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https://www.readbyqxmd.com/read/28546693/disseminated-rhinosporidiosis-with-conjunctival-involvement-in-an-immunocompromised-patient
#1
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
#2
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)...
May 22, 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
#3
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
#4
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
#5
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/28503943/transcriptional-profile-of-ethylene-glycol-monomethyl-ether-induced-testicular-toxicity-in-rats
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/28479418/development-of-an-assay-for-cellular-efflux-of-pharmaceutically-active-agents-and-its-relevance-to-understanding-drug-interactions
#12
Benigno C Valdez, Moustapha Hassan, Borje S Andersson
Drug interactions may dictate the failure or success of a treatment. Patients undergoing hematopoietic stem cell transplantation (HSCT) are exposed to various types of drugs and it is of utmost importance to understand how these drugs interact. The pharmacokinetics of busulfan, melphalan and cyclophosphamide, commonly used drugs in HSCT, are known to be affected by a variety of drugs with differing molecular structures. We hypothesized that these structurally-unrelated drugs affect the transport of DNA alkylating agents...
May 4, 2017: Experimental Hematology
https://www.readbyqxmd.com/read/28472585/real-time-imaging-of-the-azole-class-of-antifungal-drugs-in-live-candida-cells
#13
Raphael I Benhamou, Maayan Bibi, Kfir B Steinbuch, Hamutal Engel, Maayan Levin, Yael Roichman, Judith Berman, Micha Fridman
Azoles are the most commonly used class of antifungal drugs, yet where they localize within fungal cells and how they are imported remain poorly understood. Azole antifungals target lanosterol 14α-demethylase, a cytochrome P450, encoded by ERG11 in Candida albicans, the most prevalent fungal pathogen. We report the synthesis of fluorescent probes that permit visualization of antifungal azoles within live cells. Probe 1 is a dansyl dye-conjugated azole, and probe 2 is a Cy5-conjugated azole. Docking computations indicated that each of the probes can occupy the active site of the target cytochrome P450...
May 12, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28472279/the-genetic-architecture-in-saccharomyces-cerevisiae-that-contributes-to-variation-in-drug-response-to-the-antifungals-benomyl-and-ketoconazole
#14
Christina A Roberts, John H Miller, Paul H Atkinson
The genetic basis of variation in drug response was investigated in individual Saccharomyces cerevisiae strains that exhibited different susceptibility to two antifungal agents-benomyl and ketoconazole. Following dose-response screening of 25 strains, four were selected on the basis of resistance or sensitivity relative to the standard laboratory strain BY. UWOPS87-2421 and L-1374 were respectively resistant and sensitive to benomyl; DBVPG6044 and Y12 were respectively resistant and sensitive to ketoconazole...
May 2, 2017: FEMS Yeast Research
https://www.readbyqxmd.com/read/28462780/-african-histoplamosis-a-report-of-three-pediatric-cases
#15
REVIEW
J R Mabiala Babela, C Mboutol Mandavo, R Nika Evrard, B Ossibi Ibara, L Lamah, L C Ollandzobo Ikobo, A Mouko, J F Peko
Histoplasmosis duboisii (Histoplasma capsulatum var duboisii) is uncommon disease especially in children. It is observed in Africa where the incidence is unknown. The authors report a series of three pediatric cases. The report concerned 2 girls and one boy who were 3, 9 and 4 year-old, respectively. Symptoms evolved for more than two months in each case. At admission, we found fever and poor general condition. Observed lesions were lymphnodes localisation disseminated (cases 1 and 2), subcutaneous (cold abscess) and cutaneous simulating molluscum contagiosum (case 2), osteoarticular (cases 2 and 3), abdominal including peritoneal and hepatosplenic (case 1)...
April 24, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28461309/crystal-structure-of-the-new-investigational-drug-candidate-vt-1598-in-complex-with-aspergillus-fumigatus-sterol-14%C3%AE-demethylase-provides-insights-into-its-broad-spectrum-antifungal-activity
#16
Tatiana Y Hargrove, Edward P Garvey, William J Hoekstra, Christopher M Yates, Zdzislaw Wawrzak, Girish Rachakonda, Fernando Villalta, Galina I Lepesheva
Within the past decades, the incidence and complexity of human fungal infections have increased, and therefore the need for safer and more efficient, broad-spectrum antifungal agents is high. Herein, we characterize the new tetrazole-based drug candidate VT-1598 as an inhibitor of sterol 14α-demethylase (CYP51B) from the filamentous fungi Aspergillus fumigatus VT-1598 displayed a high binding affinity to the enzyme in solution (with the Kd of 13±1 nM) and in the reconstituted enzymatic reaction revealed the inhibitory potency stronger than the potencies of all other simultaneously tested antifungal drugs, including fluconazole, voriconazole, ketoconazole, and posaconazole...
May 1, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28451009/-pityriasis-versicolor-in-infants-unusual-clinical-presentation-and-role-of-corticosteroids-used-as-depigmenting-agent-for-cosmetic-purposes-in-the-mother
#17
Pauline Dioussé, Fatimata Ly, Mariama Bammo, Sarah Lizia, Thierno Abdoul Aziz Diallo, Haby Dione, Fatou Sarr, Ramatoulaye Diagne Gueye, Amadou Mactar Gueye, Mame Thierno Dieng, Bernard Marcel Diop, Mamadou Mourtalla Ka
We report two cases of Pityriasis versicolor (PV) in infants aged 12 and 18 months. The latter were brought to medical attention because of hypochromic and achromic, round macules involving the limbs and the face. Physical examination of their mothers showed voluntary depigmentation for cosmetic purposes due to the use of corticosteroids and hydroquinone, on average, over a 5-year period. The scotch tape test performed in one of the infants and his mother showed short filaments and clusters of spores. Treatment was based on ketoconazole...
2017: Pan African Medical Journal
https://www.readbyqxmd.com/read/28450771/in-vitro-antifungal-susceptibility-of-environmental-isolates-of-cryptococcus-spp-from-the-west-region-of-cameroon
#18
William Dongmo, Frederick Kechia, Roland Tchuenguem, Claude Nangwat, Iwewe Yves, Jules-Roger Kuiate, Jean Paul Dzoyem
BACKGROUND: Cryptococcus neoformans is responsible of cryptococcosis, a life-threatening infection that affects healthy and immunocompromised individuals. It is the first cause of adult acute meningitis in some sub-Saharan African countries with a mortality rate of about 100% in cases of inappropriate therapy. This study aimed at examining the occurrence and the antifungal patterns of Cryptococcus isolates from pigeon droppings and bat guanos in the west region of Cameroon. METHODS: A total of 350 samples were randomly collected from three selected localities of west region of Cameroon...
November 2016: Ethiopian Journal of Health Sciences
https://www.readbyqxmd.com/read/28449377/topical-antiviral-and-antifungal-medications-in-pregnancy-a-review-of-safety-profiles
#19
REVIEW
Viral M Patel, Robert A Schwartz, William C Lambert
Medications should be employed with caution in women of childbearing age who are pregnant or considering pregnancy. Compared to oral or parenteral agents, topical medications have limited systemic absorption and are deemed safer. However, their safety profile must be assessed cautiously due to the limited available data. In this article, we aggregate human and animal studies to provide recommendations on utilizing topical antiviral and antifungal medications in pregnancy. For antiviral medications, acyclovir and trichloroacetic acid are safe to use in pregnancy...
April 27, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/28443986/minimal-inhibitory-concentration-distributions-and-epidemiological-cutoff-values-of-five-antifungal-agents-against-sporothrix-brasiliensis
#20
Rodrigo Almeida-Paes, Fábio Brito-Santos, Maria Helena Galdino Figueiredo-Carvalho, Ana Caroline Sá Machado, Manoel Marques Evangelista Oliveira, Sandro Antonio Pereira, Maria Clara Gutierrez-Galhardo, Rosely Maria Zancopé-Oliveira
BACKGROUND: Sporothrix brasiliensis is the most virulent sporotrichosis agent. This species usually responds to antifungal drugs, but therapeutic failure can occur in some patients. Antifungal susceptibility tests have been performed on this species, but no clinical breakpoints (CBPs) are available. In this situation, minimal inhibitory concentration (MIC) distributions and epidemiological cutoff values (ECVs) support the detection of identification of resistant strains. OBJECTIVES: To study the MIC distributions of five antifungal drugs against S...
May 2017: Memórias do Instituto Oswaldo Cruz
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