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https://www.readbyqxmd.com/read/28927230/multi-azole-resistant-strains-of-cryptococcus-neoformans-var-grubii-isolated-from-a-flz-resistant-strain-by-culturing-in-medium-containing-voriconazole
#1
Rui Kano, Miki Okubo, Atsuhiko Hasegawa, Hiroshi Kamata
A Cryptococcus neoformans var. grubii strain, NUBS14020, was the first fluconazole (FLZ)-resistant strain isolated from a feline cryptococcosis. Subsequent work demonstrated that multi-azole-resistant strains are readily isolated from FLZ-resistant strains by culturing in medium containing voriconazole (VRZ). The resulting clones were assessed for mutation and expression of known target genes, including the loci encoding lanosterol 14-α demethylase (ERG11), an ATP-binding cassette (ABC) transporter (AFR1), or a multidrug efflux pump (MEP); mutation and/or overexpression of these genes is known to be associated with azole resistance...
September 11, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28926063/methylglyoxal-attenuates-insulin-signaling-and-downregulates-the-enzymes-involved-in-cholesterol-biosynthesis
#2
Arati B Deshmukh, Shakuntala Bai, Aarthy T, Rubina S Kazi, Reema Banarjee, Rajeshwari Rathore, Vijayakumar Mv, Thulasiram Hv, Manoj Kumar Bhat, Kulkarni Mj
Methylglyoxal (MG) is a highly reactive dicarbonyl known to be elevated under the hyperglycemic conditions of diabetes and is implicated in the development of diabetic complications. Therefore, the current study investigates the role of MG in exacerbating insulin resistance at the insulin signaling level, as well as its effect on the global proteomic level. By using insulin sensitive rat muscle cells (L6) and Chinese hamster ovary (CHO) cells stably expressing the insulin receptor (IR) and a glucose transporter fused with green fluorescent protein (GLUT4-GFP), we have observed that MG impairs insulin signaling, inhibits GLUT4 translocation and reduces glucose uptake...
September 19, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28888677/quantitation-of-lanosterol-in-the-vitreous-humor-of-rabbits-after-ocular-administration-of-lanosterol-thermogel-formulation-by-ultra-performance-liquid-chromatography-tandem-mass-spectrometry-with-the-electrospray-ionization-mode
#3
Lei Lv, Dan Li, Hui Wang, Chengjian Li, Xian Qian, Heng-Tao Dong, Jianguo Sun, Liang Zhao
Cataracts are the most common cause of blindness worldwide affecting tens of millions of people. Here, we report a simple, rapid, sensitive and specific method by ultra performance liquid chromatography-tandem mass spectrometry with the electrospray ionization mode (UPLC-ESI-MS/MS) for quantitation of lanosterol, a possible effective drug for cataracts, in the vitreous humor of rabbits after ocular administration. The injected lanosterol was prepared by dispersing lanosterol molecules into the poly-(dl-lactic acid-co-glycolic acid)-poly(ethylene glycol)-poly-(dl-lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) thermogel solution...
September 1, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28838629/in-vitro-antifungal-activity-of-cassia-fistula-extracts-against-fluconazole-resistant-strains-of-candida-species-from-hiv-patients
#4
P Sony, M Kalyani, D Jeyakumari, I Kannan, R G Sukumar
BACKGROUND: Candida species is the fourth common cause of blood stream infections all over the world which is life threatening. Invasive candidiasis leads to increased mortality and morbidity especially in immunosuppressed. The antifungal resistance pattern in high-risk patients is major concern. PURPOSE: The present study was to access the anticandidal activity of leaves, bark and seeds of Cassia fistula against fluconazole resistant Candida species, C. albicans, C...
August 21, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28830911/nitric-oxide-stimulates-cellular-degradation-of-human-cyp51a1-the-highly-conserved-lanosterol-14%C3%AE-demethylase
#5
Ji Won Park, Aria Byrd, Choon-Myung Lee, Edward T Morgan
Nitric oxide (NO) is known to down-regulate drug metabolizing cytochrome P450 enzymes in an enzyme-selective manner. Ubiquitin-proteasome dependent and independent pathways have been reported. Here we studied the regulation of expression of human CYP51A1, the lanosterol 14α-demethylase required for synthesis of cholesterol and other sterols in mammals, which is found in every kingdom of life.  In Huh7 human hepatoma cells, treatment with NO donors caused rapid post-translational down-regulation of CYP51A1 protein...
August 22, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28828630/lanosterol-synthase-like-is-involved-with-differential-accumulation-of-steroidal-glycoalkaloids-in-potato
#6
Akhilesh Kumar, Edna Fogelman, Mira Weissberg, Zachariah Tanami, Richard E Veilleux, Idit Ginzberg
Phytosterol homeostasis may be maintained in leaves through diversion of intermediates into glycoalkaloid biosynthesis, whereas in tuber flesh, excess intermediates are catalyzed by tuber-specific StLAS - like , resulting in low tuber glycoalkaloids. Lanosterol synthase (LAS) and cycloartenol synthase (CAS) are phylogenetically related enzymes. Cycloartenol is the accepted precursor leading to cholesterol and phytosterols, and in potato, to steroidal glycoalkaloid (SGA) biosynthesis. LAS was also shown to synthesize some plant sterols, albeit at trace amounts, questioning its role in sterol homeostasis...
August 21, 2017: Planta
https://www.readbyqxmd.com/read/28811501/characterisation-of-sterol-biosynthesis-and-validation-of-14%C3%AE-demethylase-as-a-drug-target-in-acanthamoeba
#7
Scott Thomson, Christopher A Rice, Tong Zhang, RuAngelie Edrada-Ebel, Fiona L Henriquez, Craig W Roberts
The soil amoebae Acanthamoeba causes Acanthamoeba keratitis, a severe sight-threatening infection of the eye and the almost universally fatal granulomatous amoebic encephalitis. More effective treatments are required. Sterol biosynthesis has been effectively targeted in numerous fungi using azole compounds that inhibit the cytochrome P450 enzyme sterol 14α-demethylase. Herein, using Gas Chromatography Mass Spectrometry (GCMS), we demonstrate that the major sterol of Acanthamoeba castellanii is ergosterol and identify novel putative precursors and intermediate sterols in its production...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28750236/development-validation-and-application-of-a-gc-ms-method-for-the-simultaneous-detection-and-quantification-of-neutral-lipid-species-in-trypanosoma-cruzi
#8
Mery Santivañez-Veliz, Elsa Moreno-Viguri, Silvia Pérez-Silanes, Javier Varela, Hugo Cerecetto, Mercedes González, Elena Lizarraga
The development and validation of an analytical method for the simultaneous analysis of five neutral lipids in Trypanosoma cruzi epimastigotes by GC-MS is presented in this study. The validated method meets all validation parameters for all components and the chromatographic conditions have been optimized during its development. This analytical method has demonstrated good selectivity, accuracy, within-day precision, recovery and linearity in each of the established ranges. In addition, detection and quantification limits for squalene, cholesterol, ergosterol and lanosterol have been improved and it is worth highlighting the fact that this is the first time that squalene-2,3-epoxide validation data have been reported...
July 19, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28713270/evaluation-of-selected-cyp51a1-polymorphisms-in-view-of-interactions-with-substrate-and-redox-partner
#9
Tadeja Režen, Iza Ogris, Marko Sever, Franci Merzel, Simona Golic Grdadolnik, Damjana Rozman
Cholesterol is essential for development, growth, and maintenance of organisms. Mutations in cholesterol biosynthetic genes are embryonic lethal and few polymorphisms have been so far associated with pathologies in humans. Previous analyses show that lanosterol 14α-demethylase (CYP51A1) from the late part of cholesterol biosynthesis has only a few missense mutations with low minor allele frequencies and low association with pathologies in humans. The aim of this study is to evaluate the role of amino acid changes in the natural missense mutations of the hCYP51A1 protein...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28698522/design-synthesis-and-biological-activity-of-new-triazole-and-nitro-triazole-derivatives-as-antifungal-agents
#10
Hossein Sadeghpour, Soghra Khabnadideh, Kamiar Zomorodian, Keyvan Pakshir, Khadijeh Hoseinpour, Nabiollah Javid, Ehsan Faghih-Mirzaei, Zahra Rezaei
In this study two series of fluconazole derivatives bearing nitrotriazole (series A) or piperazine ethanol (series B) side chain were designed and synthesized and then docked in the active site of lanosterol 14α-demethylase enzyme (1EA1) using the Autodock 4.2 program (The scripps research institute, La Jolla, CA, USA). The structures of synthesized compound were confirmed by various methods including elemental and spectral (NMR, CHN, and Mass) analyses. Then antifungal activities of the synthesized compound were tested against several natural and clinical strains of fungi using a broth microdilution assay against several standard and clinical fungi...
July 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28667115/cgmed3-changes-membrane-sterol-composition-to-help-candida-glabrata-tolerate-low-ph-stress
#11
Xiaobao Lin, Yanli Qi, Dongni Yan, Hui Liu, Xiulai Chen, Liming Liu
Candida glabrata is a promising microorganism for organic acid production. The present study aimed to investigate the role of C. glabrata Mediator complex subunit 3 (CgMed3p) in protecting C. glabrata under low-pH conditions. To this end, genes CgMED3A and CgMED3B were deleted, resulting in the double-deletion Cgmed3ABΔ strain. The final biomass and cell viability levels of Cgmed3ABΔ decreased by 64.5% and 35.8%, respectively, compared to the wild-type strain results at pH 2.0. In addition, lack of CgMed3ABp resulted in selective repression of a subset of genes in the lipid biosynthesis and metabolism pathways...
September 1, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28665796/contamination-of-pine-and-birch-wood-dust-with-microscopic-fungi-and-determination-of-its-sterol-contents
#12
Kinga Stuper-Szablewska, Tomasz Rogoziński, Juliusz Perkowski
Wood compounds, especially sterols, are connected with the level of contamination with microscopic fungi. Within this study, tests were conducted on wood dust samples collected at various work stations in a pine and birch timber conversion plant. Their contamination with mycobiota was measured as the concentration of ergosterol (ERG) by ultra performance liquid chromatography (UPLC). Another aim of this study was to assess the effect of contamination with microscopic fungi on the sterol contents in wood dusts...
June 27, 2017: Arhiv za Higijenu Rada i Toksikologiju
https://www.readbyqxmd.com/read/28658622/lanosterol-modulates-tlr4-mediated-innate-immune-responses-in-macrophages
#13
Elisa Araldi, Marta Fernández-Fuertes, Alberto Canfrán-Duque, Wenwen Tang, Gary W Cline, Julio Madrigal-Matute, Jordan S Pober, Miguel A Lasunción, Dianqing Wu, Carlos Fernández-Hernando, Yajaira Suárez
Macrophages perform critical functions in both innate immunity and cholesterol metabolism. Here, we report that activation of Toll-like receptor 4 (TLR4) in macrophages causes lanosterol, the first sterol intermediate in the cholesterol biosynthetic pathway, to accumulate. This effect is due to type I interferon (IFN)-dependent histone deacetylase 1 (HDAC1) transcriptional repression of lanosterol-14α-demethylase, the gene product of Cyp51A1. Lanosterol accumulation in macrophages, because of either treatment with ketoconazole or induced conditional disruption of Cyp51A1 in mouse macrophages in vitro, decreases IFNβ-mediated signal transducer and activator of transcription (STAT)1-STAT2 activation and IFNβ-stimulated gene expression...
June 27, 2017: Cell Reports
https://www.readbyqxmd.com/read/28637420/bioinformatics-insights-on-targets-receptors-of-amiodarone-in-human-and-acanthamoeba-castellanii
#14
Abdul Baig, Zohaib Rana, H R Ahmad
BACKGROUND: Amiodarone is prescribed for certain cardiac arrhythmias in medical practice. The drug targets and inhibits voltage dependent sodium (Na+v), calcium (Ca+2v), potassium (K+v) channels, and enzymes like cytochrome P450 and oxidosqualene cyclase. Past studies have shown that amiodarone exerts anti-amoebic effects against Trypanosoma cruzi and Acanthamoeba castellanii. OBJECTIVES: The presence of aforementioned targets and the type of cell death induced by amiodarone in these pathogenic eukaryotes like Acanthamoeba castellanii remain to be verified...
June 21, 2017: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/28579986/hiv-aspartic-peptidase-inhibitors-modulate-surface-molecules-and-enzyme-activities-involved-with-physiopathological-events-in-fonsecaea-pedrosoi
#15
Vanila F Palmeira, Daniela S Alviano, Lys A Braga-Silva, Fátima R V Goulart, Marcela Q Granato, Sonia Rozental, Celuta S Alviano, André L S Santos, Lucimar F Kneipp
Fonsecaea pedrosoi is the main etiological agent of chromoblastomycosis, a recalcitrant disease that is extremely difficult to treat. Therefore, new chemotherapeutics to combat this fungal infection are urgently needed. Although aspartic peptidase inhibitors (PIs) currently used in the treatment of human immunodeficiency virus (HIV) have shown anti-F. pedrosoi activity their exact mechanisms of action have not been elucidated. In the present study, we have investigated the effects of four HIV-PIs on crucial virulence attributes expressed by F...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28530827/overexpression-of-the-squalene-epoxidase-gene-alone-and-in-combination-with-the-3-hydroxy-3-methylglutaryl-coenzyme-a-gene-increases-ganoderic-acid-production-in-ganoderma-lingzhi
#16
De-Huai Zhang, Lu-Xi Jiang, Na Li, Xuya Yu, Peng Zhao, Tao Li, Jun-Wei Xu
The squalene epoxidase (SE) gene from the biosynthetic pathway of ganoderic acid (GA) was cloned and overexpressed in Ganoderma lingzhi. The strain that overexpressed the SE produced approximately 2 times more GA molecules than the wild-type (WT) strain. Moreover, SE overexpression upregulated lanosterol synthase gene expression in the biosynthetic pathway. These results indicated that SE stimulates GA accumulation. Then, the SE and 3-hydroxy-3-methylglutaryl coenzyme A (HMGR) genes were simultaneously overexpressed in G...
June 14, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28483956/the-tetrazole-vt-1161-is-a-potent-inhibitor-of-trichophyton-rubrum-through-its-inhibition-of-t-rubrum-cyp51
#17
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 CYP51, Trichophyton rubrum CYP51 was expressed in Escherichia coli, purified, and characterized. T. rubrum CYP51 bound lanosterol, obtusifoliol, and eburicol with similar affinities (dissociation constant [Kd ] values, 22.7, 20.3, and 20.9 μM, respectively) 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...
July 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28479228/design-strategies-of-oxidosqualene-cyclase-inhibitors-targeting-the-sterol-biosynthetic-pathway
#18
REVIEW
Vitor Won-Held Rabelo, Nelilma Correia Romeiro, Paula Alvarez Abreu
Targeting the sterol biosynthesis pathway has been explored for the development of new bioactive compounds. Among the enzymes of this pathway, oxidosqualene cyclase (OSC) which catalyzes lanosterol cyclization from 2,3-oxidosqualene has emerged as an attractive target. In this work, we reviewed the most promising OSC inhibitors from different organisms and their potential for the development of new antiparasitic, antifungal, hypocholesterolemic and anticancer drugs. Different strategies have been adopted for the discovery of new OSC inhibitors, such as structural modifications of the natural substrate or the reaction intermediates, the use of the enzyme's structural information to discover compounds with novel chemotypes, modifications of known inhibitors and the use of molecular modeling techniques such as docking and virtual screening to search for new inhibitors...
July 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28472585/real-time-imaging-of-the-azole-class-of-antifungal-drugs-in-live-candida-cells
#19
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/28462697/insight-mechanism-of-the-selective-lanosterol-synthase-inhibitor-molecular-modeling-docking-and-density-functional-theory-approaches
#20
Suramanian Karunagaran, Chandrasekaran Meganathan, Rengarajan Kavitha, Muthu Vadivelu, Kuen Woo Lee
BACKGROUND: Lanosterol synthase (Oxidosqualene cyclase) is an enzyme, plays a central role in cholesterol and sterols biosynthesis. Lanosterol synthase drugs used to lower the level of cholesterol in the blood and treat wide variety of diseases like atherosclerosis, coronary heart diseases etc. OBJECTIVE: There is a great interest in the identification of drugs that target this enzyme for anticholesteraemic agent using insilico tools. METHODS: Ligand based pharmacophore model was developed using Discovery Studio 2...
April 26, 2017: Current Computer-aided Drug Design
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