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antifungal drugs

Ross D Blundell, Simon J Williams, Samantha D M Arras, Jessica L Chitty, Kirsten L Blake, Daniel J Ericsson, Nidhi Tibrewal, Jurgen Rohr, Y Q Andre E Koh, Ulrike Kappler, Avril A B Robertson, Mark S Butler, Matthew A Cooper, Bostjan Kobe, James A Fraser
Opportunistic fungal pathogens such as Cryptococcus neoformans are a growing cause of morbidity and mortality among immunocompromised populations worldwide. To address the current paucity of antifungal therapeutic agents, further research into fungal-specific drug targets is required. Adenylosuccinate synthetase (AdSS) is a crucial enzyme in the adeosine triphosphate (ATP) biosynthetic pathway, catalyzing the formation of adenylosuccinate from inosine monophosphate and aspartate. We have investigated the potential of this enzyme as an antifungal drug target, finding that loss of function results in adenine auxotrophy in C...
September 9, 2016: ACS Infectious Diseases
MyungHee Ku, Yong-Un Baek, Min-Kyu Kwak, Sa-Ouk Kang
BACKGROUND: Glutathione reductase maintains the glutathione level in a reduced state. As previously demonstrated, glutathione is required for cell growth/division and its biosynthesizing-enzyme deficiency causes methylglyoxal accumulation. However, experimental evidences for reciprocal relationships between Cph1-/Efg1-mediated signaling pathway regulation and methylglyoxal production exerted by glutathione reductase on yeast morphology remain unclear. METHODS: Glutathione reductase (GLR1) disruption/overexpression were performed to investigate aspects of pathological/morphological alterations in Candida albicans...
October 14, 2016: Biochimica et Biophysica Acta
Petra Füredi, Zsófia Edit Pápay, Kristóf Kovács, Borbála Dalmadi Kiss, Krisztina Ludányi, István Antal, Imre Klebovich
The number of topical fungal infections is growing, mostly owing to immunosuppressive therapy. Several topical fungal infections, such as eye mycoses, can be treated by local administration of antimycotic drugs. One major group of the antifungal agents is triazole, such as voriconazole (VCZ), which is used as the first line treatment of aspergillosis. A disadvantage of VCZ is its low water solubility making the drug difficult to administer in a liquid preparation. The lipid-based nanoparticles (LNP) have attracted increasing attention due to their advantageous properties...
October 1, 2016: Journal of Pharmaceutical and Biomedical Analysis
Nicole Robbins, Michaela Spitzer, Wenliang Wang, Nicholas Waglechner, Dhruv J Patel, Jonathan S O'Brien, Linda Ejim, Obi Ejim, Mike Tyers, Gerard D Wright
Natural products are invaluable historic sources of drugs for infectious diseases; however, the discovery of novel antimicrobial chemical scaffolds has waned in recent years. Concurrently, there is a pressing need for improved therapeutics to treat fungal infections. We employed a co-culture screen to identify ibomycin, a large polyketide macrolactone that has preferential killing activity against Cryptococcus neoformans. Using chemical and genome methods, we determined the structure of ibomycin and identified the biosynthetic cluster responsible for its synthesis...
October 7, 2016: Cell Chemical Biology
Andrés Felipe Cartagena, Luís Antonio Esmerino, Rogerio Polak-Junior, Sibelli Olivieri Parreiras, Milton Domingos Michél, Paulo Vitor Farago, Nara Hellen Campanha
OBJECTIVE: The purpose of this study was to develop a new oral drug delivery system by incorporating polymeric miconazole nitrate (MN) microparticles on an experimental antifungal denture adhesive (DA). METHODS: Spray drying Eudragit L-100 (E) and Gantrez MS-955 (G) MN-microparticles were incorporated in DA. DAE1, DAG1, DAEG1, DAE2, DAG2, DAEG2 groups were obtained from the combination of polymers used in MN-microparticles (E, G and EG) and concentration of MN into DA (1, for 1% and 2, for 2%)...
October 10, 2016: Dental Materials: Official Publication of the Academy of Dental Materials
Sudipta Saha, Vinit Raj, Amit Rai
The chemistry of heterocyclic containing, 1,3,4-thiadiazole has been an interesting field of study from ancient years. Subsequently, 1,3,4-thiadiazole nucleus constitutes a significant class of compounds for new drug development. Recently, various 1,3,4-thiadiazole derivatives have been synthesized and evaluated their biological activities including antimicrobial, antituberculosis, antioxidant, anti-inflammatory, anticonvulsants, antidepressant and anxiolytic, antihypertensive, anticancer and antifungal activity...
October 13, 2016: Anti-cancer Agents in Medicinal Chemistry
Atefeh Abdollahi Gohar, Hamid Badali, Tahereh Shokohi, Mojtaba Nabili, Nasrin Amirrajab, Maryam Moazeni
Clinical management of fungal diseases is compromised by the emergence of antifungal drug resistance in fungi, which leads to elimination of available drug classes as treatment options. An understanding of antifungal resistance at molecular level is, therefore, essential for the development of strategies to combat the resistance. This study presents the assessment of molecular mechanisms associated with fluconazole resistance in clinical Candida glabrata isolates originated from Iran. Taking seven distinct fluconazole-resistant C...
October 15, 2016: Mycopathologia
João Paulo Zen Siqueira, Deanna A Sutton, Dania García, Josepa Gené, Pamela Thomson, Nathan Wiederhold, Josep Guarro
Aspergillus section Versicolores includes species of clinical relevance and many others that have been poorly studied but are occasionally found in clinical samples. The aim of this study was to investigate, using a multilocus phylogenetic approach, the spectrum of species of the section Versicolores and to determine their in vitro antifungal susceptibility. The study was based on a set of 77 clinical isolates from different USA medical centres, which had been previously identified as belonging to this section...
November 2016: Fungal Biology
Juliana Hotta, Wilson Gustavo Cral, Vinicius Tatsuyuji Sakima, Vanessa Soares Lara, Vanessa Migliorini Urban, Karin Hermana Neppelenbroek
BACKGROUND: Antifungal agents incorporated into temporary denture resilient liners as drug carries and delivery have been suggested as an alternative treatment for denture stomatitis. However, to test the in vivo biocompatibility of this protocol, standardization of an intraoral device for optimal drug delivery is required. OBJECTIVE: Standardized criteria were produced to adjust an acrylic intraoral device (IOD) for rats feasible for denture stomatitis treatment by sustained drug-delivery based on minimal inhibitory drug concentrations (MICs) of antifungals for Candida albicans biofilm...
October 13, 2016: Current Drug Delivery
Tanvi Shekhar-Guturja, Walters Aji Tebung, Harley Mount, Ningning Liu, Julia R Köhler, Malcolm Whiteway, Leah E Cowen
Invasive fungal infections are a leading cause of human mortality. Effective treatment is hindered by the rapid emergence of resistance to the limited number of antifungal drugs, demanding new strategies to treat life-threatening fungal infections. Here, we explore a powerful strategy to enhance antifungal efficacy using the natural product beauvericin against leading human fungal pathogens. We found that beauvericin potentiates the activity of azole antifungals against azole-resistant Candida isolates via inhibition of multidrug efflux, and that beauvericin itself is effluxed via Yor1...
October 10, 2016: Antimicrobial Agents and Chemotherapy
Yaseen A M M Elshaier, Assem Barakat, Bander M Al-Qahtany, Abdullah Mohammed Al-Majid, Mohamed H Al-Agamy
A one-pot reaction was described that results in various pyrazole-thiobarbituric acid derivatives as new pharmacophore agents. These new heterocycles were synthesized in high yields with a broad substrate scope under mild reaction conditions in water mediated by NHEt₂. The molecular structures of the synthesized compounds were assigned based on different spectroscopic techniques. The new compounds were evaluated for their antibacterial and antifungal activity. Compounds 4h and 4l were the most active compounds against C...
October 9, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Si-Sun Choi, Hee-Ju Nah, Hye-Rim Pyeon, Eung-Soo Kim
Tautomycetin (TMC) is a natural product with a linear structure that includes an ester bond connecting a dialkylmaleic moiety to a type I polyketide chain. Although TMC was originally identified as an antifungal antibiotic in the late 1980s, follow-up studies revealed its novel immunosuppressant activity. Specifically, TMC exhibited a mechanistically unique immunosuppressant activity about 100 times higher than that of cyclosporine A, a widely used immunosuppressant drug. Interestingly, a structurally close relative, tautomycin (TTM), was reported to not possess TMC-like immunosuppressant activity, suggesting that a distinctive polyketide moiety of TMC plays a critical role in immunosuppressant activity...
October 12, 2016: Journal of Industrial Microbiology & Biotechnology
Eric F Kong, Christina Tsui, Sona Kucharíková, David Andes, Patrick Van Dijck, Mary Ann Jabra-Rizk
: Biofilm-associated polymicrobial infections, particularly those involving fungi and bacteria, are responsible for significant morbidity and mortality and tend to be challenging to treat. Candida albicans and Staphylococcus aureus specifically are considered leading opportunistic fungal and bacterial pathogens, respectively, mainly due to their ability to form biofilms on catheters and indwelling medical devices. However, the impact of mixed-species biofilm growth on therapy remains largely understudied...
October 11, 2016: MBio
Sean X Zhang, Nathan P Wiederhold
Yeasts are unicellular organisms that reproduce mostly by budding and less often by fission. Most medically important yeasts originate from Ascomycota or Basidiomycota. Here, we review taxonomy, epidemiology, disease spectrum, antifungal drug susceptibility patterns of medically important yeast, laboratory diagnosis, and diagnostic strategies.
August 2016: Microbiology Spectrum
Jing Shao, GaoXiang Shi, TianMing Wang, DaQiang Wu, ChangZhong Wang
Candida tropicalis has emerged as an important pathogenic fungus in nosocomial infections due to its recalcitrant resistance to conventional antifungal agents, especially to fluconazole (FLC). Berberine (BBR) is a bioactive herbal-originated alkaloids and has been reported to possess antifungal functions against C. albicans. In this paper, we tried to figure out the antifungal mechanisms of BBR and/or FLC in a clinical C. tropicalis isolate 2006. In the microdilution test, the minimum inhibitory concentration (MIC) of BBR was found 16 μg/mL with fractional inhibitory concentration index (FICI) 0...
2016: Frontiers in Microbiology
Andrés Felipe Cartagena, Amanda Lyra, Aline Cristina Kapuchczinski, Amanda Miglirioni Urban, Luiz Antônio Esmerino, Traudi Klein, Jessica Mendes Nadal, Paulo Vitor Farago, Nara Hellen Campanha
The aim of this study was to prepare and to evaluate Eudragit L100 and Gantrez MS-955 microparticles containing miconazole nitrate for buccal delivery. Microparticles were prepared by spray-drying method in order to achieve high encapsulation efficiency and increased drug solubility. The microparticles were obtained containing 10% and 20% (w/w) of drug:polymer ratio using Eudragit L100 (E10 and E20), Gantrez MS-955 (G10 and G20) or their combination (EG10 and EG20). The influence of formulation factors (drug:polymer ratio, type of polymer) on yield, encapsulation efficiency, particle size, Fourier-transformed infrared spectroscopy (FTIR), X-ray diffraction, differential scanning calorimetry, in vitro drug release and antifungal activity were investigated...
October 6, 2016: Current Drug Delivery
Aly A Abdelbary, Wessam H Abd-Elsalam, Abdulaziz M Al-Mahallawi
The objective of this work was to encapsulate terconazole (TCZ), a water insoluble antifungal drug, into novel ultradeformable bilosomes (UBs) for achieving enhanced ocular delivery. In addition to the constituents of the conventional bilosomes; namely, Span 60, cholesterol, and the bile salts, UBs contain an edge activator which imparts extra elasticity to the vesicles and consequently hypothesized to result in improved corneal permeation. In this study, TCZ loaded UBs were prepared utilizing ethanol injection method according to 2(3) full factorial design...
October 4, 2016: International Journal of Pharmaceutics
Raphaële Nové-Josserand, Soazic Grard, Lila Auzou, Philippe Reix, Marlène Murris-Espin, François Brémont, Benyebka Mammar, Laurent Mely, Dominique Hubert, Isabelle Durieu, Pierre-Régis Burgel
Allergic bronchopulmonary aspergillosis (ABPA) affects up to 15% of patients with cystic fibrosis (CF). Corticosteroids are used as first-line therapy, but relapse and adverse effects commonly occur. Case reports have suggested the efficacy of the anti-IgE recombinant humanized monoclonal antibody omalizumab. A retrospective multicenter observational French study retrieved 32 CF patients (11 children and 21 adults) who have received omalizumab for more than 3 months in the context of ABPA. Clinical characteristics, concomitant medications (inhaled and oral corticosteroids, antifungal drugs), lung function, body mass index (BMI), and serum IgE were compared at the start and during the first year of omalizumab therapy...
October 7, 2016: Pediatric Pulmonology
Maria Clara Padovani de Souza, Andrezza Gouvêa Dos Santos, Adriano Max Moreira Reis
Background The inappropriate use of systemic antifungal agents can result in unnecessary exposure, adverse events, increased microbial resistance and increased costs. Aim This study analysed the use of systemic antifungal agents and adherence to treatment guidelines for fungal infections. Setting A Brazilian tertiary hospital. Methods This cross-sectional study investigated 183 patients who were treated with systemic antifungals. Antifungal drugs were classified according to the fourth level of the Anatomical Therapeutic Chemical classification system...
October 6, 2016: International Journal of Clinical Pharmacy
Andrée F Maheux, Adnane Sellam, Yves Piché, Maurice Boissinot, René Pelletier, Dominique K Boudreau, François J Picard, Hélène Trépanier, Marie-Josée Boily, Marc Ouellette, Paul H Roy, Michel G Bergeron
Successful treatment of a Candida infection relies on 1) an accurate identification of the pathogenic fungus and 2) on its susceptibility to antifungal drugs. In the present study we investigated the level of correlation between phylogenetical evolution and susceptibility of pathogenic Candida spp. to antifungal drugs. For this, we compared a phylogenetic tree, assembled with the concatenated sequences (2475-bp) of the ATP2, TEF1, and TUF1 genes from 20 representative Candida species, with published minimal inhibitory concentrations (MIC) of the four principal antifungal drug classes commonly used in the treatment of candidiasis: polyenes, triazoles, nucleoside analogues, and echinocandins...
October 3, 2016: Journal of Microbiological Methods
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