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https://www.readbyqxmd.com/read/28107620/chemical-interaction-of-protein-cysteine-residues-with-reactive-metabolites-of-methyleugenol
#1
Yukun Feng, Hui Wang, Qian Wang, Wenlin Huang, Ying Peng, Jiang Zheng
Methyleugenol (ME), an alkenylbenzene compound, is a natural ingredient of several herbs and is used as flavoring agent in foodstuffs and fragrance in cosmetics. The hepatotoxicity, cytotoxicity, and carcinogenesis of ME have been well documented, and metabolic activation has been suggested to involve in ME-induced toxicities. The objective of this study was to identify chemical identity of interactions of protein with reactive metabolites of ME. Modification of cysteine residues of protein was observed in microsomal incubations and mice after exposure to ME...
January 20, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28092844/enhanced-effect-in-combination-of-curcumin-and-ketoconazole-loaded-methoxy-poly-ethylene-glycol-poly-%C3%AE%C2%B5-caprolactone-micelles
#2
Fangfang Teng, Peizong Deng, Zhimei Song, Feilong Zhou, Runliang Feng
In order to enhance water-solubility and realize controlled release while keeping synergistic effects of ketoconazole and curcumin, drug-loaded methoxy poly (ethylene glycol)-b-poly (ε-caprolactone) micelles were prepared through thin membrane hydration method. Transmission electric microscopy and dynamitic light scattering characterization revealed the formation of ketoconazole- and curcumin-loaded micelles with an average size of 44.70nm and 39.56nm, respectively. The drug-loaded micelles endowed the two drugs' slow controlled release with water-solubility enhanced to 85 and 82000 folds higher than the corresponding raw drugs, respectively...
January 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28079539/preoperative-ketoconazole-therapy-for-primary-bilateral-adrenocorticotropic-hormone-independent-macronodular-adrenal-hyperplasia-syndrome
#3
Rukma Parthvi, Sunil Mehra
No abstract text is available yet for this article.
January 5, 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/28070663/the-pygidial-gland-secretion-of-the-forest-caterpillar-hunter-calosoma-calosoma-sycophanta-the-antimicrobial-properties-against-human-pathogens
#4
REVIEW
Marija Nenadić, Marina Soković, Jasmina Glamočlija, Ana Ćirić, Vesna Perić-Mataruga, Larisa Ilijin, Vele Tešević, Marina Todosijević, Ljubodrag Vujisić, Nikola Vesović, Srećko Ćurčić
Recently, various insect secretions have been tested as possible antimicrobial agents. In beetles, these secretions are essentially products of various exocrine glands, of which particular emphasis is on pygidial glands that are common for the suborder Adephaga. The antimicrobial potential of the pygidial gland secretion isolated from the adults of Calosoma sycophanta against human pathogens has been tested and compared with the potential of other carabid species, particularly within the tribe Carabini. The antimicrobial assay includes a microdilution method which was applied in order to determine the minimal inhibitory, minimal fungicidal and minimal bactericidal concentrations...
February 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28057172/substrate-specificity-of-human-cytochrome-p450-cyp-2c-subfamily-and-effect-of-azole-antifungal-agents-on-cyp2c8
#5
Toshiro Niwa, Yurie Imagawa
PURPOSE: The metabolic activities of aminopyrine N-demethylation and tolbutamide methylhydroxylation by the human hepatic cytochrome P450 (P450 or CYP) 2C subfamily were compared and the effects of azole antifungal agent on the drug-metabolizing activity of CYP2C8 were investigated. METHODS: Aminopyrine N-demethylation and tolbutamide methylhydroxylation by CYP2C8, CYP2C9, and CYP2C19 were determined by the previous reported methods. The effects of five azole antifungal agents, fluconazole, itraconazole, ketoconazole, miconazole, and voriconazole, on the aminopyrine N-demethylation activity by CYP2C8 were investigated...
October 2016: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28052338/quantitative-prediction-of-the-effect-of-cyp3a-inhibitors-and-inducers-on-venetoclax-pharmacokinetics-using-a-physiologically-based-pharmacokinetic-model
#6
Kevin J Freise, Mohamad Shebley, Ahmed Hamed Salem
The objectives of the analysis were to develop and verify a venetoclax physiologically based pharmacokinetic (PBPK) model to predict the effects of cytochrome P450 3A (CYP3A) inhibitors and inducers on the PK of venetoclax and inform dosing recommendations. A minimal PBPK model was developed based on prior in vitro and in vivo clinical data using a "middle-out" approach. The PBPK model was independently verified against clinical studies of the strong CYP3A inhibitor ketoconazole, the strong CYP3A inducer, multiple-dose rifampin, and the steady-state venetoclax PK in chronic lymphocytic leukemia (CLL) subjects by comparing predicted to observed ratios of the venetoclax maximum concentration (Cmax R) and area under the curve from time 0 to infinity (AUC∞ R) from these studies...
January 4, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28028453/identification-and-characterization-of-daldinia-eschscholtzii-isolated-from-skin-scrapings-nails-and-blood
#7
Kee Peng Ng, Chai Ling Chan, Su Mei Yew, Siok Koon Yeo, Yue Fen Toh, Hong Keat Looi, Shiang Ling Na, Kok Wei Lee, Wai-Yan Yee, Chee Sian Kuan
BACKGROUND: Daldinia eschscholtzii is a filamentous wood-inhabiting endophyte commonly found in woody plants. Here, we report the identification and characterization of nine D. eschscholtzii isolates from skin scrapings, nail clippings, and blood. METHODS: The nine isolates were identified based on colony morphology, light microscopy, and internal transcribed spacer (ITS)-based phylogeny. In vitro antifungal susceptibility of the fungal isolates was evaluated by the Etest to determine the minimum inhibitory concentration (MIC)...
2016: PeerJ
https://www.readbyqxmd.com/read/28018316/leveraging-the-attributes-of-mucor-hiemalis-derived-silver-nanoparticles-for-a-synergistic-broad-spectrum-antimicrobial-platform
#8
Nafe Aziz, Rishikesh Pandey, Ishan Barman, Ram Prasad
Driven by the need to engineer robust surface coatings for medical devices to prevent infection and sepsis, incorporation of nanoparticles has surfaced as a promising avenue to enhance non-fouling efficacy. Microbial synthesis of such nanoscale metallic structures is of substantive interest as this can offer an eco-friendly, cost-effective, and sustainable route for further development. Here we present a Mucor hiemalis-derived fungal route for synthesis of silver nanoparticles, which display significant antimicrobial properties when tested against six pathological bacterial strains (Klebsiella pneumoniae, Pseudomonas brassicacearum, Aeromonas hydrophila, Escherichia coli, Bacillus cereus, and Staphylococcus aureus) and three pathological fungal strains (Candida albicans, Fusarium oxysporum, and Aspergillus flavus)...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28017860/in-vitro-antileishmanial-activity-of-novel-azoles-3-imidazolylflavanones-against-promastigote-and-amastigote-stages-of-leishmania-major
#9
Azar Shokri, Saeed Emami, Mahdi Fakhar, Saeed Hosseini Teshnizi, Masoud Keighobadi
Leishmaniasis is a protozoan infectious disease widely distributed all around the world. First line drugs including antimoniales are insufficient due to resistance in endemic areas and high toxicity. Azole antifungals like ketoconazole (KCZ) are also used as antileishmanial agents for several decades. In the present study, we evaluated in vitro antileishmanial effects of new azole antifungals namely 3-imidazolylflavanones (IFs) and their oximes (IFOs) against Leishmania major (L. major) parasites. The obtained results showed remarkable effect of our compounds on promastigote and amastigote stages of L...
December 23, 2016: Acta Tropica
https://www.readbyqxmd.com/read/28011125/prediction-of-ketoconazole-absorption-using-an-updated-in-vitro-transfer-model-coupled-to-physiologically-based-pharmacokinetic-modelling
#10
Aaron Ruff, Tom Fiolka, Edmund S Kostewicz
The aim of this study was to optimize the in vitro transfer model and to increase its biorelevance to more accurately mimic the in vivo supersaturation and precipitation behaviour of weak basic drugs. Therefore, disintegration of the formulation, volumes of the stomach and intestinal compartments, transfer rate, bile salt concentration, pH range and paddle speed were varied over a physiological relevant range. The supersaturation and precipitation data from these experiments for Ketoconazole (KTZ) were coupled to physiologically based pharmacokinetic (PBPK) model using Stella® software, which also incorporated the disposition kinetics of KTZ taken from the literature, in order to simulate the oral absorption and plasma profile in humans...
December 21, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28004396/the-absorption-kinetics-of-ketoconazole-plays-a-major-role-in-explaining-the-reported-variability-in-the-level-of-interaction-with-midazolam-exploring-the-interplay-between-formulation-and-inhibition-of-gut-wall-and-liver-metabolism-by-using-different-doses
#11
Bo Liu, H Kim Crewe, Mahmut Ozdemir, Karen Rowland Yeo, Geoffrey Tucker, Amin Rostami-Hodjegan
The impact of different single oral doses of ketoconazole (KTZ) (100, 200 and 400 mg) and of staggering its dosage (400 mg at -12, -2, 0, 2 and 4 h), with respect to the administration of a single 5 mg oral dose of midazolam (MDZ) on the extent of inhibition of the metabolism of the latter, was evaluated in healthy subjects in two separate studies. Escalation of KTZ dosage resulted in 2.3- (1.9), 2.7- (1.7) and 4.2- (2.5) fold increases in the mean AUC(0,12 h) (and Cmax ) values of MDZ. Dose-staggering was associated with 3...
December 21, 2016: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28004371/modulation-of-erythromycin-induced-biochemical-responses-in-crucian-carp-by-ketoconazole
#12
Jianchao Liu, Guanghua Lu, Yuanfei Cai, Donghai Wu, Zhenhua Yan, Yonghua Wang
The individual and combined biochemical responses of erythromycin and ketoconazole have been examined in an organism representative of the aquatic environment, crucian carp (Carassius auratus). The possible interactions between erythromycin and ketoconazole were investigated on the bioaccumulation and the expression of biotransformation enzymes 7-ethoxyresorufin-O-deethylase (EROD) and glutathione S-transferase (GST), and an antioxidant defense enzyme superoxide dismutase (SOD) in fish tissues. After 14 days of combined exposure (erythromycin + ketoconazole), the addition of ketoconazole at nominal concentrations of 0...
December 21, 2016: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/27994139/triazoles-inhibit-cholesterol-export-from-lysosomes-by-binding-to-npc1
#13
Michael N Trinh, Feiran Lu, Xiaochun Li, Akash Das, Qiren Liang, Jef K De Brabander, Michael S Brown, Joseph L Goldstein
Niemann-Pick C1 (NPC1), a membrane protein of lysosomes, is required for the export of cholesterol derived from receptor-mediated endocytosis of LDL. Lysosomal cholesterol export is reportedly inhibited by itraconazole, a triazole that is used as an antifungal drug [Xu et al. (2010) Proc Natl Acad Sci USA 107:4764-4769]. Here we show that posaconazole, another triazole, also blocks cholesterol export from lysosomes. We prepared P-X, a photoactivatable cross-linking derivative of posaconazole. P-X cross-linked to NPC1 when added to intact cells...
January 3, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27989145/cysteine-based-protein-adduction-by-epoxide-derived-metabolite-s-of-benzbromarone
#14
Hui Wang, Yukun Feng, Qian Wang, Xiucai Guo, Wenlin Huang, Ying Peng, Jiang Zheng
Benzbromarone (BBR) is a therapeutically useful uricosuric agent but can also cause acute liver injury. The hepatotoxicity of BBR is suggested to be associated with its metabolic activation. Our recent metabolic study demonstrated that BBR was metabolized to epoxide intermediate(s) by cytochrome P450 3A, and the intermediate(s) was reactive to N-acetylcysteine. The objectives of the present study were to determine the chemical identity of the interaction of protein with the epoxide intermediate(s) of BBR and to define the association of the protein modification with hepatotoxicity induced by BBR...
December 19, 2016: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/27976369/clomiphene-and-other-antioestrogens-for-ovulation-induction-in-polycystic-ovarian-syndrome
#15
REVIEW
Julie Brown, Cindy Farquhar
BACKGROUND: Subfertility due to anovulation is a common problem in women. First-line oral treatment is with antioestrogens such as clomiphene citrate, but resistance may be apparent with clomiphene. Alternative and adjunctive treatments have been used including tamoxifen, dexamethasone, and bromocriptine. The effectiveness of these is to be determined. OBJECTIVES: To determine the relative effectiveness of antioestrogen agents including clomiphene alone or in combination with other medical therapies in women with subfertility associated with anovulation, possibly caused by polycystic ovarian syndrome...
December 15, 2016: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/27972191/the-cost-effectiveness-of-ketoconazole-versus-metyrapone-for-the-treatment-of-cushing-s-syndrome-in-a-swedish-setting
#16
Å Björstad, R Schmid, B Roser
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27966483/quaternary-ammonium-salt-n-dodecyloxycarboxymethyl-n-n-n-trimethyl-ammonium-chloride-induced-alterations-in-saccharomyces-cerevisiae-physiology
#17
Ewa Oblak, Agata Piecuch, Ewa Maciaszczyk-Dziubinska, Donata Wawrzycka
We investigated the influence of the quaternary ammonium salt (QAS) called IM (N-(dodecyloxycarboxymethyl)- N,N,N-trimethyl ammonium chloride) on yeast cells of the parental strain and the IM-resistant mutant (EO25 IMR) growth. The phenotype of this mutant was pleiotropic. The IMR mutant exhibited resistance to ethanol, osmotic shock and oxidative stress, as well as increased sensitivity to UV. Moreover, it was noted that mutant EO25 appears to have an increased resistance to clotrimazole, ketoconazole, fluconazole, nystatin and cycloheximide...
December 2016: Journal of Biosciences
https://www.readbyqxmd.com/read/27956429/in-vitro-antifungal-susceptibility-profile-of-12-antifungal-drugs-against-55-trichophyton-schoenleinii-isolated-from-tinea-capitis-favosa-in-iran-turkey-and-china
#18
Shuwen Deng, Saham Ansari, Macit Ilkit, Haleh Rafati, Mohammad T Hedayati, Mojtaba Taghizadeh-Armaki, Ayatollah Nasrollahi-Omran, Ali Tolooe, Ping Zhan, Wanqing Liao, Henrich A van der Lee, Paul E Verweij, Seyedmojtaba Seyedmousavi
Trichophyton schoenleinii is an anthropophilic dermatophyte mainly causing tinea favosa of the scalp in certain regions of the world, especially Africa and Asia. We investigated the in vitro susceptibilities of 55 T. schoenleinii collected over the last thirty years from Iran, Turkey and China against 12 antifungals using the CLSI broth-microdilution method. Our results revealed that terbinafine and ketoconazole were the most potent antifungal agents among those tested, independent of the geographical regions isolated...
12, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27943222/clinical-pharmacokinetics-and-pharmacodynamics-of-cediranib
#19
REVIEW
Weifeng Tang, Alex McCormick, Jianguo Li, Eric Masson
Cediranib potently and selectively inhibits all three vascular endothelial growth factor receptors (VEGFR-1, -2 and -3), and clinical studies have shown that it is effective in patients with ovarian cancer at a dose of 20 mg/day. Cediranib is absorbed moderately slowly; a high-fat meal reduced the cediranib area under the plasma concentration-time curve (AUC) by 24% and maximum plasma concentration (C max) by 33%. Cediranib binds to serum albumin and α1-acid glycoprotein; protein binding in human plasma is approximately 95%...
December 9, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27939799/the-consequence-of-regional-gradients-of-p-gp-and-cyp3a4-for-drug-drug-interactions-by-p-gp-inhibitors-and-the-p-gp-cyp3a4-interplay-in-the-human-intestine-ex-vivo
#20
Ming Li, Inge A M de Graaf, Evita van de Steeg, Marina H de Jager, Geny M M Groothuis
Intestinal P-gp and CYP3A4 work coordinately to reduce the intracellular concentration of drugs, and drug-drug interactions (DDIs) based on this interplay are of clinical importance and require pre-clinical investigation. Using precision-cut intestinal slices (PCIS) of human jejunum, ileum and colon, we investigated the P-gp/CYP3A4 interplay and related DDIs with P-gp inhibitors at the different regions of the human intestine with quinidine (Qi), dual substrate of P-gp and CYP3A4, as probe. All the P-gp inhibitors increased the intracellular concentrations of Qi by 2...
December 7, 2016: Toxicology in Vitro: An International Journal Published in Association with BIBRA
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