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Anti fungal agents

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https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#1
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27876749/anti-fungal-activity-of-ctn-15-34-the-c-terminal-peptide-fragment-of-crotalicidin-a-rattlesnake-venom-gland-cathelicidin
#2
Carolina Sidrim P Cavalcante, Cláudio B Falcão, Raquel Os Fontenelle, David Andreu, Gandhi Rádis-Baptista
Crotalicidin (Ctn), a 34-residue cathelicidin from a South American rattlesnake, and its fragment (Ctn[15-34]) have shown anti-infective and cytotoxic activities against Gram-negative bacteria and certain tumor lines, respectively. The extent of such effects has been related to physicochemical characteristics such as helicity and hydrophobicity. We now report the anti-fungal activity of Ctn and its fragments (Ctn[1-14]) and (Ctn[15-34]). MIC determination and luminescent cell viability assays were used to evaluate the anti-infective activity of Ctn and its fragments (Ctn[1-14]) and (Ctn[15-34]) as anti-fungal agents against opportunistic yeast and dermatophytes...
November 23, 2016: Journal of Antibiotics
https://www.readbyqxmd.com/read/27874849/systematic-chemical-genetic-and-chemical-chemical-interaction-datasets-for-prediction-of-compound-synergism
#3
Jan Wildenhain, Michaela Spitzer, Sonam Dolma, Nick Jarvik, Rachel White, Marcia Roy, Emma Griffiths, David S Bellows, Gerard D Wright, Mike Tyers
The network structure of biological systems suggests that effective therapeutic intervention may require combinations of agents that act synergistically. However, a dearth of systematic chemical combination datasets have limited the development of predictive algorithms for chemical synergism. Here, we report two large datasets of linked chemical-genetic and chemical-chemical interactions in the budding yeast Saccharomyces cerevisiae. We screened 5,518 unique compounds against 242 diverse yeast gene deletion strains to generate an extended chemical-genetic matrix (CGM) of 492,126 chemical-gene interaction measurements...
November 22, 2016: Scientific Data
https://www.readbyqxmd.com/read/27855875/mechanisms-of-antifungal-and-anti-aflatoxigenic-properties-of-essential-oil-derived-from-turmeric-curcuma-longa-l-on-aspergillus-flavus
#4
Yichen Hu, Jinming Zhang, Weijun Kong, Gang Zhao, Meihua Yang
The antifungal activity and potential mechanisms in vitro as well as anti-aflatoxigenic efficiency in vivo of natural essential oil (EO) derived from turmeric (Curcuma longa L.) against Aspergillus flavus was intensively investigated. Based on the previous chemical characterization of turmeric EO by gas chromatography-mass spectrometry, the substantially antifungal activities of turmeric EO on the mycelial growth, spore germination and aflatoxin production were observed in a dose-dependent manner. Furthermore, these antifungal effects were related to the disruption of fungal cell endomembrane system including the plasma membrane and mitochondria, specifically i...
April 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/27842800/anti-candida-albicans-natural-products-sources-of-new-antifungal-drugs-a-review
#5
REVIEW
A Zida, S Bamba, A Yacouba, R Ouedraogo-Traore, R T Guiguemdé
INTRODUCTION: Candida albicans is the most prevalent fungal pathogen in humans. Due to the development of drug resistance, there is today a need for new antifungal agents for the efficient management of C. albicans infections. Therefore, we reviewed antifungal activity, mechanisms of action, possible synergism with antifungal drugs of all natural substances experimented to be efficient against C. albicans for future. METHODS: An extensive and systematic review of the literature was undertaken and all relevant abstracts and full-text articles analyzed and included in the review...
November 11, 2016: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/27829814/quinoline-based-furanones-and-their-nitrogen-analogues-docking-synthesis-and-biological-evaluation
#6
Sukhbir Lal Khokra, Jyoti, Chetan, Pawan Kaushik, M M Alam, M S Zaman, Aftab Ahmad, Shah Alam Khan, Asif Husain
A small library of twenty-four quinoline based butenolides also known as furanones and their nitrogen analogues was prepared by using two different aroylpropionic acids, viz. 3-(2-naphthoyl)propionic acid (3) and 3-(biphenyl-4-yl)propionic acid (4), as starting materials. The 3-aroylpropionic acids were reacted with different 6-substituted-2-chloroquinolin-3-carbaldehydes (2a-d) to obtain the corresponding furan-2(3H)-ones (5a-h). The purified and characterized furanones were then converted into their corresponding 2(3H)-pyrrolones (6a-h) and N-benzyl-pyrrol-2(3H)-ones (7a-h)...
November 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/27816628/amphotericin-b-copper-ii-complex-shows-improved-therapeutic-index-in-vitro
#7
Barbara Chudzik, Grzegorz Czernel, Arkadiusz Miaskowski, Mariusz Gagoś
The AmB-Cu(II) complex has recently been reported as an antifungal agent with reduced aggregation of AmB in aqueous solutions, increased anti C. albicans activity and lower toxicity against human cells in vitro. In the present work, investigations of the activity of the AmB-Cu (II) complex against fungal pathogens with varying susceptibility, including C. albicans and C. parapsilosis strains and intrinsically resistant A. niger, and cytotoxicity in normal human dermal fibroblasts (NHDF) in vitro were performed...
November 2, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27806050/protein-translation-enzyme-lysyl-trna-synthetase-presents-a-new-target-for-drug-development-against-causative-agents-of-loiasis-and-schistosomiasis
#8
Arvind Sharma, Manmohan Sharma, Manickam Yogavel, Amit Sharma
Helminth parasites are an assemblage of two major phyla of nematodes (also known as roundworms) and platyhelminths (also called flatworms). These parasites are a major human health burden, and infections caused by helminths are considered under neglected tropical diseases (NTDs). These infections are typified by limited clinical treatment options and threat of drug resistance. Aminoacyl-tRNA synthetases (aaRSs) are vital enzymes that decode genetic information and enable protein translation. The specific inhibition of pathogen aaRSs bores well for development of next generation anti-parasitics...
November 2016: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/27801509/anti-rhodotorula-activity-of-mycophenolic-acid-enhanced-in-the-presence-of-polyene-antibiotic-nystatin
#9
Hiroshi Kinoshita, Sarach Wongsuntornpoj, Fumio Ihara, Takuya Nihira
Rhodotorula species are opportunistic pathogens, which cause not only systemic fungemia but other localized infections. Despite the serious side effects such as nephrotoxicity and hypokalemia, amphotericin B (a polyene antifungal) has been commonly prescribed for Rhodotorula infection because Rhodotorula species are resistant against a candin family of antifungal agents. In this study, novel active compounds against Rhodotorula species were screened from the extracts of entomopathogenic fungi based on the synergistic effect of polyene nystatin (NYS), which causes efficient targeting of compounds due to the increased permeability through the fungal cell membrane...
November 1, 2016: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/27789337/aspergillus-flavus-induced-alterations-in-tear-protein-profile-reveal-pathogen-induced-host-response-to-fungal-infection
#10
Jeyalakshmi Kandhavelu, Naveen Luke Demonte, Venkatesh Prajna Namperumalsamy, Lalitha Prajna, Chitra Thangavel, Jeya Maheshwari Jayapal, Dharmalingam Kuppamuthu
: Aspergillus flavus and Fusarium sp. are primary causative agents of keratitis that results in corneal tissue damage leading to vision loss particularly in individuals from the tropical parts of the world. Proteins in the tear film collected from control and keratitis patients was profiled and compared. A total of 1873 proteins from control and 1400 proteins from patient tear were identified by mass spectrometry. While 847 proteins were found to be glycosylated in the patient tear, only 726 were glycosylated in control tear...
October 24, 2016: Journal of Proteomics
https://www.readbyqxmd.com/read/27789295/effect-of-stress-on-heat-shock-protein-levels-immune-response-and-survival-to-fungal-infection-of-mamestra-brassicae-larvae
#11
E H Richards, M P Dani, Y Lu, T Butt, R J Weaver
Although the utilisation of fungal biological control agents to kill insect pests is desirable, it is known that the outcome of infection may be influenced by a number of criteria, including whether or not the target insect is stressed. In the current work, topical treatment of larvae of the lepidopteran pest, Mamestra brassicae, with conidia of Beauveria bassiana, followed by a heat stress (HS; 37°C for 1h) 48h later, resulted in a similar level of larval survival to that occurring for no heat stress (No-HS), fungus-treated larvae...
October 24, 2016: Journal of Insect Physiology
https://www.readbyqxmd.com/read/27786247/galvanic-microcells-as-control-agent-of-indoor-microorganisms
#12
Wojciech Spisak, Andrzej Chlebicki, Mariusz Kaszczyszyn
Today, fungicides are part of the basic tool kit for indoor surface maintenance. However, fungi develop resistance to fungicides, which consequently accelerates the evolution of virulence. Fungicides also carry the risk of adverse effects in humans. Galvanic microcells are a new tool for fungal control on indoor surfaces. We used two types of electrodes, Zn and Cu, with two potential anti-fungal mechanisms: the oligodynamic action of the metal ions themselves and the electricidal effect of the current between the electrodes...
October 27, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27769618/novel-substituted-hydrazono-indolo-2-1-b-quinazoline-6-12-dione-analogues-as-cytostatic-agents-synthesis-crystal-structure-biological-evaluation-and-molecular-docking-studies
#13
Ramu Guda, Sirassu Narsimha, Ramavath Babu, Srujana Muthadi, Harikiran Lingabathula, Rambabu Palabindela, Narsimha Reddy Yellu, Girijesh Kumar, Mamatha Kasula
A series of novel substituted hydrazono indolo[2,1-b]quinazoline-6,12-dione analogues have been synthesized and screened for their in vitro cytotoxic and antimicrobial activities. Among all the target compounds, 3c exhibited the most potent inhibitory activity against three cancer cell lines MCF-7, A549, HeLa with IC50 values 07.14±1.285μM, 09.18±0.968μM and 10.57±0.581μM respectively, while maintaining low toxicity towards non-cancer originated cell line, HEK-293. The detailed studies about molecular interactions with probable target protein indoleamine 2,3-dioxygenase (IDO1) were done by using docking simulations...
October 5, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27766695/invasive-fungal-infections-in-pediatric-patients-treated-with-tumor-necrosis-alpha-tnf-%C3%AE-inhibitors
#14
Athanasios Tragiannidis, Ioannis Kyriakidis, Ilse Zündorf, Andreas H Groll
Macromolecular immunosuppressive monoclonal antibodies and fusion proteins directed against molecules or cells involved in inflammation and immunity represent a recent and important addition to our therapeutic armamentarium. Tumor necrosis alpha (TNFα) is a cytokine involved in systemic inflammation and clinical utilization of its antagonists has revolutionized treatment of juvenile rheumatoid and psoriatic arthritis, ankylosing spondylitis, Crohn's disease, ulcerative colitis, and plaque psoriasis. Clinical utility has also been demonstrated for use against steroid-refractory graft-vs-host disease and other immune-mediated conditions...
October 21, 2016: Mycoses
https://www.readbyqxmd.com/read/27760442/metabolomics-guided-isolation-of-anti-trypanosomal-metabolites-from-the-endophytic-fungus-lasiodiplodia-theobromae
#15
Nurkhalida Kamal, Christina V Viegelmann, Carol J Clements, RuAngelie Edrada-Ebel
Fungal endophytes offer diverse and unique secondary metabolites, making these organisms potential sources of promising drug leads. The application of high-resolution-liquid chromatography mass spectrometry and nuclear magnetic resonance-based metabolomics to fungal endophytes is practical in terms of dereplication studies and the mining of bioactive compounds. In this paper, we report the application of metabolomics in parallel with anti-trypanosomal assays to determine the ideal conditions for the medium-scale fermentation of the endophyte Lasiodiplodia theobromae...
October 19, 2016: Planta Medica
https://www.readbyqxmd.com/read/27760211/biological-role-of-paenilarvins-iturin-like-lipopeptide-secondary-metabolites-produced-by-the-honey-bee-pathogen-paenibacillus-larvae
#16
Gillian Hertlein, Marlene Seiffert, Sebastian Gensel, Eva Garcia-Gonzalez, Julia Ebeling, Ranko Skobalj, Anja Kuthning, Roderich D Süssmuth, Elke Genersch
The Gram-positive bacterium Paenibacillus larvae (P. larvae) is the causative agent of a deadly honey bee brood disease called American Foulbrood (AFB). AFB is a notifiable epizootic in most countries and, hence, P. larvae is of considerable relevance for veterinarians and apiculturists alike. Over the last decade, much progress has been made in the understanding of the (patho)biology of P. larvae. Recently, several non-ribosomally produced peptides (NRP) and peptide/polyketide (NRP/PK) hybrids produced by P...
2016: PloS One
https://www.readbyqxmd.com/read/27737019/an-rnai-based-control-of-fusarium-graminearum-infections-through-spraying-of-long-dsrnas-involves-a-plant-passage-and-is-controlled-by-the-fungal-silencing-machinery
#17
Aline Koch, Dagmar Biedenkopf, Alexandra Furch, Lennart Weber, Oliver Rossbach, Eltayb Abdellatef, Lukas Linicus, Jan Johannsmeier, Lukas Jelonek, Alexander Goesmann, Vinitha Cardoza, John McMillan, Tobias Mentzel, Karl-Heinz Kogel
Meeting the increasing food and energy demands of a growing population will require the development of ground-breaking strategies that promote sustainable plant production. Host-induced gene silencing has shown great potential for controlling pest and diseases in crop plants. However, while delivery of inhibitory noncoding double-stranded (ds)RNA by transgenic expression is a promising concept, it requires the generation of transgenic crop plants which may cause substantial delay for application strategies depending on the transformability and genetic stability of the crop plant species...
October 2016: PLoS Pathogens
https://www.readbyqxmd.com/read/27713026/agents-that-activate-the-high-osmolarity-glycerol-pathway-as-a-means-to-combat-pathogenic-molds
#18
Annegret Wiedemann, Anja Spadinger, Axel Löwe, Allison Seeger, Frank Ebel
Treatment of invasive fungal infections often fails due to the limited number of therapeutic options. In this study, we have analyzed the impact of agents activating the High Osmolarity Glycerol (HOG) pathway on molds that cause infections in humans and livestock. We found that agents like fludioxonil and iprodione, have a clear anti-fungal activity against pathogenic Aspergillus, Lichtheimia, Rhizopus and Scedosporium species. Only A. terreus turned out to be resistant to fludioxonil, even though it is sensitive to iprodione and able to adapt to hyperosmotic conditions...
September 28, 2016: International Journal of Medical Microbiology: IJMM
https://www.readbyqxmd.com/read/27671284/pyocyanin-as-anti-tyrosinase-and-anti-tinea-corporis-a-novel-treatment-study
#19
REVIEW
Nessma A El-Zawawy, Sameh S Ali
OBJECTIVE: The aim of this study was to evaluate the efficiency of pyocyanin pigment as a novel compound active against tyrosinase with its depigmentation efficiency for combating Trichophyton rubrum which could be a major causative agent of tinea corporis. METHODS: Fifty swabs of fungal tinea corporis infections were collected and identified. Five MDRPA isolates were tested for their levels of pyocyanin production. The purified extracted pyocyanin was characterized by UV spectrum and FT-IR analysis...
November 2016: Microbial Pathogenesis
https://www.readbyqxmd.com/read/27666589/antifungal-activity-of-rhamnolipids-against-dimorphic-fungi
#20
Ruyi Sha, Qin Meng
In this paper, rhamnolipids are investigated, for the first time, for their feasibility for inhibiting dimorphic fungi. Rhamnolipids were found to effectively inhibit a dimorphic fungus isolated from tomato plants which was identified as Mucor circinelloides according to characterizations by morphologies as well as 28S rDNA sequences. Rhamnolipids markedly reduced growth of this fungus in both the yeast-like form and the filamentous form. Such an inhibitive effect was similarly obtained with Verticillium dahliae, a representative member of dimorphic fungi, confirming the effectiveness of rhamnolipids in the two growth forms of dimorphic fungi...
September 21, 2016: Journal of General and Applied Microbiology
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