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https://www.readbyqxmd.com/read/28727431/pd-catalyzed-iodide-promoted-%C3%AE-arylation-of-ketones-for-the-regioselective-synthesis-of-isocoumarins
#1
Alessandra Casnati, Raimondo Maggi, Giovanni Maestri, Nicola Della Ca', Elena Motti
A variety of isocoumarins have been synthesized directly from 2-halobenzoates and ketones through a palladium-catalyzed α-arylation step followed by an intramolecular cyclization process. The addition of iodide anions to the reaction mixture increased yields and selectivities especially when 2-bromobenzoates were employed. This phosphine-free one-pot synthesis features a high functional group tolerance and gives access to richly decorated isocoumarins. This general methodology was successful in the total synthesis of Xyridin A, an important natural product with antibacterial and antifungal activity...
July 20, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28725901/zinc-binding-sites-in-pra1-a-zincophore-from-candida-albicans
#2
Dorota Łoboda, Magdalena Rowińska-Żyrek
The aim of this work is to understand the interactions of Zn(ii) with Pra1, a zincophore from Candida albicans, one of the most common causes of serious fungal infections in humans. Pra1 is a 299 amino acid protein, secreted from the fungus to specifically bind Zn(ii) and deliver it to a transmembrane zinc transporter, Zrt1. We take the first step towards understanding the bioinorganic chemistry of this process, by pointing out the Zn(ii) binding sites in Pra1 and understanding the thermodynamics of such interactions...
July 20, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28725632/medicinal-importance-pharmacological-activities-and-analytical-aspects-of-hispidulin-a-concise-report
#3
REVIEW
Kanika Patel, Dinesh Kumar Patel
Herbal medicines have been played an important role in the human civilization since very ancient time as a food, cloth, medicine and other aspects. Some of the important drugs in the modern medicine were derived from the natural sources such as aspirin, digitalis, quinine, vincristine, vinblastine etc. Hispidulin (4', 5, 7-trihydroxy-6-methoxyflavone) is a flavones derivative found in plant such as Grindelia argentina, Arrabidaea chica, Saussurea involucrate, Crossostephium chinense, Artemisia and Salvia species...
July 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28725622/authentication-of-piper-betle-l-folium-and-quantification-of-their-antifungal-activity
#4
I Made Agus Gelgel Wirasuta, I Gusti Ayu Made Srinadi, Ida Bagus Gede Dwidasmara, Ni Luh Putu Putri Ardiyanti, I Gusti Ayu Arya Trisnadewi, Ni Luh Putu Vidya Paramita
The TLC profiles of intra- and inter-day precision for Piper betle L. (PBL) folium methanol extract was studied for their peak marker recognition and identification. The Numerical chromatographic parameters (NCPs) of the peak markers, the hierarchical clustering analysis (HCA) and the principal component analysis (PCA) were applied to authenticate the PBL. folium extract from other Piper species folium extract and to ensure the antifungal activity quality of the PBL essential oil. The spotted extract was developed with the mobile phase of toluene: ethyl acetate; 93:7, (v/v)...
July 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/28725545/a-severe-transmissible-majocchi-s-granuloma-in-an-immunocompetent-returned-traveler
#5
James G Gallo, Marion Woods, Rikki M Graham, Amy V Jennison
Severe dermatophyte infection is rare in immunocompetent adults. Recently cases have been described in travelers returning from South East Asia (Luchsinger et al., 2015) [1]. These may be sexually transmitted and can have permanent sequelae. We describe the first reported case of Majocchi's granuloma (MG) in an Australian returned traveler and its subsequent transmission via sexual contact. Both patients were successfully treated with systemic antifungals. MG should be considered in patients with severe rash after travel to South East Asia...
December 2017: Medical Mycology Case Reports
https://www.readbyqxmd.com/read/28725238/a-non-targeted-metabolomics-approach-unravels-the-vocs-associated-with-the-tomato-immune-response-against-pseudomonas-syringae
#6
María Pilar López-Gresa, Purificación Lisón, Laura Campos, Ismael Rodrigo, José Luis Rambla, Antonio Granell, Vicente Conejero, José María Bellés
Volatile organic compounds (VOCs) emitted by plants are secondary metabolites that mediate the plant interaction with pathogens and herbivores. These compounds may perform direct defensive functions, i.e., acting as antioxidant, antibacterial, or antifungal agents, or indirectly by signaling the activation of the plant's defensive responses. Using a non-targeted GC-MS metabolomics approach, we identified the profile of the VOCs associated with the differential immune response of the Rio Grande tomato leaves infected with either virulent or avirulent strains of Pseudomonas syringae DC3000 pv...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28724695/caryolan-1-ol-an-antifungal-volatile-produced-by-streptomyces-spp-inhibits-the-endomembrane-system-of-fungi
#7
Gyeongjun Cho, Junheon Kim, Chung Gyoo Park, Corey Nislow, David M Weller, Youn-Sig Kwak
Streptomyces spp. have the ability to produce a wide variety of secondary metabolites that interact with the environment. This study aimed to discover antifungal volatiles from the genus Streptomyces and to determine the mechanisms of inhibition. Volatiles identified from Streptomyces spp. included three major terpenes, geosmin, caryolan-1-ol and an unknown sesquiterpene. antiSMASH and KEGG predicted that the volatile terpene synthase gene clusters occur in the Streptomyces genome. Growth inhibition was observed when fungi were exposed to the volatiles...
July 2017: Open Biology
https://www.readbyqxmd.com/read/28724328/smart-tetrazole-based-antibacterial-nanoparticles-as-multifunctional-drug-carriers-for-cancer-combination-therapy
#8
Elham Zakerzadeh, Roya Salehi, Mehrdad Mahkam
Due to multidrug resistance of cancer tissues and immune-suppression of cancerous patients during chemotherapy in one hand and the use of tetrazole derivatives in medicine because of its anticancer, antifungal and antiviral properties, on the other, we were encouraged to design novel smart antibacterial nanocomposites-based polymer of tetrazole as dual anticancer drug delivery systems. The structures of nanocomposites characterized by FTIR, (1)H NMR, FESEM-EDX and TGA analyses and antibacterial activity of smart carriers were evaluated by determination of minimum inhibitory concentration (MIC) values against some bacteria and fungi...
July 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28722255/drug-drug-interactions-between-triazole-antifungal-agents-used-to-treat-invasive-aspergillosis-and-immunosuppressants-metabolized-by-cytochrome-p450-3a4
#9
REVIEW
Andreas H Groll, Robert Townsend, Amit Desai, Nkechi Azie, Mark Jones, Marc Engelhardt, Anne-Hortense Schmitt-Hoffman, Robert J Brüggemann
Patients undergoing treatment with immunosuppressant drugs following solid organ or hematopoietic stem cell transplantation are at particular risk for development of serious infections such as invasive aspergillosis. Four triazole antifungal drugs, voriconazole, posaconazole, itraconazole, and isavuconazole, are approved to treat invasive aspergillosis either as first- or second-line therapy. All of these agents are inhibitors of cytochrome P450 3A4, which plays a key role in metabolizing immunosuppressant drugs such as cyclosporine, tacrolimus, and sirolimus...
July 19, 2017: Transplant Infectious Disease: An Official Journal of the Transplantation Society
https://www.readbyqxmd.com/read/28721507/the-diversity-and-antibiotic-properties-of-actinobacteria-associated-with-endemic-deepwater-amphipods-of-lake-baikal
#10
Eugenii S Protasov, Denis V Axenov-Gribanov, Yuriy V Rebets, Irina V Voytsekhovskaya, Bogdan T Tokovenko, Zhanna M Shatilina, Andriy N Luzhetskyy, Maxim A Timofeyev
The emergence of pathogenic bacteria resistant to antibiotics increases the need for discovery of new effective antimicrobials. Unique habitats such as marine deposits, wetlands and caves or unexplored biological communities are promising sources for the isolation of actinobacteria, which are among the major antibiotic producers. The present study aimed at examining cultivated actinobacteria strains associated with endemic Lake Baikal deepwater amphipods and estimating their antibiotic activity. We isolated 42 actinobacterial strains from crustaceans belonging to Ommatogammarus albinus and Ommatogammarus flavus...
July 18, 2017: Antonie Van Leeuwenhoek
https://www.readbyqxmd.com/read/28720735/a-nonredundant-phosphopantetheinyl-transferase-ppta-is-a-novel-antifungal-target-that-directs-secondary-metabolite-siderophore-and-lysine-biosynthesis-in-aspergillus-fumigatus-and-is-critical-for-pathogenicity
#11
Anna Johns, Daniel H Scharf, Fabio Gsaller, Hella Schmidt, Thorsten Heinekamp, Maria Straßburger, Jason D Oliver, Mike Birch, Nicola Beckmann, Katharine S Dobb, Jane Gilsenan, Bharatkumar Rash, Elaine Bignell, Axel A Brakhage, Michael J Bromley
Secondary metabolites are key mediators of virulence for many pathogens. Aspergillus fumigatus produces a vast array of these bioactive molecules, the biosynthesis of which is catalyzed by nonribosomal peptide synthetases (NRPSs) or polyketide synthases (PKSs). Both NRPSs and PKSs harbor carrier domains that are primed for acceptance of secondary metabolic building blocks by a phosphopantetheinyl transferase (P-pant). The A. fumigatus P-pant PptA has been shown to prime the putative NRPS Pes1 in vitro and has an independent role in lysine biosynthesis; however, its role in global secondary metabolism and its impact on virulence has not been described...
July 18, 2017: MBio
https://www.readbyqxmd.com/read/28720726/mitochondrial-cochaperone-mge1-is-involved-in-regulating-susceptibility-to-fluconazole-in-saccharomyces-cerevisiae-and-candida-species
#12
Liesbeth Demuyser, Erwin Swinnen, Alessandro Fiori, Beatriz Herrera-Malaver, Kevin Vestrepen, Patrick Van Dijck
MGE1 encodes a yeast chaperone involved in Fe-S cluster metabolism and protein import into the mitochondria. In this study, we identified MGE1 as a multicopy suppressor of susceptibility to the antifungal fluconazole in the model yeast Saccharomyces cerevisiae We demonstrate that this phenomenon is not exclusively dependent on the integrity of the mitochondrial DNA or on the presence of the drug efflux pump Pdr5. Instead, we show that the increased dosage of Mge1 plays a protective role by retaining increased amounts of ergosterol upon fluconazole treatment...
July 18, 2017: MBio
https://www.readbyqxmd.com/read/28720287/occurrence-toxicity-bioaccessibility-and-mitigation-strategies-of-beauvericin-a-minor-fusarium-mycotoxin
#13
REVIEW
C Luz, F Saladino, F B Luciano, J Mañes, G Meca
Emerging Fusarium mycotoxins include the toxic secondary metabolites fusaproliferin, enniatins, beauvericin (BEA), and moniliform. BEA is produced by some entomo- and phytopathogenic Fusarium species and occurs naturally on corn and corn-based foods and feeds infected by Fusarium spp. BEA has shown various biological activities (antibacterial, antifungal, and insecticidal) and possesses toxic activity, including the induction of apoptosis, increase cytoplasmic calcium concentration and lead to DNA fragmentation in mammalian cell lines...
July 15, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28719861/stabilized-cationic-dipeptide-capped-gold-silver-nanohybrids-towards-enhanced-antibacterial-and-antifungal-efficacy
#14
Manish Bajaj, Satish K Pandey, Tamanna Nain, Surinder K Brar, Prabhjot Singh, Shivakanksha Singh, Nishima Wangoo, Rohit K Sharma
The nanoparticles of silver/gold and cationic peptides have been recognized as potent antimicrobials for long, but their combined effect has so far not been explored. The present study reports the green synthesis of short cationic dipeptide stabilized AuNPs/AgNPs based nanohybrid materials. It thoroughly investigates the effect of conjugation of short cationic peptides on the antimicrobial properties of metallic nanoparticles. In the context of the antimicrobial evaluation of synthesized nanoconjugates, it was observed that peptide capped AgNPs exhibited higher antimicrobial activity as compared to peptide capped AuNPs as well as native peptides and unconjugated metallic nanoparticles...
July 9, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28719812/the-impact-of-zno-and-tio2-on-the-stability-of-clotrimazole-under-uva-irradiation-identification-of-photocatalytic-degradation-products-and-in-vitro-cytotoxicity-assessment
#15
Agata Kryczyk, Paweł Żmudzki, Paulina Koczurkiewicz, Joanna Piotrowska, Elżbieta Pękala, Urszula Hubicka
In order to ensure the safe and effective use of pharmaceutical products especially for topical administration photostability testing is necessary. The current paper presents an in-depth analysis of the stability of one of the most common antifungal agents, namely clotrimazole. Clotrimazole has proven to be stable under UVA irradiation in applied experimental conditions, but the presence of catalysts such as ZnO and TiO2 has contributed significantly to the degradation of this compound. The findings indicate that its photocatalytic degradation reactions followed the pseudo first-order kinetics with rate constant depending on the pH and the used solvent...
June 19, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28718996/production-of-ligninolytic-enzymes-and-some-diffusible-antifungal-compounds-by-white-rot-fungi-using-potato-solid-wastes-as-the-sole-nutrient-source
#16
H Schalchli, E Hormazábal, O Rubilar, G Briceño, A Mutis, G J Zocolo, C Diez
AIMS: The aim of this study was to evaluate the synthesis of ligninolytic enzymes and some diffusible antifungal compounds by white-rot fungi using peels or discarded potato as the sole nutrient source. METHODS AND RESULTS: The strain Trametes hirsuta Ru-513 has been highlighted for its laccase activity (595 ± 33 U l(-1) ), which is able to decolourise 87% of an anthraquinone dye using potato peels as the sole nutritional support. A native polyacrylamide gel of laccase proteins showed the presence of two isoenzymes, corresponding to proteins of 56 and 67 kDa, which were detected by SDS-PAGE...
July 18, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28717672/coccidioidomycosis-a-cause-of-sarcoidosis
#17
Tim Kuberski, Isaac Yourison
BACKGROUND: Sarcoidosis is a granulomatous disease of unknown etiology and coccidioidomycosis is a granulomatous fungal infection endemic to the southwestern United States. Clinical observations on patients with sarcoidosis and coccidioidomycosis simultaneously led to the hypothesis that sarcoidosis can be caused by the fungus Coccidioides. METHODS: Two patients with sarcoidosis and coccidioidomycosis were studied, one prospectively (ie, a patient with sarcoidosis was predicted to develop coccidioidomycosis) and the other retrospectively (ie, a patient with coccidioidomycosis develops sarcoidosis)...
2017: Open Forum Infectious Diseases
https://www.readbyqxmd.com/read/28717232/the-epichlo%C3%A3-festucae-antifungal-protein-has-activity-against-the-plant-pathogen-sclerotinia-homoeocarpa-the-causal-agent-of-dollar-spot-disease
#18
Zipeng Tian, Ruying Wang, Karen V Ambrose, Bruce B Clarke, Faith C Belanger
Epichloë spp. are naturally occurring fungal endophytic symbionts of many cool-season grasses. Infection by the fungal endophytes often confers biotic and abiotic stress tolerance to their hosts. Endophyte-mediated disease resistance is well-established in the fine fescue grass Festuca rubra subsp. rubra (strong creeping red fescue) infected with E. festucae. Resistance to fungal pathogens is not an established effect of endophyte infection of other grass species, and may therefore be unique to the fine fescues...
July 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28715972/defensins-in-viral-infection-and-pathogenesis
#19
Mayumi K Holly, Karina Diaz, Jason G Smith
α, β, and ω defensins are effectors of the innate immune system with potent antibacterial, antiviral, and antifungal activity. Defensins have direct antiviral activity in cell culture, with varied mechanisms for individual viruses, although some common themes have emerged. In addition, defensins have potent immunomodulatory activity that can alter innate and adaptive immune responses to viral infection. In some cases, there is evidence for paradoxical escape from defensin neutralization or enhancement of viral infection...
July 17, 2017: Annual Review of Virology
https://www.readbyqxmd.com/read/28715707/design-synthesis-and-2d-qsar-study-of-novel-pyridine-and-quinolone-hydrazone-derivatives-as-potential-antimicrobial-and-antitubercular-agents
#20
Mohamed A Abdelrahman, Ismail Salama, Mohamed S Gomaa, Mahmoud M Elaasser, Marwa M Abdel-Aziz, Dalia H Soliman
The increased development of highly resistant bacterial strains and tuberculosis, constitute a serious public health threat, highlighting the urgent need of novel antibacterial agents. In this work, two novel series of nicotinic acid hydrazone derivatives (6a-r) and quinolone hydrazide derivatives (12a-l) were synthesized and evaluated as antimicrobial and antitubercular agents. The synthesized compounds were evaluated in vitro for their antibacterial, antifungal and antimycobacterial activities. Compounds 6f and 6p bearing the 3,4,5- (OCH3)3 and 2,5-(OCH3)2 benzylidene motifs were the most potent and as antibacterial, antifungal (MIC: 0...
July 4, 2017: European Journal of Medicinal Chemistry
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