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https://www.readbyqxmd.com/read/28924162/insights-into-the-functionality-of-endophytic-actinobacteria-with-a-focus-on-their-biosynthetic-potential-and-secondary-metabolites-production
#1
Ajit Kumar Passari, Vineet Kumar Mishra, Garima Singh, Pratibha Singh, Brijesh Kumar, Vijai Kumar Gupta, Rupak Kumar Sharma, Ratul Saikia, Anthonia O' Donovan, Bhim Pratap Singh
Endophytic actinobacteria play an important role in growth promotion and development of host plant by producing enormous quantities of novel bioactive natural products. In the present investigation, 169 endophytic actinobacteria were isolated from endospheric tissues of Rhynchotoechum ellipticum. Based on their antimicrobial potential, 81 strains were identified by 16rRNA gene analysis, which were taxonomically grouped into 15 genera. All identified strains were screened for their plant growth promoting attributes and, for the presence of modular polyketide synthases (PKSI, PKSII and nonribosomal peptide synthetase (NRPS) gene clusters to correlate the biosynthetic genes with their functional properties...
September 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28921992/a-mechanistic-understanding-of-the-synergistic-potential-of-azole-fungicides-in-the-aquatic-invertebrate-gammarus-pulex
#2
Andrea Rösch, Michele Gottardi, Caroline Vignet, Nina Cedergreen, Juliane Hollender
Azole fungicides are known inhibitors of the important enzyme class cytochrome P450 monooxygenases (CYPs), thereby influencing the detoxification of co-occurring substances via biotransformation. This synergism in mixtures containing an azole has mostly been studied by effect measurements, while the underlying mechanism has been less well investigated. In this study, six azole fungicides (cyproconazole, epoxiconazole, ketoconazole, prochloraz, propiconazole and tebuconazole) were selected to investigate their synergistic potential and their CYP inhibition strength in the aquatic invertebrate Gammarus pulex...
September 18, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28919384/the-combination-of-gis-and-biphasic-to-better-predict-in-vivo-dissolution-of-bcs-class-iib-drugs-ketoconazole-and-raloxifene
#3
Yasuhiro Tsume, Naoto Igawa, Adam J Drelich, Gregory E Amidon, Gordon L Amidon
The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the human gastrointestinal (GI) tract. Since the GI environment influences the drug dissolution of BCS class II drugs, the human GI characteristics should be incorporated into the in vitro dissolution system to predict bioperformance of BCS class II drugs. An absorptive compartment may be important in dissolution apparatus for BCS class II drugs, especially for bases (BCS IIb) because of high permeability, precipitation and supersaturation...
September 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28912253/physiologically-based-pharmacokinetic-model-predictions-of-panobinostat-lbh589-as-a-victim-and-perpetrator-of-drug-drug-interactions
#4
Heidi J Einolf, Wen Lin, Christina S Won, Lai Wang, Helen Gu, Dung Yu Chun, Handan He, James B Mangold
Panobinostat (Farydak®) is an orally active hydroxamic acid derived histone deacetylase inhibitor for the treatment of relapsed/refractory multiple myeloma. Based upon recombinant cytochrome P450 (CYP) kinetic analyses in vitro, panobinostat oxidative metabolism in human liver microsomes was found to be primarily mediated by CYP3A4 with lower contributions by CYP2D6 and CYP2C19. Panobinostat was also shown to be an in vitro reversible and time-dependent inhibitor of CYP3A4/5, and a reversible inhibitor of CYP2D6 and CYP2C19...
September 14, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28902012/comparison-of-oral-voriconazole-versus-oral-ketoconazole-as-an-adjunct-to-topical-natamycin-in-severe-fungal-keratitis-a-randomized-controlled-trial
#5
Namrata Sharma, Deepali Singhal, Prafulla K Maharana, Rajesh Sinha, Tushar Agarwal, Ashish D Upadhyay, Thirumurthy Velpandian, Gita Satpathy, Jeewan S Titiyal
PURPOSE: To compare the efficacy of oral voriconazole (VCZ) with oral ketoconazole (KCZ) as an adjunct to topical natamycin in severe fungal keratitis. METHODS: Fifty eyes of 50 patients with proven severe fungal keratitis, (>5 mm size, involving >4 mm central cornea and >50% stromal depth), smear, and/or culture positive were randomized to receive either oral VCZ (n = 25) or oral KCZ (n = 25) 200 mg twice a day. Both groups received topical natamycin along with oral medication...
September 8, 2017: Cornea
https://www.readbyqxmd.com/read/28879796/assessment-of-the-pulmonary-cyp1a1-metabolism-of-mavoglurant-afq056-in-rat
#6
Yildiz Yilmaz, Kenichi Umehara, Gareth Williams, Thomas Faller, Hilmar Schiller, Markus Walles, Stephan Kraehenbuehl, Gian Camenisch, Nenad Manevski
1. AFQ056 phenotyping results indicate that CYP1A1 is responsible for the formation of the oxidative metabolite, M3. In line with the predominant assumption that CYP1A1 is mainly expressed in extrahepatic tissues, only traces of M3 were detected in hepatic systems. The aim of this study was to investigate the pulmonary CYP1A1 mediated metabolism of AFQ056 in rat. 2. Western blot analysis confirmed that CYP1A1 is expressed in rat lung albeit at low levels. M3 formation was clearly observed in recombinant rat CYP1A1, lung microsomes and lung tissue slices and was strongly inhibited by ketoconazole in the incubations...
September 7, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28878412/putative-contact-ketoconazole-shampoo-triggered-pemphigus-foliaceus-in-a-dog
#7
Hyun-Jeong Sung, In-Hwa Yoon, Jung-Hyun Kim
A 10-year-old spayed female cocker spaniel dog was referred for an evaluation of acute-onset generalized pustular cutaneous lesions following application of ketoconazole shampoo. Cytologic and histopathologic examinations of the lesions revealed intra-epidermal pustules with predominantly neutrophils and acantholytic cells. This is the first description of putative contact ketoconazole shampoo-triggered pemphigus foliaceus in a dog.
September 2017: Canadian Veterinary Journal. la Revue Vétérinaire Canadienne
https://www.readbyqxmd.com/read/28857851/antifungal-prevention-of-systemic-candidiasis-in-immunocompetent-icu-adults-systematic-review-and-meta-analysis-of-clinical-trials
#8
Hervé Dupont, Yazine Mahjoub, Taieb Chouaki, Emmanuel Lorne, Elie Zogheib
OBJECTIVES: The aim of this study was to identify the impact of antifungal prevention in critically ill immunocompetent adult patients on mortality and subsequent infection. DATA SOURCES: A systematic review and meta-analysis of randomized controlled trials comparing any antifungal use versus placebo to prevent candidiasis in ICU patients were performed. STUDY SELECTION: Searches were performed on PubMed, Embase, Scopus, main conference proceedings, and ClinicalTrials...
August 28, 2017: Critical Care Medicine
https://www.readbyqxmd.com/read/28851254/quantitative-prediction-of-the-extent-of-drug-drug-interaction-using-a-physiologically-based-pharmacokinetic-model-that-includes-inhibition-of-drug-metabolism-determined-in-cryopreserved-hepatocytes
#9
Shinji Iwasaki, Hideki Hirabayashi, Nobuyuki Amano
1. A physiologically based pharmacokinetic (PBPK) model that includes inhibition constant evaluated in cryopreserved hepatocytes was used to predict drug-drug interactions (DDIs) between orally administered nifedipine, a CYP substrate, and fluconazole or ketoconazole, CYP inhibitors, in rats. 2. The Kp,uu, ratio of unbound inhibitor concentration in liver ([I]liver,u) to that in plasma ([I]sys,u), of fluconazole and ketoconazole was 1.0 and 13.0, indicating that ketoconazole accumulates in liver. The ratios of inhibition constants in rat liver microsomes (Ki,mic,u) to that in rat cryopreserved hepatocytes (Ki,hep,u) for fluconazole and ketoconazole were 1...
September 4, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28835348/synthesis-antimicrobial-activity-structure-activity-relationship-and-cytotoxic-studies-of-a-new-series-of-functionalized-z-3-2-oxo-2-substituted-ethylidene-3-4-dihydro-2h-benzo-b-1-4-oxazin-2-ones
#10
Ritu Sharma, Lalit Yadav, Jaggi Lal, Pradeep K Jaiswal, Manas Mathur, Ajit K Swami, Sandeep Chaudhary
A new series of functionalized (Z)-3-(2-oxo-2-substituted ethylidene)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-ones 23-26, incorporating pharmaceutically privileged substructures such as cyclopropyl, naphthyl, biphenyl and cyclohexylphenyl were synthesized in excellent yields. All the synthesized compounds were screened for their in vitro antibacterial activity against gram-(+)ve and gram-(-)ve bacterial species i.e. S. griseus, S. aureus, B. subtillis and E. coli as well as in vitro antifungal activity against fungal species i...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28834733/development-of-a-phosphorylated-momordica-charantia-protein-system-for-inhibiting-susceptible-dose-dependent-c-albicans-to-available-antimycotics-an-allosteric-regulation-of-protein
#11
Yuanbiao Qiao, Li Song, Chenchen Zhu, Qian Wang, Tianyan Guo, Yanhua Yan, Qingshan Li
A regulatory Momordica charantia protein system was constructed allosterically by in vitro protein phosphorylation, in an attempt to evaluate antimycological pluripotency against dose-dependent susceptibilities in C. albicans. Fungal strain lineages susceptible to ketoconazole, econazole, miconazole, 5-flucytosine, nystatin and amphotericin B were prepared in laboratory, followed by identification via antifungal susceptibility testing. Protein phosphorylation was carried out in reactions with 5'-adenylic, guanidylic, cytidylic and uridylic acids and cyclic adenosine triphosphate, through catalysis of cyclin-dependent kinase 1, protein kinase A and protein kinase C respectively...
August 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28834279/the-cytochrome-p450-enzyme-responsible-for-the-production-of-z-norendoxifen-in-vitro
#12
Dabei Tang, Zhong Chu, Jessica Bo Li Lu, Jinzhong Liu, Qingyuan Zhang
BACKGROUND: Norendoxifen, an active metabolite of tamoxifen, is a potent aromatase inhibitor. Little information is available regarding production of norendoxifen in vitro. Here, we conducted a series of kinetic and inhibition studies in human liver microsomes (HLMs) and expressed P450s to study the metabolic disposition of norendoxifen. METHODS: To validate that norendoxifen was the metabolite of endoxifen, metabolites in HLMs incubates of endoxifen were measured using a HPLC/MS/MS method...
August 17, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28827987/aromatase-inhibitory-activity-of-1-4-naphthoquinone-derivatives-and-qsar-study
#13
Veda Prachayasittikul, Ratchanok Pingaew, Apilak Worachartcheewan, Somkid Sitthimonchai, Chanin Nantasenamat, Supaluk Prachayasittikul, Somsak Ruchirawat, Virapong Prachayasittikul
A series of 2-amino(chloro)-3-chloro-1,4-naphthoquinone derivatives (1-11) were investigated for their aromatase inhibitory activities. 1,4-Naphthoquinones 1 and 4 were found to be the most potent compounds affording IC50 values 5.2 times lower than the reference drug, ketoconazole. A quantitative structure-activity relationship (QSAR) model provided good predictive performance (R(2)CV = 0.9783 and RMSECV = 0.0748) and indicated mass (Mor04m and H8m), electronegativity (Mor08e), van der Waals volume (G1v) and structural information content index (SIC2) descriptors as key descriptors governing the activity...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28826241/a-novel-thermo-sensitive-hydrogel-based-on-poly-n-isopropylacrylamide-hyaluronic-acid-of-ketoconazole-for-ophthalmic-delivery
#14
Minqi Zhu, Jing Wang, Na Li
The aim of this study is to develop thermo-sensitive in situ gelling formulation of KCL based on poly(N-isopropylacrylamide)/hyaluronic acid. The prepared preparations were characterized for in vitro gelation, drug release and antifungal activity. In this study, drug content of prepared gels was found to be in the range of 91-96%. The pH value was in the range of 6.0-7.5. By measuring the gelation temperature of the prepared PN-HA thermogelling solutions, it was 33 °C. In vitro release showed that the release of KCL from in situ gels was moderate without burst effects...
August 21, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28819225/cytochrome-p450-abc-transporter-inhibition-simultaneously-enhances-ivermectin-pharmacokinetics-in-the-mammal-host-and-pharmacodynamics-in-anopheles-gambiae
#15
Carlos J Chaccour, Felix Hammann, Marta Alustiza, Sandra Castejon, Brian B Tarimo, Gloria Abizanda, Ángel Irigoyen Barrio, Helena Martí Soler, Rafael Moncada, José Ignacio Bilbao, Azucena Aldaz, Marta Maia, José Luis Del Pozo
Mass administration of endectocides, drugs that kill blood-feeding arthropods, has been proposed as a complementary strategy to reduce malaria transmission. Ivermectin is one of the leading candidates given its excellent safety profile. Here we provide proof that the effect of ivermectin can be boosted at two different levels by drugs inhibiting the cytochrome or ABC transporter in the mammal host and the target mosquitoes. Using a mini-pig model, we show that drug-mediated cytochrome P450/ABC transporter inhibition results in a 3-fold increase in the time ivermectin remains above mosquito-killing concentrations...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28805726/chemical-identity-of-interaction-of-protein-with-reactive-metabolite-of-diosbulbin-b-in-vitro-and-in-vivo
#16
Kai Wang, Dongju Lin, Xiucai Guo, Wenlin Huang, Ying Peng, Jiang Zheng
Diosbulbin B (DIOB), a hepatotoxic furan-containing compound, is a primary ingredient in Dioscorea bulbifera L., a common herbal medicine. Metabolic activation is required for DIOB-induced liver injury. Protein covalent binding of an electrophilic reactive intermediate of DIOB is considered to be one of the key mechanisms of cytotoxicity. A bromine-based analytical technique was developed to characterize the chemical identity of interaction of protein with reactive intermediate of DIOB. Cysteine (Cys) and lysine (Lys) residues were found to react with the reactive intermediate to form three types of protein modification, including Cys adduction, Schiff's base, and Cys/Lys crosslink...
August 14, 2017: Toxins
https://www.readbyqxmd.com/read/28802958/interaction-of-erythromycin-and-ketoconazole-on-the-neurological-biochemical-and-behavioral-responses-in-crucian-carp
#17
Jianchao Liu, Yuanfei Cai, Guanghua Lu, Xiaoxiang Dan, Donghai Wu, Zhenhua Yan
The presence of pharmaceuticals in the aquatic environment has received great attention due to their potential impacts on public health. The single, as well as the combined toxicities of erythromycin (ERY) and ketoconazole (KCZ) on the bioaccumulation, biochemical and behavioral responses, were examined in crucian carp. This study focused on the uptake of contaminants, acetylcholinesterase (AChE) activity in the brain, swimming and shoaling behavior of fish. After 14days of binary exposure, the addition of KCZ at nominal concentrations of 0...
August 7, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28800141/effects-of-strong-cyp3a-inhibition-and-induction-on-the-pharmacokinetics-of-ixazomib-an-oral-proteasome-inhibitor-results-of-drug-drug-interaction-studies-in-patients-with-advanced-solid-tumors-or-lymphoma-and-a-physiologically-based-pharmacokinetic-analysis
#18
Neeraj Gupta, Michael J Hanley, Karthik Venkatakrishnan, Alberto Bessudo, Drew W Rasco, Sunil Sharma, Bert H O'Neil, Bingxia Wang, Guohui Liu, Alice Ke, Chirag Patel, Karen Rowland Yeo, Cindy Xia, Xiaoquan Zhang, Dixie-Lee Esseltine, John Nemunaitis
At clinically relevant ixazomib concentrations, in vitro studies demonstrated that no specific cytochrome P450 (CYP) enzyme predominantly contributes to ixazomib metabolism. However, at higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms, with the estimated relative contribution being highest for CYP3A at 42%. This multiarm phase 1 study (Clinicaltrials.gov identifier: NCT01454076) investigated the effect of the strong CYP3A inhibitors ketoconazole and clarithromycin and the strong CYP3A inducer rifampin on the pharmacokinetics of ixazomib...
August 11, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28796631/endocrine-disruption-in-human-fetal-testis-explants-by-individual-and-combined-exposures-to-selected-pharmaceuticals-pesticides-and-environmental-pollutants
#19
Pierre Gaudriault, Séverine Mazaud-Guittot, Vincent Lavoué, Isabelle Coiffec, Laurianne Lesné, Nathalie Dejucq-Rainsford, Martin Scholze, Andreas Kortenkamp, Bernard Jégou
BACKGROUND: Numerous chemicals are capable of disrupting androgen production, but the possibility that they might act together to produce effects greater than those of the most effective component in the mixture has not been studied directly in human tissues. Suppression of androgen synthesis in fetal life has been associated with testis maldescent, malformations of the genitalia at birth, and poor semen quality later in life. OBJECTIVES: Our aim was to investigate whether chemicals can act together to disrupt androgen production in human fetal testis explants and to evaluate the importance of mixture effects when characterizing the hazard of individual chemicals...
August 4, 2017: Environmental Health Perspectives
https://www.readbyqxmd.com/read/28776447/analysis-of-imidazoles-and-triazoles-in-biological-samples-after-microextraction-by-packed-sorbent
#20
Cristina Campestre, Marcello Locatelli, Paolo Guglielmi, Elisa De Luca, Giuseppe Bellagamba, Sergio Menta, Gokhan Zengin, Christian Celia, Luisa Di Marzio, Simone Carradori
This paper reports the MEPS-HPLC-DAD method for the simultaneous determination of 12 azole drugs (bifonazole, butoconazole, clotrimazole, econazole, itraconazole, ketoconazole, miconazole, posaconazole, ravuconazole, terconazole, tioconazole and voriconazole) administered to treat different systemic and topical fungal infections, in biological samples. Azole drugs separation was performed in 36 min. The analytical method was validated in the ranges as follows: 0.02-5 μg mL(-1) for ravuconazole; 0.2-5 μg mL(-1) for terconazole; 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
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