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The Celecoxib Derivative AR-12 Has Broad-Spectrum Antifungal Activity In Vitro and Improves the Activity of Fluconazole in a Murine Model of Cryptococcosis

Only one new class of antifungal drugs has been introduced into clinical practice in the last 30 years, and thus the identification of small molecules with novel mechanisms of action is an important goal of current anti-infective research. Here, we describe the characterization of the spectrum of in vitro activity and in vivo activity ofAR-12, a celecoxib derivative which has been tested in a phase I clinical trial as an anticancer agent.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news

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Authors: El-Housiny S, Shams Eldeen MA, El-Attar YA, Salem HA, Attia D, Bendas ER, El-Nabarawi MA Abstract Solid lipid nanoparticles (SLNs) are very potential formulations for topical delivery of antifungal drugs. Hence, the purpose of this research was to formulate the well-known antifungal agent Fluconazole (FLZ)-loaded SLNs topical gel to improve its efficiency for treatment of Pityriasis Versicolor (PV). FLZ-SLNs were prepared by modified high shear homogenization and ultrasonication method using different concentration of solid lipid (Compritol 888 ATO, Precirol ATO5) and surfactant (Cremophor RH40, Poloxamer ...
Source: Drug Delivery - Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research
Publication date: Available online 9 December 2017 Source:Microbial Pathogenesis Author(s): Ali Mohd Lone, Muneer Ahmad Bhat, Muzafar Ahmad Rather, Wajaht Amin Shah, Zubair Shanib Bhat, Irfan Qadir Tantry, Poonam Prakash The study was designed with an aim to synthesize a series of 2-(((2-ether)amino)methylene)-dimedone derivatives and evaluate the synthesized compounds for antimicrobial activity. Compound library was synthesized by reaction with alkyl, alkenyl, alkynyl and alicyclic bromo-compounds. Characterization of the synthesized compounds was performed by 1H NMR, 13C NMR and mass spectral techniques. The compounds w...
Source: Microbial Pathogenesis - Category: Infectious Diseases Source Type: research
In this study, we attempted to improve the incorporation capacity of a displayed heterologous enzyme by disrupting a native cell-wall protein. β-Glucosidase (BGL1) from Aspergillus aculeatus was fused with Saccharomyces cerevisiae Sed1 and displayed on the cell surface of S. cerevisiae BY4741 strain and its SED1 disruptant. Sed1 is one of the most abundant stationary phase yeast cell wall protein. A time course analysis revealed that BGL1 activity of the control strain reached saturation after 48 h of cultivation. In contrast, the BGL1 activity of the SED1 disruptant increased until 72 h of cultivation ...
Source: Journal of Bioscience and Bioengineering - Category: Biomedical Science Source Type: research
Publication date: Available online 6 December 2017 Source:Journal of Hospital Infection Author(s): Ruth-Aoibheann OLeary, Sharon Einav, Marc Leone, Krisztina Madách, Claude Martin, Ignacio Martin-Loeches Objective The global burden of invasive fungal disease is increasing. Candida albicans remains the leading cause of fungal blood stream infections although non-albicans Candidal infections are emerging. Areas of controversy regarding diagnosis and management are hampering our ability to respond effectively to this evolving threat. The purpose of this narrative review is to address current controversies and provide ...
Source: Journal of Hospital Infection - Category: Infectious Diseases Source Type: research
Conclusions: Frequency of infection in APAP cases were similar to the previous report. Infection might improve or deteriorate the clinical course of APAP.Financial support: This study was partially granted from AMED; DLD/14526278 to Y. Inoue and T. Arai and PAP/14526182 to Y. Inoue.
Source: European Respiratory Journal - Category: Respiratory Medicine Authors: Tags: Diffuse Parenchymal Lung Disease Source Type: research
Authors: Kano R Abstract  Canine and feline upper respiratory tract (URT) infection due to Aspergillus spp. is considered an emerging disease, with the number of reported cases continuing to rise in Japan. Aspergillus fumigatus has been the most frequently reported etiologic agent of sino-orbital aspergillosis in dogs and cats; the other Aspergillus species, Aspergillus felis, Aspergillus fischeri, Aspergillus udagawae, Aspergillus viridinutans, and A. fumigatus, have also been implicated in feline cases. The minimum inhibitory concentrations (MICs) of antifungal drugs are elevated for these cryptic species co...
Source: Medical Mycology Journal - Category: Biology Tags: Med Mycol J Source Type: research
Only one new class of antifungal drugs has been introduced into clinical practice in the last 30 years, and thus the identification of small molecules with novel mechanisms of action is an important goal of current anti-infective research. Here, we describe the characterization of the spectrum of in vitro activity and in vivo activity of AR-12, a celecoxib derivative which has been tested in a phase I clinical trial as an anticancer agent. AR-12 inhibits fungal acetyl coenzyme A (acetyl-CoA) synthetase in vitro and is fungicidal at concentrations similar to those achieved in human plasma.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
Abstract Diagnostic tools for invasive fungal infections have continuously improved within the last decades. Nowadays, cultural methods, antigen testing, and molecular tests, such as polymerase chain reaction, are widely used. These methods, however, are accompanied with different limitations as various availability, various turnaround time or high costs. A new generation of point-of-care test has shown promising results in various studies and may overcome some of these limitations. We therefore reviewed the literature for the most promising new point-of-care tests for invasive aspergillosis (Aspergillus-specific ...
Source: Current Fungal Infection Reports - Category: Infectious Diseases Source Type: research
Abstract Every year, Candida, Aspergillus, Cryptococcus and Pneumocystis infect an estimated two million individuals worldwide. Most are immunocompromised or critically ill. Candida is the most common fungal pathogen of the critically ill and of recipients of transplanted abdominal organs. In high-risk haemato-oncological patients, in contrast, the introduction of antifungal prophylaxis with fluconazole and later with mould-active posaconazole has led to a remarkable reduction of invasive candidiasis and is likely to have a similar effect on invasive aspergillosis. Invasive aspergillosis remains the dominant invas...
Source: Swiss Medical Weekly - Category: Journals (General) Authors: Tags: Swiss Med Wkly Source Type: research
We report a case of 60 years old immunocompetent female, presented with cough, chest pain and shortness of breath. The chest X-ray showed a large thick walled cavity in the lower and mid zone of right lung with positive water lily sign. Surgical enucleation of the echinococcal cyst revealed aspergilloma involving the cavity with massive invasion of laminated ectocyst by filamentous fungus, morphologically resembling an Aspergillus species and was further treated with Itraconazole for 3 months. This unique coexistence of active pulmonary echinococcosis and aspergillosis is being reported because of its rarity and clinical i...
Source: Ghana Medical Journal - Category: African Health Tags: Ghana Med J Source Type: research
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