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https://www.readbyqxmd.com/read/28533238/posaconazole-induced-hypertension-and-hypokalemia-in-vivo-11%C3%AE-hydroxysteroid-dehydrogenase-inhibition
#1
George R Thompson, Diana Chang, Rebecca R Wittenberg, Ian McHardy, Alison Semrad
We describe a case of apparent mineralocorticoid excess (AME) secondary to posaconazole and suggest the biochemical mechanism. Clinical and laboratory investigation confirmed 11β-hydroxysteroid dehydrogenase inhibition and withholding therapy led to a resolution of all clinical and laboratory abnormalities. A lower dose of posaconazole was later restarted and avoided recurrence of this syndrome. Additional studies are necessary to determine the frequency of posaconazole induced AME and whether other azole antifungals can be associated with this phenomenon...
May 22, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28532662/molecular-design-of-flotation-collectors-a-recent-progress
#2
REVIEW
Guangyi Liu, Xianglin Yang, Hong Zhong
The nature of froth flotation is to selectively hydrophobize valuable minerals by collector adsorption so that the hydrophobized mineral particles can attach air bubbles. In recent years, the increasing commercial production of refractory complex ores has been urgent to develop special collectors for enhancing flotation separation efficiency of valuable minerals from these ores. Molecular design methods offer an effective way for understanding the structure-property relationship of flotation collectors and developing new ones...
May 10, 2017: Advances in Colloid and Interface Science
https://www.readbyqxmd.com/read/28527633/anthelmintic-activity-of-cytochrome-p450-inhibitors-miconazole-and-clotrimazole-in-vitro-effect-on-the-liver-fluke-opisthorchis-felineus
#3
Viatcheslav A Mordvinov, Alexander G Shilov, Maria Y Pakharukova
Discovery of drugs for the treatment of opisthorchiasis and schistosomiasis is a high priority. The basic metabolic cytochrome P450 (CYP) system in parasitic flatworms contains a single gene. CYP of the liver fluke Opisthorchis felineus, the causative agent of opisthorchiasis, is important for survival of the worm, so may be a promising target for therapeutics against liver fluke infection. The aims of this study were: (i) to analyse in-vitro anthelmintic activity of various CYP inhibitors using standard motility and mortality assays against juvenile and adult O...
May 17, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28515716/antifungal-activity-of-the-biphosphinic-cyclopalladate-c7a-against-candida-albicans-yeast-forms-in-vitro-and-in-vivo
#4
Julian E Muñoz, Diego C P Rossi, Kelly Ishida, Cristina C Spadari, Marcia S C Melhem, Daniel M Garcia, Antonio C F Caires, Carlos P Taborda, Elaine G Rodrigues
Vulvovaginal and invasive candidiasis are frequent conditions in immunosuppressed individuals caused by Candida albicans and non-albicans Candida spp. Fluconazole and Amphotericin B are the main drugs used to fight the infection. However, resistance to fluconazole and other azole antifungal drugs is an important clinical problem that encourages the search for new therapeutic alternatives. In this work, we evaluate the antifungal activity of the biphosphinic cyclopalladate C7a in the in vitro and in vivo model...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28515220/culture-based-methods-and-molecular-tools-for-azole-resistant-aspergillus-fumigatus-detection-in-a-belgian-university-hospital
#5
I Montesinos, M A Argudín, M Hites, F Ahajjam, M Dodémont, C Dagyaran, M Bakkali, I Etienne, F Jacobs, C Knoop, S Patteet, K Lagrou
Azole-resistant Aspergillus fumigatus is an increasing worldwide problem with major clinical implications. Surveillance is warranted to guide clinicians to provide optimal treatment to patients. To investigate azole resistance in clinical Aspergillus isolates in our institution, a Belgian university hospital, we conducted a laboratory-based surveillance between June 2015 and October 2016. Two different approaches were used: a prospective culture-based surveillance using VIPcheck™ on unselected A. fumigatus (n=109 patients, including 19 patients with proven or probable IA), followed by molecular detection of mutations conferring azole resistance and a retrospective detection of azole-resistant A...
May 17, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28515217/an-analytical-and-clinical-evaluation-of-the-pathonostics-aspergenius%C3%A2-assay-for-the-detection-of-invasive-aspergillosis-and-resistance-to-azole-antifungal-drugs-direct-from-plasma-samples
#6
P Lewis White, Raquel B Posso, Rosemary A Barnes
With the proposal to include Aspergillus PCR in the revised EORTC/MSG definitions for fungal disease, commercially manufactured assays may be required to provide standardisation and accessibility. The PathoNostics AsperGenius® assay represents one such test that has the ability to detect a range of Aspergillus species and azole-resistance in A. fumigatus Performance has been validated when testing BAL and serum specimens, but recent evidence suggests that testing plasma may enhance sensitivity over serum. It was decided to evaluate the analytical and clinical performance of the PathoNostics AsperGenius® assay when testing plasma...
May 17, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28513771/species-distribution-and-antifungal-susceptibility-patterns-of-candida-isolates-from-a-public-tertiary-teaching-hospital-in-the-eastern-cape-province-south-africa
#7
P Mnge, B I Okeleye, S D Vasaikar, T Apalata
Candida species are the leading cause of invasive fungal infections, and over the past decade there has been an increased isolation of drug resistant Candida species. This study aimed to identify the species distribution of Candida isolates and to determine their unique antifungal susceptibility and resistance patterns. During a cross-sectional study, 209 Candida isolates (recovered from 206 clinical samples) were collected and their species distribution was determined using ChromAgar Candida. The Vitek-2 system (Biomerieux, South Africa) was used to determine minimum inhibitory concentrations (MICs) to azoles (fluconazole, voriconazole), echinocandins (caspofungin, micafungin), polyenes (amphotericin B) and flucytosine...
May 15, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28513650/photo-induced-copper-catalyzed-c-h-chalcogenation-of-azoles-at-room-temperature
#8
Parthasarathy Gandeepan, Jiayu Mo, Lutz Ackermann
Inexpensive copper catalysts enabled direct C-H chalcogenations at ambient temperature by means of photo-induced catalysis. The expedient copper catalysis set the stage for C-S and C-Se bond formation from readily accessible non-volatile elemental chalcogens. The photo-assisted copper catalysis manifold proved suitable for a wide range of substrates with good functional group tolerance and exhibited high catalytic efficacy even at a reaction temperature of 25 °C.
May 17, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28510690/trichosporonosis-in-pediatric-patients-with-a-hematologic-disorder
#9
Catherine E Foster, Morven S Edwards, Julienne Brackett, Deborah A Schady, C Mary Healy, Carol J Baker
Background.: Trichosporonosis is an emerging and often fatal opportunistic fungal infection in immunocompromised patients, particularly those with hematologic malignancy, but data in children are lacking. Methods.: We report here 3 cases of invasive infection caused by Trichosporon asahii in pediatric patients with acute lymphoblastic leukemia at Texas Children's Hospital in Houston, Texas. We also conducted a literature review and identified 16 additional reports of pediatric patients with invasive T asahii infection and an underlying malignant or nonmalignant hematologic disorder...
May 16, 2017: Journal of the Pediatric Infectious Diseases Society
https://www.readbyqxmd.com/read/28509430/trapping-co2-by-adduct-formation-with-nhc-s-a-theoretical-study
#10
Ibon Alkorta, Maria de la Merced Montero-Campillo, José Elguero
Carbon dioxide can form compounds with nitrogen heterocyclic carbenes (NHC) based on azoles through non-covalent interactions or by covalent bonding. It has been observed a narrow dependence between the preference for one or another type of bonding and the carbene structure, as revealed by a series of physicochemical descriptors. In our survey, a set of NHC based on azole family (three classical, three abnormal and one remote) was shown to bind CO2 at the accurate G4MP2 computational level. In most cases, exothermic reaction profiles towards the covalently bound form were found, reaching stabilization enthalpies up to -77 kJ·mol-1 for the remote carbene case...
May 16, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28507111/real-life-assessment-of-the-safety-and-effectiveness-of-the-new-tablet-and-intravenous-formulations-of-posaconazole-in-the-prophylaxis-of-invasive-fungal-infections-analysis-of-343-courses
#11
Frank P Tverdek, Sang Taek Heo, Samuel L Aitken, Bruno Granwehr, Dimitrios P Kontoyiannis
BACKGROUND: Posaconazole is the preferred mold-active azole for prophylaxis against invasive fungal infection (IFI) in patients with hematologic malignancy (HM). Delayed release tablet and intravenous formulations of posaconazole have recently become available, but clinical data are limited. We sought to examine the real-world pharmacokinetics and prophylactic effectiveness of the new formulations of posaconazole given as prophylaxis in patients with HM. METHODS: A retrospective cohort of all consecutive adult inpatients with HM who received ≥3 days of posaconazole as tablet or intravenous from 12/1/2013-12/31/2015 for primary IFI prophylaxis at MD Anderson Cancer center...
May 15, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28507109/erg11-gene-mutations-and-mdr1-up-regulation-confer-pan-azole-resistance-in-candida-tropicalis-causing-disseminated-candidiasis-while-on-posaconazole-prophylaxis-in-an-acute-lymphoblastic-leukemia-patient
#12
Liangshun You, Wenbin Qian, Qing Yang, Liping Mao, Li Zhu, Xianbo Huang, Jie Jin, Haitao Meng
In this study, we presented a rare case of fatal breakthrough Candida tropicalis in a patient with acute lymphoblastic leukemia (ALL) while on posaconazole prophylaxis. And then we explored the mechanisms underlying azole resistance by focusing on enhanced efflux pumps and changes in the azole target enzyme Erg11p, which was encoded by the ERG11 gene. Our study demonstrates that Y132C substitution of Erg11p combined with MDR1 overexpression may be the pan-azole-resistance mechanisms in Candida tropicalis.
May 15, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28504057/molecular-dynamic-modeling-of-cyp51b-in-complex-with-azole-inhibitors
#13
Pan Gao, Yinglu Cui, Rongling Wu
Cytochrome P450 14α-sterol demethylase (CYP51), the key enzyme in sterol biosynthesis pathway, is an important target protein of cholesterol-lowering agents, antifungal drugs and herbicides. CYP51B enzyme is one of the CYP51 family members. In the present study, we have chosen four representative inhibitors of CYP51B: diniconazole(Din), fluconazole(Flu), tebuconazole(Teb), voriconazole(Vor) and launched to investigate the binding features of CYP51B-inhibitor and gating characteristics via molecular docking and molecular dynamics(MD) simulations...
May 13, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28501465/candiduria-evidence-based-approach-to-management-are-we-there-yet
#14
REVIEW
W A Alfouzan, R Dhar
Candiduria is considered one of the most controversial issues in patient management. Neither the diagnosis nor the optimal treatment options are standardized. This is further complicated by lack of defined laboratory criteria for diagnosis as most of the studies were set for bacterial rather than fungal urinary tract infection (UTI). Furthermore, since Candida species is a known commensal of the genitourinary tract its presence in the urine sample adds ambiguity to making a definitive diagnosis of candidal UTI...
May 10, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28497646/azole-resistant-aspergillus-fumigatus-in-sawmills-of-eastern-france
#15
Audrey Jeanvoine, Steffi Rocchi, Gabriel Reboux, Nadia Crini, Grégorio Crini, Laurence Millon
AIMS: Emergence of azole-resistant Aspergillus fumigatus complicates management of Aspergillus diseases.Currently, selection pressure caused by azole fungicide use in farming is strongly suspected of creating resistance. As sawmills also use azole fungicides, we investigated the presence of azole-resistant strains in this environment and studied the relationship between azole fungicide use and development of resistance. METHODS: Air (n = 200) and substrate (n = 600) samples were taken in 20 sawmills...
May 12, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28497389/elucidating-and-engineering-thiopeptide-biosynthesis
#16
REVIEW
Philip R Bennallack, Joel S Griffitts
Initially discovered in the mid-twentieth century, thiopeptides constitute a diverse family of bacterially produced natural products exhibiting a remarkable array of biological properties. Only in the last several years have the details of thiopeptide biosynthesis been uncovered by a combination of genomic, genetic, and biochemical approaches. Thiopeptides are now known to be ribosomally synthesized and subsequently densely modified to carry azol(in)es, dehydro amino acids, and various other pathway-specific decorations...
June 2017: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28496146/the-antifungal-pipeline-a-reality-check
#17
REVIEW
John R Perfect
Invasive fungal infections continue to appear in record numbers as the immunocompromised population of the world increases, owing partially to the increased number of individuals who are infected with HIV and partially to the successful treatment of serious underlying diseases. The effectiveness of current antifungal therapies - polyenes, flucytosine, azoles and echinocandins (as monotherapies or in combinations for prophylaxis, or as empiric, pre-emptive or specific therapies) - in the management of these infections has plateaued...
May 12, 2017: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/28494138/rational-design-and-synthesis-of-1-arylideneamino-4-aryl-1h-imidazole-2-amine-derivatives-as-antiplatelet-agents
#18
Salimeh Amidi, Marjan Esfahanizadeh, Kimia Tabib, Zohreh Soleimani, Farzad Kobarfard
Based on the previous studies indicating the pharmacophoric role of hydrazone group and azole rings for antiplatelet aggregation activity, a few series of compounds with both hydrazone and azole (imidazole) ring in their structures were synthesized and their platelet aggregation inhibitory effect was evaluated. Two compounds among the 1-(arylideneamino)-4-aryl-1H-imidazole-2-amine derivatives compound 4a and 4p showed IC50 values comparable to that of aspirin against collagen as platelet aggregation inducer...
May 11, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28493006/activity-of-combined-antifungal-agents-against-multidrug-resistant-candida-glabrata-strains
#19
Laura Bedin Denardi, Jéssica Tairine Keller, Vanessa Oliveira, Débora Alves Nunes Mario, Janio Morais Santurio, Sydney Hartz Alves
In this study, we evaluated the in vitro activity of echinocandins, azoles, and amphotericin B alone and in combination against echinocandin/azole-sensitive and echinocandin/azole-resistant Candida glabrata isolates. Susceptibility tests were performed using the broth microdilution method in accordance with the Clinical and Laboratory Standards Institute document M27-A3. The checkerboard method was used to evaluate the fractional inhibitory concentration index of the interactions. Cross-resistance was observed among echinocandins; 15% of the isolates resistant to caspofungin were also resistant to anidulafungin and micafungin...
May 10, 2017: Mycopathologia
https://www.readbyqxmd.com/read/28485428/exploring-micropollutant-biotransformation-in-three-freshwater-phytoplankton-species
#20
Michael A Stravs, Francesco Pomati, Juliane Hollender
Phytoplankton constitute an important component of surface water ecosystems; however little is known about their contribution to biotransformation of organic micropollutants. To elucidate biotransformation processes, batch experiments with two cyanobacterial species (Microcystis aeruginosa and Synechococcus sp.) and one green algal species (Chlamydomonas reinhardtii) were conducted. Twenty-four micropollutants were studied, including 15 fungicides and 9 pharmaceuticals. Online solid phase extraction (SPE) coupled with liquid chromatography (LC)-high resolution tandem mass spectrometry (HRMS/MS) was used together with suspect and nontarget screening to identify transformation products (TPs)...
May 9, 2017: Environmental Science. Processes & Impacts
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