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https://www.readbyqxmd.com/read/28329820/hepatocellular-toxicity-of-imidazole-and-triazole-antimycotic-agents
#1
Patrizia Haegler, Lorenz Joerin, Stephan Krähenbühl, Jamal Bouitbir
Hepatotoxicity has been described for all antimycotic azoles currently marketed. A possible mechanism involving mitochondrial dysfunction has been postulated for ketoconazole, but not for the other azoles. The aim of the current investigations was to study the toxicity of different azoles in human cell models and to find out mechanisms of their toxicity. In HepG2 cells, posaconazole and ketoconazole were cytotoxic starting at 20 and 50 µM and decreased the cellular ATP content starting at 5 and 10 µM, respectively...
January 27, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28323096/nanoparticles-as-safe-and-effective-delivery-systems-of-antifungal-agents-achievements-and-challenges
#2
REVIEW
Ghareb M Soliman
Invasive fungal infections are becoming a major health concern in several groups of patients leading to severe morbidity and mortality. Moreover, cutaneous fungal infections are a major cause of visits to outpatient skin clinics. Despite the availability of several effective agents in the antifungal drug arena, their therapeutic outcome is less than optimal due to limitations related to drug physicochemical properties and toxicity. For instance, poor aqueous solubility limits the formulations options and efficacy of several azole antifungal drugs while toxicity limits the benefits of many other drugs...
March 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28322011/fcrav2-a-gene-with-rogdi-domain-involved-in-fusarium-head-blight-and-crown-rot-on-durum-wheat-caused-by-fusarium-culmorum
#3
Francesca Spanu, Barbara Scherm, Irene Camboni, Virgilio Balmas, Giovanna Pani, Safa Oufensou, Nicolo' Macciotta, Matias Pasquali, Quirico Migheli
Fusarium culmorum is a soil-borne fungal pathogen able to cause foot and root rot and Fusarium head blight on small grain cereals, particularly on wheat and barley. It causes significant yield and quality loss and results in the contamination of kernels with type B trichothecene mycotoxins. Knowledge on pathogenicity factors of this fungus is still limited. A transposon tagging approach based on the mimp1/impala double component system has allowed us to select a mutant altered in multiple metabolic and morphological processes, trichothecene production and virulence...
March 21, 2017: Molecular Plant Pathology
https://www.readbyqxmd.com/read/28317305/invasive-pulmonary-aspergillosis-due-to-azole-resistant-aspergillus-lentulus
#4
Nobuyuki Tetsuka, Takashi Yaguchi, Hiroyuki Machida, Shuichi Ito, Isao Miyairi
No abstract text is available yet for this article.
March 2017: Pediatrics International: Official Journal of the Japan Pediatric Society
https://www.readbyqxmd.com/read/28299183/challenges-in-microbiological-diagnosis-of-invasive-aspergillus-infections
#5
REVIEW
Alexandre Alanio, Stéphane Bretagne
Invasive aspergillosis (IA) has been increasingly reported in populations other than the historical hematology patients and there are new questions about the performance of microbiological tools. Microscopy and culture have been completed by biomarkers, either antigens or DNA, and in blood or respiratory specimens or both. First studied in hematology, the antigen galactomannan performance in serum is low in other patient populations where the pathophysiology of the infection can be different and the prevalence of IA is much lower...
2017: F1000Research
https://www.readbyqxmd.com/read/28295690/azole-resistance-in-candida-albicans-from-animals-highlights-on-efflux-pump-activity-and-gene-overexpression
#6
Marcos Fábio Gadelha Rocha, Silviane Praciano Bandeira, Lucas Pereira de Alencar, Luciana Magalhães Melo, Jamille Alencar Sales, Manoel de Araújo Neto Paiva, Carlos Eduardo Cordeiro Teixeira, Débora de Souza Collares Maia Castelo-Branco, Waldemiro de Aquino Pereira-Neto, Rossana de Aguiar Cordeiro, José Júlio Costa Sidrim, Raimunda Sâmia Nogueira Brilhante
This study investigated potential mechanisms of azole resistance among Candida albicans from animals, including efflux pump activity, ergosterol content and gene expression. For this purpose, 30 azole-resistant C. albicans strains from animals were tested for their antifungal susceptibility, according to document M27-A3, efflux pump activity by rhodamine 6G test, ergosterol content and expression of the genes CDR1, CDR2, MDR1, ERG11 by RT-qPCR. These strains were resistant to at least one azole derivative...
March 10, 2017: Mycoses
https://www.readbyqxmd.com/read/28294249/visible-light-mediated-c2-amination-of-thiophenes-by-using-ddq-as-an-organophotocatalyst
#7
Chunlan Song, Hong Yi, Bowen Dou, Yiying Li, Atul K Singh, Aiwen Lei
In this work, a direct C-H activation of thiophenes was presented via an oxidation pathway under visible-light irradiation, in which the thiophene radical cation serves as the key intermediate. Various thiophenes and azoles could be transformed into the corresponding amination products well, and H2O was the only byproduct which is environmentally benign. Our results showed that tert-butyl nitrite (TBN) served as the electron transfer mediator and O2 as the terminal oxidant to regenerate the photocatalyst DDQ and revive the photocatalytic cycle...
March 15, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28293420/candidemia-in-a-major-regional-tertiary-referral-hospital-epidemiology-practice-patterns-and-outcomes
#8
Jocelyn Qi-Min Teo, Samuel Rocky Candra, Shannon Jing-Yi Lee, Shannon Yu-Hng Chia, Hui Leck, Ai-Ling Tan, Hui-Peng Neo, Kenneth Wei-Liang Leow, Yiying Cai, Rachel Pui-Lai Ee, Tze-Peng Lim, Winnie Lee, Andrea Lay-Hoon Kwa
BACKGROUND: Candidemia is a common cause of nosocomial bloodstream infections, resulting in high morbidity and mortality. This study was conducted to describe the epidemiology, species distribution, antifungal susceptibility patterns and outcomes of candidemia in a large regional tertiary referral hospital. METHODS: A retrospective surveillance study of patients with candidemia was conducted at Singapore General Hospital between July 2012 and December 2015. In addition, incidence densities and species distribution of candidemia episodes were analysed from 2008 to 2015...
2017: Antimicrobial Resistance and Infection Control
https://www.readbyqxmd.com/read/28282632/evaluation-of-the-combination-mode-of-azoles-antifungal-inhibitors-with-cacyp51-and-the-influence-of-site-directed-mutation
#9
Bin Sun, Wanxu Huang, Min Liu
14α-demethylase (CYP51) is an essential metabolic enzyme for fungal survival and has been considered as an interesting target for the development of new antifungal inhibitors. Azoles antifungal inhibitors in the treatment of fungal diseases are good candidates via the interaction with the target enzyme CYP51 of fungus. In the study, we constructed the homology model for Candida albicans CYP51 (CACYP51) and analyzed the active site. In order to better understand the structural characteristics of azoles inhibitors and combination mode, the common feature pharmacophore model and the molecular docking were performed...
February 21, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28282366/comparing-azole-plasma-trough-levels-in-lung-transplant-recipients-percentage-of-therapeutic-levels-and-intrapatient-variability
#10
Daniela Stelzer, Alexandra Weber, Franziska Ihle, Sandhya Matthes, Felix Ceelen, Gregor Zimmermann, Nikolaus Kneidinger, Rene Schramm, Hauke Winter, Michael Zoller, Michael Vogeser, Juergen Behr, Claus Neurohr
BACKGROUND: This study compared therapeutic azole plasma trough levels (APL) of the azole antimycotics itraconazole (ITR), voriconazole (VOR), and posaconazole (POS) in lung transplant recipients and analyzed the influencing factors. In addition, intrapatient variability for each azole was determined. METHODS: From July 2012 to July 2015, 806 APL of ITR, VOR, posaconazole liquid (POS-Liq), and posaconazole tablets (POS-Tab) were measured in 173 patients of the Munich Lung Transplantation Program...
April 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28264849/genetic-diversity-and-in-vitro-antifungal-susceptibility-of-200-clinical-and-environmental-aspergillus-flavus-isolates
#11
Mojtaba Taghizadeh-Armaki, Mohammad Taghi Hedayati, Saham Ansari, Saeed Mahdavi Omran, Sasan Saber, Haleh Rafati, Jan Zoll, Henrich A van der Lee, Willem J G Melchers, Paul E Verweij, Seyedmojtaba Seyedmousavi
Aspergillus flavus has been frequently reported as the leading cause of invasive aspergillosis in certain tropical and sub-tropical countries.Two hundred A. flavus strains originating from clinical and environmental sources and collected between 2008 and 2015 were phylogenetically identified at the species level by analyzing partial β-tubulin and calmodulin genes. In vitro antifungal susceptibility testing was performed against antifungals using the EUCAST (European Committee on Antimicrobial Susceptibility Testing) broth microdilution method...
March 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28264842/contributions-of-both-atp-binding-cassette-transporter-and-cyp51a-proteins-are-essential-for-azole-resistance-in-aspergillus-fumigatus
#12
Sanjoy Paul, Daniel Diekema, W Scott Moye-Rowley
While azole drugs targeting the biosynthesis of ergosterol are effective antifungal agents, their extensive use has led to the development of resistant organisms. Infections involving azole resistant forms of the filamentous fungus Aspergillus fumigatus are often associated with genetic changes in the cyp51A gene encoding the lanosterol α14 demethylase target enzyme. Both a sequence duplication in the cyp51A promoter (TR34) as well as a substitution mutation in the coding sequence (L98H) are required for full expression of azole resistance...
March 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28263823/embryotoxic-and-pharmacologic-potency-ranking-of-six-azoles-in-the-rat-whole-embryo-culture-by-morphological-and-transcriptomic-analysis
#13
Myrto Dimopoulou, Aart Verhoef, Jeroen L A Pennings, Bennard van Ravenzwaay, Ivonne M C M Rietjens, Aldert H Piersma
Differential gene expression analysis in the rat whole embryo culture (WEC) assay provides mechanistic insight into the embryotoxicity of test compounds. In our study, we hypothesized that comparative analysis of the transcriptomes of rat embryos exposed to six azoles (flusilazole, triadimefon, ketoconazole, miconazole, difenoconazole and prothioconazole) could lead to a better mechanism-based understanding of their embryotoxicity and pharmacological action. For evaluating embryotoxicity, we applied the total morphological scoring system (TMS) in embryos exposed for 48h...
March 3, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28260509/adsorption-of-antifungal-drugs-inside-pristine-and-functionalized-fullerenes-and-nanotubes-dft-investigation
#14
Tomasz Pieńko, Monika Grudzień, Przemysław Paweł Taciak, Aleksander Paweł Mazurek
BACKGROUND: Econazole, sulconazole and tioconazole usage as antifungal agents is limited due to poor pharmacokinetic properties. Pristine and hydroxylated structures of the C240 fullerene and single walled carbon nanotube (SWCNT) were proposed as transporters of these imidazoles potentially enhancing their pharmacokinetics. METHODS: To assess possibility of creation of the endohedral complexes of the azoles and carbon nanostructures, their adsorption and interaction energies were calculated with the hybrid exchange-correlation density functional B97-1 and 6-31(d,p) basis set...
March 3, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28259787/development-of-a-common-carp-cyprinus-carpio-pregnane-x-receptor-cpxr-transactivation-reporter-assay-and-its-activation-by-azole-fungicides-and-pharmaceutical-chemicals
#15
Anke Lange, Jenna Corcoran, Shinichi Miyagawa, Taisen Iguchi, Matthew J Winter, Charles R Tyler
In mammals, the pregnane X receptor (PXR) is a transcription factor with a key role in regulating expression of several genes involved in drug biotransformation. PXR is present in fish and some genes known to be under its control can be up-regulated by mammalian PXR ligands. Despite this, direct involvement of PXR in drug biotransformation in fish has yet to be established. Here, the full length PXR sequence was cloned from carp (Cyprinus carpio) and used in a luciferase reporter assay to elucidate its role in xenobiotic metabolism in fish...
March 1, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28258218/structural-analyses-of-candida-albicans-sterol-14%C3%AE-demethylase-complexed-with-azole-drugs-address-the-molecular-basis-of-azole-mediated-inhibition-of-fungal-sterol-biosynthesis
#16
Tatiana Y Hargrove, Laura Friggeri, Zdzislaw Wawrzak, Aidong Qi, William J Hoekstra, Robert J Schotzinger, John D York, F Peter Guengerich, Galina I Lepesheva
With some advances in modern medicine (such as cancer chemotherapy, broad exposure to antibiotics, and immunosuppression) the incidence of opportunistic fungal pathogens such as Candida albicans has increased. Cases of drug resistance among these pathogens have become more frequent, requiring the development of new drugs and a better understanding of the targeted enzymes. Sterol 14α-demethylase (CYP51) is a cytochrome P450 enzyme required for biosynthesis of sterols in eukaryotic cells and the major target of clinical drugs for managing fungal pathogens, but some of the CYP51 key features important for rational drug design have remained obscure...
March 3, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28256131/ycao-dependent-posttranslational-amide-activation-biosynthesis-structure-and-function
#17
Brandon J Burkhart, Christopher J Schwalen, Greg Mann, James H Naismith, Douglas A Mitchell
With advances in sequencing technology, uncharacterized proteins and domains of unknown function (DUFs) are rapidly accumulating in sequence databases and offer an opportunity to discover new protein chemistry and reaction mechanisms. The focus of this review, the formerly enigmatic YcaO superfamily (DUF181), has been found to catalyze a unique phosphorylation of a ribosomal peptide backbone amide upon attack by different nucleophiles. Established nucleophiles are the side chains of Cys, Ser, and Thr which gives rise to azoline/azole biosynthesis in ribosomally synthesized and posttranslationally modified peptide (RiPP) natural products...
March 3, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28250360/a-new-amino-acid-substitution-at-g150s-in-lanosterol-14-%C3%AE-demethylase-erg11-protein-in-multi-azole-resistant-trichosporon-asahii
#18
Hisako Kushima, Issei Tokimatsu, Hiroshi Ishii, Rie Kawano, Kentaro Watanabe, Jun-Ichi Kadota
The mechanisms of azole resistance in Trichosporon asahii have not yet been fully clarified. We previously showed that T. asahii has the ERG11 gene, coding lanosterol 14-α-demethylase (Erg11 protein; Erg11p), which is the primary target of azoles. A single amino acid substitution at G453R in Erg11p was found to induce changes in the affinity of this enzyme for azoles, especially fluconazole, in vitro. In the present study, we investigated the DNA sequences of the ERG11 gene using six different strains of clinically isolated T...
2017: Medical Mycology Journal
https://www.readbyqxmd.com/read/28249055/weakness-and-pain-in-arms-and-legs-%C3%A2-dark-urine-%C3%A2-history-of-vertebral-osteomyelitis-%C3%A2-dx
#19
Antonios Charokopos, Tariq Muhammad, Sidana Surbhi, Andrei Brateanu
Rhabdomyolysis is a serious complication of statin treatment. Both higher statin doses and pharmacokinetic factors can raise statin levels, leading to this serious usclerelated syndrome. Co-administration of statins with drugs that are strong inhibitors of cytochrome P450 (CYP) 3A4 (the main cytochrome P450 isoform that metabolizes most statins) can increase statin levels several fold. The trigger for our patient's statin-induced rhabdomyolysis was fluconazole, a known moderate inhibitor of CYP3A4, which is comparatively weaker than certain potent azoles like itraconazole or ketoconazole...
March 2017: Journal of Family Practice
https://www.readbyqxmd.com/read/28248527/accessing-n-acyl-azoles-via-oxoammonium-salt-mediated-oxidative-amidation
#20
John M Ovian, Christopher B Kelly, Vincent A Pistritto, Nicholas E Leadbeater
An operationally simple, robust, metal-free approach to the synthesis of N-acyl azoles from both alcohols and aldehydes is described. Oxidative amidation is facilitated by a commercially available organic oxidant (4-acetamido-2,2,6,6-tetramethylpiperidine-1-oxoammonium tetrafluoroborate) and proceeds under very mild conditions for an array of structurally diverse substrates. Tandem reactions of these activated amides, such as transamidation and esterification, enable further elaboration. Also, the spent oxidant can be recovered and used to regenerate the oxoammonium salt...
March 1, 2017: Organic Letters
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