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https://www.readbyqxmd.com/read/27932461/structural-characterization-and-ligand-inhibitor-identification-provide-functional-insights-into-the-mycobacterium-tuberculosis-cytochrome-p450-cyp126a1
#1
Jude T Chenge, Duyet Van Le, Shalini Swami, Kirsty J McLean, Madeline E Kavanagh, Anthony G Coyne, Stephen E J Rigby, Myles R Cheesman, Hazel M Girvan, Colin W Levy, Bernd Rupp, Jens P von Kries, Chris Abell, David Leys, Andrew W Munro
The Mycobacterium tuberculosis (Mtb) H37Rv genome encodes 20 cytochromes P450, including P450s crucial to infection and bacterial viability. Many Mtb P450s remain uncharacterized, suggesting their further analysis may provide new insights into Mtb metabolic processes and new targets for drug discovery. CYP126A1 is representative of a P450 family widely distributed in mycobacteria and other bacteria. Here we explore the biochemical and structural properties of CYP126A1, including its interactions with new chemical ligands...
December 8, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27928841/fusarium-species-causing-eumycetoma-report-of-two-cases-and-comprehensive-review-of-the-literature
#2
Abdullah M S Al-Hatmi, Alexandro Bonifaz, Andrés Tirado-Sánchez, Jacques F Meis, G Sybren de Hoog, Sarah A Ahmed
Recently, mycetoma was added to the World Health Organization's list of neglected tropical disease priorities. Fusarium as a genus has been reported to cause eumycetoma, but little is known about the species involved in this infection and their identification. In this study, molecular tools were applied to identify Fusarium agents from human eumycetoma cases. The partial translation elongation factor 1-alpha (TEF-1α) gene was used as diagnostic parameter. Two additional cases of eumycetoma, due to F. keratoplasticum and F...
December 7, 2016: Mycoses
https://www.readbyqxmd.com/read/27894193/currently-used-and-investigational-drugs-for-cushing%C3%A2-s-disease
#3
Denis Ciato, Aizhar G Mumbach, Marcelo Paez-Pereda, Günter K Stalla
Cushing's disease (CD) is caused by a corticotroph adenoma of the pituitary gland that secretes excess adrenocorticotropic hormone (ACTH) causing increased morbidity and mortality. Surgery is the treatment of choice, but is not always successful. Alternatives include radiotherapy, adrenal surgery, and pharmaceutical therapy. The latter is increasingly gaining momentum due to the recent development of compounds that reduce hypercortisolaemia or its symptoms, acting through different mechanisms. Areas covered: In this article, the authors provide a complete overview of the treatment options for Cushing´s disease, including adrenal-directed, tumor-targeted, and peripheral therapies that are currently used or in development, and discuss their potential advantages and limitations...
November 29, 2016: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27888010/indole-3-acetic-acid-diol-based-ph-sensitive-biological-macromolecule-for-antibacterial-antifungal-and-antioxidant-applications
#4
Chitra G, Franklin D S, Sudarsan S, Sakthivel M, Guhanathan S
Indole-3-acetic acid (IAA)/diol based pH-sensitive biopolymeric hydrogels with tunable biological properties (cytotoxicity, anti-oxidant and anti-fungal) have been synthesized via condensation polymerization. The present study focused on the synthesis of heterocyclic hydrogel using citric acid (CA), indole-3-acetic acid (IAA) and diethylene glycol (DEG) by condensation polymerization. The hydrogels revealed a pH-sensitive swelling behaviour, with increased swelling in acidic media, then turns to decreased the swelling in the basic media...
November 22, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27885419/ketoconazole-inhibits-malassezia-furfur-morphogenesis-in-vitro-under-filamentation-optimized-conditions
#5
Sirida Youngchim, Joshua D Nosanchuk, Siriporn Chongkae, Nongnuch Vanittanokom
Malassezia furfur, a constituent of the normal human skin flora, is an etiological agent of pityriasis versicolor, which represents one of the most common human skin diseases. Under certain conditions, both exogenous and endogenous, the fungus can transition from a yeast form to a pathogenic mycelial form. To develop a standardized medium for reproducible production of the mycelial form of M. furfur to develop and optimize susceptibility testing for this pathogen, we examined and characterized variables, including kojic acid and glycine concentration, agar percentage, and pH, to generate a chemically defined minimal medium on which specific inoculums of M...
November 24, 2016: Archives of Dermatological Research
https://www.readbyqxmd.com/read/27882460/development-of-a-specific-substrate-inhibitor-panel-liver-on-a-chip-for-evaluation-of-cytochrome-p450-activity
#6
A A Zakhariants, O A Burmistrova, M Y Shkurnikov, A A Poloznikov, D A Sakharov
We developed a cytochrome P450 substrate-inhibitor panel for preclinical in vitro evaluation of drugs in a 3D histotypical microfluidic cell model of human liver (liver-on-a-chip technology). The concentrations of substrates and inhibitors were optimized to ensure reliable detection of the principal metabolites by HPLC-mass-spectroscopy. The selected specific substrate-inhibitor pairs, namely bupropion/2-phenyl-2-(1-piperidinyl)propane) for evaluation of CYP2B6B activity, tolbutamide/sulfaphenazole for CYP2C9, omeprazole/(+)-N-benzylnirvanol for CYP2C19, and testosterone/ketoconazole for CYP3A4, enable reliable evaluation of the drug metabolism pathway...
November 23, 2016: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/27879678/new-thiazolyl-triazole-schiff-bases-synthesis-and-evaluation-of-the-anti-candida-potential
#7
Anca Stana, Alexandra Enache, Dan Cristian Vodnar, Cristina Nastasă, Daniela Benedec, Ioana Ionuț, Cezar Login, Gabriel Marc, Ovidiu Oniga, Brîndușa Tiperciuc
In the context of the dangerous phenomenon of fungal resistance to the available therapies, we present here the chemical synthesis of a new series of thiazolyl-triazole Schiff bases B1-B15, which were in vitro assessed for their anti-Candida potential. Compound B10 was found to be more potent against Candida spp. when compared with the reference drugs Fluconazole and Ketoconazole. A docking study of the newly synthesized Schiff bases was performed, and results showed good binding affinity in the active site of co-crystallized Itraconazole-lanosterol 14α-demethylase isolated from Saccharomyces cerevisiae...
November 22, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27876085/onychomycosis-in-diabetic-patients-in-fako-division-of-cameroon-prevalence-causative-agents-associated-factors-and-antifungal-sensitivity-patterns
#8
Marvlyn Eba, Anna Longdoh Njunda, Rene Njikam Mouliom, Emmanuel Tebit Kwenti, Anold Nsoh Fuh, Gordon Takop Nchanji, Julius Atashili
BACKGROUND: Onychomycosis is an infection of the nail unit by a fungus. This is a very common infection amongst diabetics. Its occurrence among diabetics in Fako division is unknown. In this study we provide information on the characteristics of onychomycosis in diabetics in Fako division, Cameroon. METHODS: A cross-sectional descriptive and analytical hospital-based study was conducted in two diabetic clinics in the Buea and Limbe regional hospitals. We recruited 152 consenting diabetics into the study...
November 22, 2016: BMC Research Notes
https://www.readbyqxmd.com/read/27869874/-pharmacological-treatment-in-adrenal-cushing-s-syndrome
#9
Antonio Stigliano, Lidia Cerquetti, Vincenzo Toscano
ACTH-independent adrenal Cushing's syndrome is the least common form of endogenous hypercortisolism. Recently, advances in genetics have allowed the description of several forms different to pathogenetic etiology, morphostructural characteristics and evolution towards the hypercortisolism. Alongside these, the adrenocortical carcinoma is also frequently responsible of a hypercortisolism clinical picture. The availability of steroidogenesis inhibitors, such as metyrapone and ketoconazole, provides to endocrinologist a therapeutic chance against different metabolic disorders sustained by hypercortisolism...
November 2016: Recenti Progressi in Medicina
https://www.readbyqxmd.com/read/27865610/assessment-of-bioequivalence-of-weak-base-formulations-under-various-dosing-conditions-using-physiologically-based-pharmacokinetic-simulations-in-virtual-populations-case-examples-ketoconazole-and-posaconazole
#10
Rodrigo Cristofoletti, Nikunjkumar Patel, Jennifer B Dressman
Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way. The aim of this study was to evaluate whether the oral absorption of 2 poorly soluble, weakly basic APIs, ketoconazole (KETO) and posaconazole (POSA), would be equally sensitive to changes in dissolution rate under the following dosing conditions-coadministration with water, with food, with carbonated drinks, and in drug-induced hypochlorhydria...
November 16, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27859472/effect-of-ketoconazole-a-strong-cyp3a-inhibitor-on-the-pharmacokinetics-of-venetoclax-a-bcl-2-inhibitor-in-patients-with-non-hodgkin-lymphoma
#11
Suresh K Agarwal, Ahmed Hamed Salem, Alexey V Danilov, Beibei Hu, Soham Puvvada, Martin Gutierrez, David Chien, Lionel D Lewis, Shekman L Wong
AIM: To examine the effect of a strong CYP3A inhibitor, ketoconazole, on the pharmacokinetics, safety, and tolerability of venetoclax. METHODS: Twelve patients with Non-Hodgkin lymphoma (NHL) were enrolled in this Phase 1, open-label, fixed-sequence study. Patients received a single 50 mg dose of venetoclax orally on Day 1 and Day 8, and a 400 mg once daily dose of ketoconazole on Days 5 through 11. Blood samples were collected predose and up to 96 hours after each venetoclax dose on Day 1 and Day 8...
November 2, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27856196/a-fabric-phase-sorptive-extraction-high-performance-liquid-chromatography-photo-diode-array-detection-method-for-the-determination-of-twelve-azole-antimicrobial-drug-residues-in-human-plasma-and-urine
#12
Marcello Locatelli, Abuzar Kabir, Denise Innosa, Teresa Lopatriello, Kenneth G Furton
This paper reports a novel fabric phase sorptive extraction-high performance liquid chromatography-photodiode array detection (FPSE-HPLC-PDA) method for the simultaneous extraction and analysis of twelve azole antimicrobial drug residues that include ketoconazole, terconazole, voriconazole, bifonazole, clotrimazole, tioconazole, econazole, butoconazole, miconazole, posaconazole, ravuconazole, and itraconazole in human plasma and urine samples. The selected azole antimicrobial drugs were well resolved by using a Luna C18 column (250mm×4...
November 11, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27853018/infectious-pseudomonas-and-bipolaris-scleritis-following-history-of-pterygium-surgery
#13
Ashkan M Abbey, Nisha V Shah, Richard K Forster, Leejee H Suh
We report an interesting case of infectious scleritis from coinfection of Pseudomonas aeruginosa and Bipolaris with no corneal infiltrate. A healthy 60-year-old man with a history of infectious scleritis following pterygium excision presented with purulent material growing P. aeruginosa and 1+ colonies of Bipolaris species of fungus. Broad spectrum treatment was initiated with hourly topical moxifloxacin, fortified tobramycin, and natamycin along with a subconjunctival injection of voriconazole and topical cyclosporine, with PO ketoconazole...
September 2016: Indian Journal of Ophthalmology
https://www.readbyqxmd.com/read/27844446/severe-infliximab-induced-alopecia-and-scalp-psoriasis-in-a-woman-with-crohn-s-disease-dramatic-improvement-after-drug-discontinuation-and-treatment-with-adjuvant-systemic-and-topical-therapies
#14
Jeremy Udkoff, Philip R Cohen
Scalp psoriasis with alopecia is a rare cutaneous reaction to tumor necrosis factor alpha antagonists. This reaction often reverses with discontinuation of the offending drug and initiation of topical treatments; however, irreversible hair loss may occur if a scarring alopecia develops. We describe a woman with Crohn's disease who developed scalp psoriasis and alopecia secondary to infliximab. She had a remarkable recovery after discontinuation of infliximab and treatment with oral minocycline and topical therapy: mineral oil under occlusion, betamethasone lotion, and sequential coal tar, salicylic acid, and ketoconazole shampoos each day...
December 2016: Dermatology and Therapy
https://www.readbyqxmd.com/read/27836712/application-of-substrate-depletion-assay-to-evaluation-of-cyp-isoforms-responsible-for-stereoselective-metabolism-of-carvedilol
#15
Masahiro Iwaki, Toshiro Niwa, Saya Bandoh, Megumi Itoh, Hitomi Hirose, Atsushi Kawase, Hiroshi Komura
To evaluate the relative contribution of cytochrome P450 (CYP) isoforms responsible for carvedilol (CAR) oxidation, enantioselective metabolism of CAR was investigated in human liver microsomes (HLMs) and recombinant human CYPs by using the substrate depletion assay. CYP2D6 exhibited the highest contribution to the metabolism of R-CAR, followed by CYP3A4, CYP1A2, and CYP2C9, whereas the metabolism of the S-enantiomer was mainly mediated by CYP1A2, followed by CYP2D6 and CYP3A4. In HLMs, metabolism of R- and S-CAR was markedly inhibited by quinidine; R-CAR metabolism (57-61% decrease) was more inhibited than S-CAR metabolism (37-43% decrease), and furafylline and ketoconazole almost equally inhibited metabolism of both enantiomers by 25-32% and 30-50%, respectively...
September 2, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27836570/metabolic-induced-cytotoxicity-of-diosbulbin-b-in-cyp3a4-expressing-cells
#16
Ji-Zong Jiang, Bao-Hua Yang, Li-Li Ji, Li Yang, Yu-Chang Mao, Zhuo-Han Hu, Zheng-Tao Wang, Chang-Hong Wang
As a candidate antitumor agent, diosbulbin B (DB) can induce serious liver toxicity and other adverse reactions. DB is mainly metabolized by CYP3A4 in vitro and in vivo, but the cytotoxicity and anti-tumor mechanisms of DB have yet to be clarified. This study aimed to determine whether the cytotoxicity and anti-tumor effects of DB are related to the metabolism-induced activation of CYP3A4 in various cell models, including CYP-free NIH3T3 cells, primary rat hepatocytes, HepG2 and L02 cells of high CYP3A4 expression and wild-type...
November 9, 2016: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/27828657/pityriasis-amiantacea-a-study-of-seven-cases
#17
Gustavo Moreira Amorim, Nurimar Conceição Fernandes
Pityriasis amiantacea was first described in 1832. The disease may be secondary to any skin condition that primarily affects the scalp, including seborrheic dermatitis. Its pathogenesis remains uncertain. We aim to analyze the epidemiological and clinical profiles of patients with pityriasis amiantacea to better understand treatment responses. We identified seven cases of pityriasis amiantacea and a female predominance in a sample of 63 pediatric patients with seborrheic dermatitis followed for an average of 20...
September 2016: Anais Brasileiros de Dermatologia
https://www.readbyqxmd.com/read/27821711/low-potential-of-basimglurant-to-be-involved-in-drug-drug-interactions-influence-of-non-michaelis-menten-cyp-kinetics-on-fraction-metabolized
#18
Stephen M Fowler, Elena Guerini, NaHong Qiu, Yumi Cleary, Neil J Parrott, Gerard Greig, Navita L Mallalieu
Basimglurant, a novel mGlu5 negative allosteric modulator under development for the treatment of major depressive disorder, is cleared via cytochrome P450 (CYP) mediated oxidative metabolism. Initial enzyme phenotyping studies indicated that CYP3A4/5 dominated basimglurant metabolism and highlighted a risk for drug-drug interactions when comedicated with strong CYP3A4/5 inhibitors or inactivators. However, a clinical drug-drug interaction (DDI) study using the potent and selective CYP3A4/5 inhibitor ketoconazole resulted in an AUCi/AUC ratio of only 1...
November 7, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27816466/lysine-and-cysteine-based-protein-adductions-derived-from-toxic-metabolites-of-8-epidiosbulbin-e-acetate
#19
Dongju Lin, Kai Wang, Xiucai Guo, Huiyuan Gao, Ying Peng, Jiang Zheng
Furanoid 8-epidiosbulbin E acetate (EEA) is a major constituent of herbal medicine Dioscorea bulbifera L. (DB), a traditional herbal medicine widely used in Asian nations. Our early studies demonstrated that administration of EEA caused acute hepatotoxicity in mice and the observed toxicity required P450-mediated metabolic activation. Protein modification by reactive metabolites of EEA has been suggested to be an important mechanism of EEA-induced hepatotoxicity. The objectives of the present study were to investigate the interaction of the electrophilic reactive metabolites derived from EEA with lysine and cysteine residues of proteins and to define the correlation of protein adductions of EEA and the hepatotoxicity induced by EEA...
November 2, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27815659/in-vitro-antifungal-susceptibility-of-neoscytalidium-dimidiatum-clinical-isolates-from-malaysia
#20
Jasper Elvin James, Jacinta Santhanam, Mei Chen Lee, Choon Xian Wong, Parameswari Sabaratnam, Hamidah Yusoff, Mohd Nizam Tzar, Mohd Fuat Abdul Razak
Neoscytalidium dimidiatum is an opportunistic fungus causing cutaneous infections mostly, which are difficult to treat due to antifungal resistance. In Malaysia, N. dimidiatum is associated with skin and nail infections, especially in the elderly. These infections may be mistaken for dermatophyte infections due to similar clinical appearance. In this study, Neoscytalidium isolates from cutaneous specimens, identified using morphological and molecular methods (28 Neoscytalidium dimidiatum and 1 Neoscytalidium sp...
November 4, 2016: Mycopathologia
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