Search results for "Antifungal"

Community Composition, Antifungal Activity and Chemical Analyses of Ant-Derived Actinobacteria

2020

Actinobacteria associated with insects represent one potentially rich source of novel natural products with antifungal activity. Here, we investigated the phylogenetic diversity and community composition of actinobacteria associated with ants using a combination of culture-dependent and -independent methods. Further, we assessed the antagonistic activity against phytopathogenic fungi and identified the secondary metabolites from isolates with bioactivity. A total of 416 actinobacterial isolates were obtained from three ant species (Camponotus japonicus, Lasius fuliginosus, and Lasius flavus) located in five nests. The largest amount of isolates were observed in the head samples. 16S rRNA ge…

Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1,3-(benzo)thiazol-2-…

2012

Abstract A series of new N-[(benzo)thiazol-2-yl]-2/3-[3,4-dihydroisoquinolin-2(1H)-yl]ethan/propanamide derivatives was synthesized and characterized by 1H, 13C NMR and IR spectroscopy and mass-spectrometry. A single crystal X-ray study of N-(1,3-benzothiazol-2-yl)-2-[3,4-dihydroisoquinolin-2(1H)-yl]ethanamide is reported to determine its conformational feature. The investigated compounds were found to be active in psychotropic in vivo, anti-inflammatory in vivo and cytotoxicity in vitro screening. They possess marked sedative action, reveal high anti-inflammatory activity, have selective cytotoxic effects and NO-induction ability concerning tumour cell lines. Some of the compounds synthesi…

An enantioselective synthesis of the C(33)–C(37) fragment of Amphotericin B

2003

An enantioselective synthesis of the C(33)–C(37) tripropionate fragment of Amphotericin B has been developed in only 6 steps. Peer reviewed

Itraconazole inhibits nuclear delivery of extracellular vesicle cargo by disrupting the entry of late endosomes into the nucleoplasmic reticulum

2021

ABSTRACT Extracellular vesicles (EVs) are mediators of intercellular communication under both healthy and pathological conditions, including the induction of pro‐metastatic traits, but it is not yet known how and where functional cargoes of EVs are delivered to their targets in host cell compartments. We have described that after endocytosis, EVs reach Rab7+ late endosomes and a fraction of these enter the nucleoplasmic reticulum and transport EV biomaterials to the host cell nucleoplasm. Their entry therein and docking to outer nuclear membrane occur through a tripartite complex formed by the proteins VAP‐A, ORP3 and Rab7 (VOR complex). Here, we report that the antifungal compound itracona…

Design and Synthesis of Novel 1,3-Thiazole and 2-Hydrazinyl-1,3-Thiazole Derivatives as Anti-

2019

In the context of there being a limited number of clinically approved drugs for the treatment of Candida sp.-based infections, along with the rapid development of resistance to the existing antifungals, two novel series of 4-phenyl-1,3-thiazole and 2-hydrazinyl-4-phenyl-1,3-thiazole derivatives were synthesized and tested in vitro for their anti-Candida potential. Two compounds (7a and 7e) showed promising inhibitory activity against the pathogenic C. albicans strain, exhibiting substantially lower MIC values (7.81 μg/mL and 3.9 μg/mL, respectively) as compared with the reference drug fluconazole (15.62 μg/mL). Their anti-Candida activity is also supported by molecular docking studies, usin…

Soft X-ray tomography of phenotypic switching and the cellular response to antifungal peptoids in Candida albicans.

2009

The opportunistic pathogen Candida albicans can undergo phenotypic switching between a benign, unicellular phenotype and an invasive, multicellular form that causes candidiasis. Increasingly, strains of Candida are becoming resistant to antifungal drugs, making the treatment of candidiasis difficult, especially in immunocompromised or critically ill patients. Consequently, there is a pressing need to develop new drugs that circumvent fungal drug-resistance mechanisms. In this work we used soft X-ray tomography to image the subcellular changes that occur as a consequence of both phenotypic switching and of treating C. albicans with antifungal peptoids, a class of candidate therapeutics unaf…

The Impact of NFAT Inhibition on Neutrophil Antifungal Defense and Myelopoiesis in Cyclosporine A Treated and NFATc1LysM Mice

2015

Abstract Background and Aims: Immunodeficient patients after allogeneic stem cell transplantation (HSCT) are heavily threatened by opportunistic fungal infections like invasive pulmonary aspergillosis (IPA), partly due to immunosuppressive medication e.g. by calcineurin inhibitors like cyclosporine A (CsA) or tacrolimus. It is well known that the nuclear factor of activated T cells (NFAT) is an important transcription factor downstream of calcineurin in the adaptive immune system especially in T cells. Additionally, there is a growing body of evidence that NFAT also plays a substantial role in innate immune response against invasive fungal diseases by polymorphonuclear neutrophils (PMN), as…

Composition and in vitro antifungal activity of essential oils of Erigeron canadensis and Myrtus communis from France. CHEMISTRY OF NATURAL COMPOUNDS…

2003

Impact of glucuronide interferences on therapeutic drug monitoring of posaconazole by tandem mass spectrometry.

2010

Abstract Background: Posaconazole is a novel antifungal drug for oral application intended especially for therapy of invasive mycoses. Due to variable gastrointestinal absorption, adverse side effects, and suspected drug-drug interactions, therapeutic drug monitoring (TDM) of posaconazole is recommended. Method: A fast ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for quantification of posaconazole with a run-time <3 min was developed and compared to a LC-MS/MS method and HPLC method with fluorescence detection. Results: During evaluation of UPLC-MS/MS, two earlier eluting peaks were observed in the MRM trace of posaconazole. This was only seen in p…

Antifungal Activity of Biocontrol Agents In Vitro and Potential Application to Reduce Mycotoxins (Aflatoxin B1 and Ochratoxin A)

2021

Food bio-preservatives are requested as substituents of chemical pesticides in food. The aim of this study was to carry out a screening of twenty biocontrol agents (BCAs) for their potential fungicidal activity in vitro. Twenty BCAs were tested against ten pathogenic fungi. Some of the cell-free supernatants (CFS) tested showed in vitro antifungal activity versus pathogenic fungi. The highest fungicidal activity was observed in the fermented CFS of Paenibacillus chibensis CECT 375, Bacillus amyloliquefaciens CECT 493, and Pantoea agglomerans CECT 850, which showed a minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values of 125 and 250 g/L, respectively. The…