivities (up to 98 %). The reaction is air-tolerant and has been used in the synthesis of the antifungal agent miconazole.