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https://www.readbyqxmd.com/read/28624525/regulation-of-hepatic-abcb4-and-cyp3a65-gene-expression-and-multidrug-multixenobiotic-resistance-mdr-mxr-functional-activity-in-the-model-teleost-danio-rerio-zebrafish
#1
Jeremy S Jackson, Christopher J Kennedy
Multidrug/multixenobiotic resistance (MDR/MXR) confers resistance to a diverse range of potentially toxic pharmaceuticals and environmental contaminants through a cellular response that involves the coordinated induction and activity of the ATP-binding cassette (ABC) transporter P-glycoprotein (P-gp) and the Phase I metabolizing enzyme cytochrome P450 3A (CYP3A). In mammals, ligand-mediated pregnane X receptor (PXR) transcriptional activity regulates the induction of P-gp and CYP3A; however, this mechanism has not been well-characterized in fish...
June 14, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28620619/effects-of-1e-4e-2-methyl-1-5-bis-4-nitrophenyl-penta-1-4-dien-3-one-on-trypanosoma-cruzi-and-its-combinational-effect-with-benznidazole-ketoconazole-or-fluconazole
#2
Francieli Peron, Danielle Lazarin-Bidóia, Zia Ud Din, Edson Rodrigues-Filho, Tânia Ueda-Nakamura, Sueli de Oliveira Silva, Celso Vataru Nakamura
This study reports the activity induced by (1E,4E)-2-methyl-1,5-bis(4-nitrophenyl)penta-1,4-dien-3-one (A3K2A3) against Trypanosoma cruzi. This compound showed trypanocidal activity against the multiplicative epimastigote and amastigote forms of this protozoan, with IC50 values of 1.99 ± 0.17 and 1.20 ± 0.16 μM, respectively, and EC50 value of 15.57 ± 0.34 μM against trypomastigotes. The combination of A3K2A3 with benznidazole or ketoconazole demonstrated strong synergism, increasing effectiveness against trypomastigotes or epimastigotes of T...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28603935/the-effects-of-ketoconazole-and-cimetidine-on-the-pharmacokinetics-of-oral-tramadol-in-greyhound-dogs
#3
B KuKanich, K KuKanich, J Black
Tramadol is administered to dogs for analgesia but has variability in its extent of absorption, which may hinder its efficacy. Additionally, the active opioid metabolite (M1) occurs in low concentrations. The purpose of this study was to determine if administration of oral tramadol with suspected metabolism inhibitors (ketoconazole, cimetidine) would lead to improved bioavailability of tramadol and M1. Six healthy Greyhounds were included. They were administered tramadol orally and intravenously, M1 intravenously, oral tramadol with oral ketoconazole and oral tramadol with oral cimetidine...
June 11, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28601511/synthesis-molecular-modelling-and-cyp24a1-inhibitory-activity-of-novel-of-e-n-2-1h-imidazol-1-yl-2-phenylethyl-3-4-styrylbenzamides
#4
Ismail M Taban, Jinge Zhu, Hector F DeLuca, Claire Simons
CYP24A1 (25-hydroxyvitamin D-24-hydroxylase) is a useful enzyme target for a range of medical conditions including cancer, cardiovascular and autoimmune disease, which show elevated CYP24A1 levels and corresponding reduction of calcitriol (the biologically active form of vitamin D). A series of (E)-N-(2-(1H-imidazol-1-yl)-2-(phenylethyl)-3/4-styrylbenzamides have been synthesised using an efficient synthetic route and shown to be potent inhibitors of CYP24A1 (IC50 0.11-0.35μM) compared with the standard ketoconazole...
May 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28595275/antifungal-susceptibility-of-sporothrix-schenckii-complex-biofilms
#5
Raimunda Sâmia Nogueira Brilhante, Felipe Rodrigues Magalhães de Aguiar, Maria Lucilene Queiroz da Silva, Jonathas Sales de Oliveira, Zoilo Pires de Camargo, Anderson Messias Rodrigues, Vandbergue Santos Pereira, Rosana Serpa, Débora de Souza Collares Maia Castelo-Branco, Edmilson Emanuel Monteiro Correia, Waldemiro Aquino Pereira-Neto, Rossana de Aguiar Cordeiro, Marcos Fábio Gadelha Rocha, José Júlio Costa Sidrim
Sporotrichosis, caused by species of Sporothrix schenckii complex, is the most prevalent subcutaneous mycosis in many areas of Latin America. The aim of this study was to evaluate the ability of Sporothrix spp. to form biofilms in vitro and to characterize the growth kinetics, morphology, and antifungal susceptibility of biofilms against classical antifungals. We investigated the ability of strains to produce biofilms in vitro and determined the effects of exposure to amphotericin B, itraconazole, caspofungin, ketoconazole, voriconazole, and fluconazole at minimum inhibitory concentration (MIC) against planktonic form and at 10× MIC and 50× MIC on the biomass and metabolic activity of these biofilms...
June 8, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28584446/antimicrobial-activity-of-various-ethanolic-plant-extracts-against-pathogenic-multi-drug-resistant-candida-spp
#6
Shaista Khan, Mohd Imran, Mohammed Imran, Nuzhat Pindari
A total of 50 Candida isolates were isolated and identified from clinical specimens and these were tested for resistance to various antifungal drugs. It was observed multi-drug resistance in all candida isolates by 84%, 62%, 60%, 76%, 46, 30%, and 22% against fluconazole, clotrimazole, Amphotericin B, itraconazole, ketoconazole, miconazole and nystatin tested respectively. The isolates, which were found to be resistant to antifungal drugs were selected and subjected to antifungal testing against six ethanolic plants, extract namely Azadiracta indica, Allium sativum, Cordia dichotoma Ocimum sanctum, Syzygium cumini and Trigonella foenum grecum...
2017: Bioinformation
https://www.readbyqxmd.com/read/28584167/severe-cushing-s-syndrome-due-to-small-cell-prostate-carcinoma-a-case-and-review-of-literature
#7
Marianne Elston, Veronica Crawford, Michael Swarbrick, Michael Dray, Michelle Head, John V Conaglen
Cushings syndrome (CS) due to ectopic adrenocorticotrophic hormone (ACTH) is associated with a variety of tumours most of which arise in the thorax or abdomen. Prostate carcinoma is a rare but important cause of rapidly progressive CS. To report a case of severe CS due to ACTH production from prostate neuroendocrine carcinoma and summarise previous published cases. A 71 year old man presented with profound hypokalaemia, oedema and new onset hypertension. He reported two weeks of weight gain, muscle weakness, labile mood and insomnia...
June 5, 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28578073/identification-of-endocrine-disrupting-chemicals-acting-on-human-aromatase
#8
Roberta Baravalle, Alberto Ciaramella, Francesca Baj, Giovanna Di Nardo, Gianfranco Gilardi
Human aromatase is the cytochrome P450 catalysing the conversion of androgens into estrogens playing a key role in the endocrine system. Due to this role, it is likely to be a target of the so-called endocrine disrupting chemicals, a series of compounds able to interfere with the hormone system with toxic effects. If on one side the toxicity of some compounds such as bisphenol A is well known, on the other side the toxic concentrations of such compounds as well as the effect of the many other molecules that are in contact with us in everyday life still need a deep investigation...
May 31, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28575987/y-shaped-methoxy-poly-ethylene-glycol-block-poly-epsilon-caprolactone-based-micelles-for-skin-delivery-of-ketoconazole-in-vitro-study-and-in-vivo-evaluation
#9
Peizong Deng, Fangfang Teng, Feilong Zhou, Zhimei Song, Ning Meng, Na Liu, Runliang Feng
Ketoconazole is a hydrophobic broad-spectrum antifungal agent for skin infection therapy. In order to develop topical formulation of ketoconazole for improving its selective skin deposition and water-solubility, ketoconazole-loaded Y-shaped monomethoxy poly(ethylene glycol)-block-poly(ɛ-caprolactone) micelles were prepared through thin-film hydration method with high entrapment efficiency (96.1±0.76%) and small particle (about 58.66nm). The drug-loaded micelles showed comparative in vitro antimicrobial activity with KET cream...
September 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28546693/disseminated-rhinosporidiosis-with-conjunctival-involvement-in-an-immunocompromised-patient
#10
Deepa John, Satheesh S T Selvin, Aparna Irodi, Pushpa Jacob
Rhinosporidiosis is a granulomatous infection of mucocutaneous tissue caused by Rhinosporidium seeberi that most commonly occurs in the nasal cavity. Ocular rhinosporidiosis affects primarily the conjunctiva. Diagnosis of rhinosporidiosis is based on strong clinical suspicion and is confirmed by histopathological examination. We report a rare case of conjunctival rhinosporidiosis in an immunocompromised patient (human immunodeficiency virus) with disseminated cutaneous rhinosporidiosis. A 44-year-old male presented with a swelling in the right upper eyelid for 6 months...
January 2017: Middle East African Journal of Ophthalmology
https://www.readbyqxmd.com/read/28540871/clinico-mycological-study-of-dermatophytic-infections-and-their-sensitivity-to-antifungal-drugs-in-a-tertiary-care-center
#11
Soniya Mahajan, Ragini Tilak, Satyendra K Kaushal, Rabindra N Mishra, Shyam S Pandey
BACKGROUND: Worldwide, dermatophytic infections are running a chronic course either due to ineffective treatment or emerging drug resistance. In the past three decades, there has been an increase in incidence and non-responsiveness to conventional antifungals, which suggests that there is a need of antifungal sensitivity testing. AIMS: This study was aimed at identifying clinico-mycological pattern of dermatophytic infections in patients attending thedermatology outpatient department of a tertiary care hospital, and to obtain the sensitivity pattern of isolates against six commonly used oral antifungals (fluconazole, terbinafine, itraconazole, ketoconazole, griseofulvin and voriconazole)...
July 2017: Indian Journal of Dermatology, Venereology and Leprology
https://www.readbyqxmd.com/read/28539243/synthesis-sar-and-molecular-docking-studies-of-benzo-d-thiazole-hydrazones-as-potential-antibacterial-and-antifungal-agents
#12
Gao-Feng Zha, Jing Leng, N Darshini, T Shubhavathi, H K Vivek, Abdullah M Asiri, Hadi M Marwani, K P Rakesh, N Mallesha, Hua-Li Qin
A series of new benzo[d]thiazole-hydrazones analogues were synthesized and screened for their in vitro antibacterial and antifungal activities. The results revealed that compounds 13, 14, 15, 19, 20, 28 and 30 exhibited superior antibacterial potency compared to the reference drug chloramphenicol and rifampicin. Compounds 5, 9, 10, 11, 12, 28 and 30 were found to be good antifungal activity compared to the standard drug ketoconazole. A preliminary study of the structure-activity relationship (SAR) revealed that the antimicrobial activity depended on the effect of different substituents on the phenyl ring...
May 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28535410/effect-of-enzyme-inhibition-on-perampanel-pharmacokinetics-why-study-design-matters
#13
Barry E Gidal, Rama Maganti, Antonio Laurenza, Haichen Yang, David A Verbel, Edgar Schuck, Jim Ferry
OBJECTIVES: Perampanel, a selective, noncompetitive AMPA receptor antagonist, is indicated as adjunctive therapy for the treatment of partial seizures with or without secondarily generalized seizures and primary generalized tonic-clonic seizures in patients with epilepsy aged 12years and older. In vitro studies and Phase I trials indicate that perampanel is metabolized almost exclusively by CYP3A, with an elimination half-life (t1/2) averaging approximately 105h. Understanding of pharmacokinetic (PK) interactions-enzyme inhibition or induction-and anticipating their occurrence are important for management of patients with epilepsy...
April 26, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28527633/anthelmintic-activity-of-cytochrome-p450-inhibitors-miconazole-and-clotrimazole-in-vitro-effect-on-the-liver-fluke-opisthorchis-felineus
#14
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 it 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/28503943/transcriptional-profile-of-ethylene-glycol-monomethyl-ether-induced-testicular-toxicity-in-rats
#15
Takuya Matsuyama, Koichi Yabe, Chiharu Kuwata, Kazumi Ito, Yosuke Ando, Hiroshi Iida, Kazuhiko Mori
To clarify the molecular mechanism of ethylene glycol monomethyl ether (EGME)-induced testicular toxicity, the potential for EGME-related changes in transcript levels of genes including spermatocyte-specific genes was evaluated in the testis of rats given single dosing of EGME at 200, 600, or 2000 mg/kg. Furthermore, the contribution of decreased testicular testosterone on EGME-induced spermatocyte toxicity was investigated by comparing to transcriptional profile due to a testosterone synthesis inhibitor, ketoconazole (KET), at 30 or 300 mg/kg...
May 15, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/28503781/assessment-of-effect-of-cyp3a-inhibition-cyp-induction-oatp1b-inhibition-and-high-fat-meal-on-pharmacokinetics-of-the-jak1-inhibitor-upadacitinib
#16
Mohamed-Eslam F Mohamed, Steven Jungerwirth, Armen Asatryan, Ping Jiang, Ahmed A Othman
AIMS: Upadacitinib (ABT-494) is a selective Janus kinase 1 inhibitor developed for treatment of auto-immune inflammatory disorders. This work evaluated effects of high-fat meal, cytochrome P450 (CYP) 3A inhibition, CYP induction, and organic anion transporting polypeptide (OATP) 1B inhibition on upadacitinib pharmacokinetics. METHODS: Two Phase 1 evaluations were conducted, each in 12 healthy subjects. In Study 1, using a randomized, 2-sequence cross-over design, a 3 mg dose of upadacitinib (immediate-release capsules) was administered alone under fasting conditions, after high-fat meal, or on Day 4 of a 6-day regimen of 400 mg once-daily ketoconazole...
May 14, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28495902/regio-and-stereo-selective-oxidation-of-a-cardiovascular-drug-metoprolol-mediated-by-cytochrome-p450-2d-and-3a-enzymes-in-marmoset-livers
#17
Shotaro Uehahara, Sakura Ishii, Yasuhiro Uno, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
A β-blocker metoprolol is one of the in vivo probes for human cytochrome P450 (P450) 2D6. Investigation of non-human primate P450 enzymes helps improve accuracy of the extrapolation of pharmacokinetic data from animals into humans. Common marmosets (Callithrix jacchus) are a potential primate model for preclinical research, but detailed roles of marmoset P450 enzymes in metoprolol oxidations remained unknown. In this study, regio- and stereo-selectivity of metoprolol oxidations by a variety of P450 enzymes in marmoset and human livers were investigated in vitro...
May 11, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28492744/surface-properties-of-temporary-soft-liners-modified-by-minimum-inhibitory-concentrations-of-antifungals
#18
Mírian Galvão Bueno, Elen Juliana Bonassa de Sousa, Juliana Hotta, Vinícius Carvalho Porto, Vanessa Migliorini Urban, Karin Hermana Neppelenbroek
Evaluating the addition of minimum inhibitory concentrations (MICs) of antifungals for Candida albicans biofilm on the hardness and roughness of temporary denture soft liners. Specimens (n=8; 36×7×6 mm) of tissue conditioner (Softone) and resilient liner (Trusoft) were produced either without (control) or with incorporation of drugs at MICs: nystatin (0.032 g/mL), chlorhexidine diacetate (0.064 g/mL), ketoconazole (0.128 g/mL), miconazole (0.256 g/mL) and itraconazole (0.256 g/mL). Specimens were stored in distilled water at 37 °C for 24 h, 7 days and 14 days prior to the hardness/roughness measurements...
January 2017: Brazilian Dental Journal
https://www.readbyqxmd.com/read/28483956/the-tetrazole-vt-1161-is-a-potent-inhibitor-of-trichophyton-rubrum-through-its-inhibition-of-t-rubrum-cyp51
#19
Andrew G S Warrilow, Josie E Parker, Claire L Price, Edward P Garvey, William J Hoekstra, Robert J Schotzinger, Nathan P Wiederhold, W David Nes, Diane E Kelly, Steven L Kelly
Prior to characterization of antifungal inhibitors that target this enzyme, Trichophyton rubrum CYP51 was expressed in Escherichia coli, purified and characterized. T. rubrum CYP51 bound lanosterol, obtusifoliol and eburicol with similar affinities (Kd values 22.7, 20.3 and 20.9 μM), but displayed substrate specificity insofar as only eburicol was demethylated in CYP51 reconstitution assays (turnover number 1.55 min(-1), Km value 2 μM). The investigational agent VT-1161 bound tightly to T. rubrum CYP51 (Kd = 242 nM) with similar affinity as clotrimazole, fluconazole, ketoconazole and voriconazole (Kd values 179, 173, 312, and 304 nM, respectively), and with lower affinity than itraconazole (Kd = 53 nM)...
May 8, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28482538/spherical-silver-nanoparticles-as-substrates-in-surface-enhanced-raman-spectroscopy-for-enhanced-characterization-of-ketoconazole
#20
Mutasem M Al-Shalalfeh, Abdulmujeeb T Onawole, Tawfik A Saleh, Abdulaziz A Al-Saadi
A new method was developed for the characterization and detection of ketoconazole using surface enhanced Raman spectroscopy (SERS) by designing substrates and performing the bands' assignments. Thus, spherical silver nanoparticles (Ag-NPs) were synthesized by a reduction method and designed as substrates for SERS application. The Ag-NPs were characterized using a scanning electron microscope, Fourier transformed infrared spectroscopy and a high-resolution transmission electron microscope. TEM results indicated that the average size of the Ag-NPs was 15nm...
July 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
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