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https://www.readbyqxmd.com/read/29770459/identification-of-correlative-shifts-in-indices-of-brain-cholesterol-metabolism-in-the-c57bl6-mecp2-tm1-1bird-mouse-a-model-for-rett-syndrome
#1
Dieter Lütjohann, Adam M Lopez, Jen-Chieh Chuang, Anja Kerksiek, Stephen D Turley
Rett syndrome (RS) is a pervasive neurodevelopmental disorder resulting from loss-of-function mutations in the X-linked gene methyl-Cpg-binding protein 2 (MECP2). Using a well-defined model for RS, the C57BL6/Mecp2 tm1.1Bird mouse, we have previously found a moderate but persistently lower rate of cholesterol synthesis, measured in vivo, in the brains of Mecp2 -/y mice, starting from about the third week after birth. There was no genotypic difference in the total cholesterol concentration throughout the brain at any age...
May 17, 2018: Lipids
https://www.readbyqxmd.com/read/29766800/antifungal-activity-gas-chromatographic-mass-spectrometric-analysis-and-in-silico-study-of-punica-granatum-peel-extracts-against-fluconazole-resistant-strains-of-candida-species
#2
Sony Paul, M Kalyani, I Kannan
AIMS: Candida species is the common cause of opportunistic fungal infections all over the world with increased mortality and morbidity especially in immunosuppressed patients. Fluconazole is the first line therapy for candidiasis. The antifungal resistance pattern in high-risk patients is a major concern. The present study was aimed to assess the anticandidal activity of Punica granatum peel against fluconazole resistant Candida species isolated from HIV patients. MATERIALS & METHODS: Ethanol, chloroform, petroleum ether and aqueous extracts of the peel of P...
May 14, 2018: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29748145/design-synthesis-and-evaluation-of-benzoheterocycle-analogues-as-potent-antifungal-agents-targeting-cyp51
#3
Shizhen Zhao, Peng Wei, Mengya Wu, Xiangqian Zhang, Liyu Zhao, Xiaolin Jiang, Chenzhou Hao, Xin Su, Dongmei Zhao, Maosheng Cheng
To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compound 1, a series of benzoheterocycle analogues were designed, synthesized and evaluated for their in vitro antifungal activity. The most promising compounds 13s and 14a exhibited excellent antifungal activity against C. albicans, C. neoformans, A. fumigatus and fluconazole-resistant C. albicans strains, that was superior or comparable to those of the reference drugs fluconazole and voriconazole. GC-MS analyses suggested that the novel compound 13s might have a similar mechanism to fluconazole by inhibiting fungal lanosterol 14α-demethylase (CYP51)...
April 27, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29734526/synthesis-of-lanostane-type-triterpenoid-n-glycosides-and-their-cytotoxicity-against-human-cancer-cell-lines
#4
Motohiko Ukiya, Teppei Hayakawa, Kouta Okazaki, Maiko Hikawa, Hiroyuki Akazawa, Wei Li, Kazuo Koike, Makoto Fukatsu
Seventeen lanostane-type triterpenoid derivatives (2-18), including 11 N-glycosides (8-18), were synthesized from the natural triterpenoid, lanosterol (1), and were evaluated for their cytotoxicity against the human cancer cell lines, HL-60, A549, and MKN45, as well as the normal human lung cells, WI-38. Among them, N-β-d-2-acetamido-2-deoxyglucoside (10) showed cytotoxicity against HL-60, A549, MKN45, and WI-38 cells (IC50 0.0078-2.8 μm). However, N-β-d-galactoside (12) showed cytotoxicity against HL-60 and MKN45 cells (IC50 0...
May 7, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29617329/synthesis-and-anticandidal-activity-of-new-imidazole-chalcones
#5
Derya Osmaniye, Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Serkan Levent, Ulviye Acar Çevik, Özlem Atlı, Yusuf Özkay, Zafer Asım Kaplancıklı
In the present work, 15 new 1-(4-(1 H -imidazol-1-yl)phenyl)-3-(4-substituedphenyl)prop-2-en-1-one derivatives ( 3a – 3o ) were synthesized to evaluate their antifungal activity. Structures of newly synthesized imidazole derivatives ( 3a – 3o ) were characterized by IR, ¹H-NMR,13 C-NMR, and LCMSMS spectroscopic methods. The anticandidal activity of compounds ( 3a – 3o ) against C. albicans (ATCC 24433), C. krusei (ATCC 6258), C. parapsilosis (ATCC 22019), and C. glabrata (ATCC 90030) was elucidated according to the EUCAST definitive (EDef 7...
April 4, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29574072/recovery-of-lipid-metabolic-alterations-in-hepatitis-c-patients-after-viral-clearance-incomplete-restoration-with-accelerated-%C3%AF-oxidation
#6
Su-Wei Chang, Mei-Ling Cheng, Ming-Shi Shiao, Chau-Ting Yeh, Chao-Hung Wang, Chun-Ming Fan, Cheng-Tang Chiu, Ming-Ling Chang
BACKGROUND: How hepatitis C virus (HCV)-associated lipid metabolic alterations recover after sustained virological response (SVR) remains elusive. OBJECTIVE: The aforementioned recovery pattern was investigated. METHODS: In a prospective cohort study of 438 chronic hepatitis C (CHC) patients with SVR after anti-HCV therapy, 164 sex- and age-matched genotype I (G1) and G2 patients underwent paired-serum liquid chromatography-tandem mass spectrometry analyses before and 24 weeks after therapy...
March 2, 2018: Journal of Clinical Lipidology
https://www.readbyqxmd.com/read/29534874/a-phase-2-randomized-double-blind-placebo-controlled-dose-ranging-study-to-evaluate-the-efficacy-and-safety-of-orally-administered-vt-1161-in-the-treatment-of-recurrent-vulvovaginal-candidiasis
#7
Stephen R Brand, Thorsten P Degenhardt, Karen Person, Jack D Sobel, Paul Nyirjesy, Robert J Schotzinger, Amir Tavakkol
BACKGROUND: Lanosterol demethylase (CYP51), is an enzyme essential for fungal growth, and catalyzes an early step in the biosynthetic pathway of ergosterol, a sterol required for fungal cell membrane formation and integrity. CYP51 is the molecular target of the class of drugs referred to as 'azole antifungals.' VT-1161 is a novel, oral, selective inhibitor of fungal CYP51, and is being developed for the treatment of recurrent vulvovaginal candidiasis. OBJECTIVE: We evaluated the efficacy and safety of 4 dosing regimens of oral VT-1161 compared to placebo in women with recurrent vulvovaginal candidiasis, defined as at least 3 symptomatic episodes of acute vulvovaginal candidiasis within a 12-month period...
March 10, 2018: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/29522952/azoles-additively-inhibit-cytochrome-p450-1-erod-and-19-aromatase-in-rainbow-trout-oncorhynchus-mykiss
#8
Kristina Beijer, Maria Jönsson, Siraz Shaik, Daphné Behrens, Björn Brunström, Ingvar Brandt
Antifungal azoles are widely used in medicine, agriculture, and material protection and several antifungal azoles have been found in environmental samples. Although these compounds were designed to inhibit fungal enzymes such as lanosterol-14-demethylase (cytochrome P450 (CYP) 51), it is well established that the inhibitory actions of azoles are not specific for fungal CYP isozymes. We refined a gill filament assay to determine the inhibition of CYP1, measured as reduced 7-ethoxyresorufin-O-deethylase (EROD) activity, in rainbow trout (Oncorhynchus mykiss) gill tissue ex vivo...
May 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29518930/synthesis-molecular-docking-and-antimycotic-evaluation-of-some-3-acyl-imidazo-1-2-a-pyrimidines
#9
Omar Gómez-García, Dulce Andrade-Pavón, Elena Campos-Aldrete, Ricardo Ballinas-Indilí, Alfonso Méndez-Tenorio, Lourdes Villa-Tanaca, Cecilio Álvarez-Toledano
A series of 3-benzoyl imidazo[1,2- a ]pyrimidines, obtained from N -heteroarylformamidines in good yields, was tested in silico and in vitro for binding and inhibition of seven Candida species ( Candida albicans (ATCC 10231), Candida dubliniensis (CD36), Candida glabrata (CBS138), Candida guilliermondii (ATCC 6260), Candida kefyr , Candida krusei (ATCC 6358) and Candida tropicalis (MYA-3404)). To predict binding mode and energy, each compound was docked in the active site of the lanosterol 14α-demethylase enzyme (CYP51), essential for fungal growth of Candida species...
March 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29476632/biosynthesis-of-a-ganoderic-acid-in-saccharomyces-cerevisiae-by-expressing-a-cytochrome-p450-gene-from-ganoderma-lucidum
#10
Wen-Fang Wang, Han Xiao, Jian-Jiang Zhong
Ganoderic acid (GA), a triterpenoid from the traditional Chinese medicinal higher fungus Ganoderma lucidum, possesses antitumor and other significant pharmacological activities. Owing to the notorious difficulty and immaturity in genetic manipulation of higher fungi as well as their slow growth, biosynthesis of GAs in a heterologous host is an attractive alternative for their efficient bioproduction. In this study, using Saccharomyces cerevisiae as a host, we did a systematic screening of cytochrome P450 monooxygenase (CYP450) gene candidates from G...
February 24, 2018: Biotechnology and Bioengineering
https://www.readbyqxmd.com/read/29437525/3-5-disubstituted-thiazolidine-2-4-diones-design-microwave-assisted-synthesis-antifungal-activity-and-admet-screening
#11
Gabriel Marc, Anca Stana, Adrian Pîrnău, Laurian Vlase, Dan C Vodnar, Mihaela Duma, Brînduşa Tiperciuc, Ovidiu Oniga
A series of 12 new thiazolidine-2,4-dione derivatives were obtained by microwave-assisted synthesis. All compounds were physicochemically characterized by quantitative elemental C, H, N, S analysis and spectral data (mass spectrometry [MS], infrared [IR], and nuclear magnetic resonance [NMR]), with the results being in agreement with the expected data. An in vitro screening performed on Candida albicans ATCC 10231 showed their moderate antifungal activity, which was further investigated by determining the minimum inhibitory concentration and minimum fungicidal concentration values for the most active compounds on four strains of Candida...
February 1, 2018: SLAS Discovery
https://www.readbyqxmd.com/read/29433936/microrna-219-reduces-viral-load-and-pathologic-changes-in-theiler-s-virus-induced-demyelinating-disease
#12
Ana Lis Moyano, Jeffrey Steplowski, Haibo Wang, Kyung-No Son, Diana I Rapolti, Jeffrey Marshall, Vince Elackattu, Michael S Marshall, Amy K Hebert, Cory R Reiter, Viviana Ulloa, Katarzyna C Pituch, Maria I Givogri, Q Richard Lu, Howard L Lipton, Ernesto R Bongarzone
Analysis of microRNA (miR) expression in the central nervous system white matter of SJL mice infected with the BeAn strain of Theiler's murine encephalomyelitis virus (TMEV) revealed a significant reduction of miR-219, a critical regulator of myelin assembly and repair. Restoration of miR-219 expression by intranasal administration of a synthetic miR-219 mimic before disease onset ameliorates clinical disease, reduces neurogliosis, and partially recovers motor and sensorimotor function by negatively regulating proinflammatory cytokines and virus RNA replication...
March 7, 2018: Molecular Therapy: the Journal of the American Society of Gene Therapy
https://www.readbyqxmd.com/read/29421651/an-update-on-oxysterol-biochemistry-new-discoveries-in-lipidomics
#13
William J Griffiths, Yuqin Wang
Oxysterols are oxidised derivatives of cholesterol or its precursors post lanosterol. They are intermediates in the biosynthesis of bile acids, steroid hormones and 1,25-dihydroxyvitamin D3. Although often considered as metabolic intermediates there is a growing body of evidence that many oxysterols are bioactive and their absence or excess may be part of the cause of a disease phenotype. Using global lipidomics approaches oxysterols are underrepresented encouraging the development of targeted approaches. In this article, we discuss recent discoveries important in oxysterol biochemistry and some of the targeted lipidomic approaches used to make these discoveries...
February 5, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29379348/triterpenoid-modulates-the-salt-tolerance-of-lanosterol-synthase-deficient-saccharomyces-cerevisiae-gil77
#14
Masashi Inafuku, Mohammad Basyuni, Hirosuke Oku
This study examined the effect of triterpenoid on the salt tolerance of lanosterol synthase deficient yeast mutant GIL77. The expression of the triterpenoid synthase gene under GAL1 promoter in GIL77 increased the triterpenoid concentration of both whole cell and plasma membrane fractions. Without the induction of the genes, the growth curve of BgbAS or RsM1 transformant depicted patterns similar to control cells in both the presence and absence of salt with growth inhibition at 500 mM NaCl. The induction of BgbAS and RsM1 gene expression slightly repressed growth compared with control cells in the absence of NaCl...
January 2018: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/29363024/cloning-expression-purification-and-spectrophotometric-analysis-of-lanosterol-14-alpha-demethylase-from-leishmania-braziliensis-lbcyp51
#15
Humberto F Freitas, Acássia Benjamim Leal Pires, Marcelo S Castilho
Leishmaniasis, a neglected tropical disease, is a major cause of morbidity and mortality worldwide. Of the three main clinical forms, cutaneous leishmaniasis (CL) is the most common and 40 million people are at risk in the endemic areas. Currently, the available drugs to fight leishmaniasis have high toxicity and poor efficiency. Then, it is very important to search for effective and safe drugs that would target essential enzymes from the parasite, such as lanosterol 14-alpha demethylase (CYP51, EC 1.14.13...
April 2018: Molecular Biology Reports
https://www.readbyqxmd.com/read/29324705/influence-of-chitosan-treatment-on-surrogate-serum-markers-of-cholesterol-metabolism-in-obese-subjects
#16
Dieter Lütjohann, Milka Marinova, Karsten Wolter, Winfried Willinek, Norman Bitterlich, Martin Coenen, Christoph Coch, Frans Stellaard
Chitosan treatment results in significantly lower serum low density lipoprotein (LDL) cholesterol concentrations. To assess the working mechanisms of chitosan, we measured serum surrogate markers of cholesterol absorption (campesterol, sitosterol, cholestanol), synthesis (lathosterol, lanosterol, desmosterol), and degradation to bile acids (7α-hydroxy-cholesterol, 27-hydroxy-cholesterol), corrected for cholesterol concentration (R_sterols). Over 12 weeks, 116 obese subjects (Body Mass Index, BMI 31.7, range 28...
January 11, 2018: Nutrients
https://www.readbyqxmd.com/read/29238706/angular-phenozaxine-ethers-as-potent-multi-microbial-targets-inhibitors-design-synthesis-and-molecular-docking-studies
#17
Mercy A Ezeokonkwo, Onyinyechi N Ogbonna, Sunday N Okafor, Evelyn U Godwin-Nwakwasi, Fidelia N Ibeanu, Uchechukwu C Okoro
The reaction of diaza-5H-benzo[a]phenoxazin-5-one and 5H-benzo[a]phenoxazin-5-one with various phenols catalyzed by Pd/t-BuXPhos/K3 PO4 system gave previously unknown ether derivatives ( 7a-f and 8a-f ) in good yields. UV-visible, FTIR, and1 H NMR data were used to confirm structures of the synthesized compounds. The parent compounds and the derivatives were screened in-silico for their drug-likeness and binding affinities to the microbial targets through molecular docking. Molinspiration software and AutoDock were used for the drug-likeness and docking studies, respectively...
2017: Frontiers in Chemistry
https://www.readbyqxmd.com/read/29203557/a-single-oxidosqualene-cyclase-produces-the-seco-triterpenoid-%C3%AE-onocerin
#18
Aldo Almeida, Lemeng Dong, Bekzod Khakimov, Jean-Etienne Bassard, Tessa Moses, Frederic Lota, Alain Goossens, Giovanni Appendino, Søren Bak
8,14- seco -Triterpenoids are characterized by their unusual open C-ring. Their distribution in nature is rare and scattered in taxonomically unrelated plants. The 8,14- seco -triterpenoid α-onocerin is only known from the evolutionarily distant clubmoss genus Lycopodium and the leguminous genus Ononis , which makes the biosynthesis of this seco -triterpenoid intriguing from an evolutionary standpoint. In our experiments with Ononis spinosa, α-onocerin was detected only in the roots. Through transcriptome analysis of the roots, an oxidosqualene cyclase, OsONS1, was identified that produces α-onocerin from squalene-2,3;22,23-dioxide when transiently expressed in Nicotiana bethamiana In contrast, in Lycopodium clavatum , two sequential cyclases, LcLCC and LcLCD, are required to produce α-onocerin in the N...
February 2018: Plant Physiology
https://www.readbyqxmd.com/read/29199581/molecular-dynamics-and-virtual-screening-analysis-of-lanosterol-derivatives-from-ganoderma-medicinal-mushrooms-agaricomycetes-as-selective-ligands-of-human-androgen-receptor
#19
Abraham M Vidal-Limon, Oscar Daniel Luna-Martinez, Fausto Rojas-Durán, Thuluz Meza-Menchaca, Maria Elena Hernández-Aguilar, Angel Trigos, Jorge Suárez-Medellín
Male sex hormones such as testosterone and dihydrotestosterone play important roles in several physiological and pathological processes. The biological activities of the aforementioned metabolites are mediated by the multidomain androgen receptor (AR), which is therefore a well-studied drug target. Ganoderma mushroom lanostanoid extracts have previously been shown to exert antiandrogenic activity; therefore, this work aims to identify which lanostane derivatives might act as selective ligands for AR. Because protein flexibility is of paramount importance for ligand binding, different conformations of AR were sampled to account for binding modes within a ligand binding site, then subjected to virtual screening against a metabolite library...
2017: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/29190549/cholesterol-oversynthesis-markers-define-familial-combined-hyperlipidemia-versus-other-genetic-hypercholesterolemias-independently-of-body-weight
#20
Lucía Baila-Rueda, Ana Cenarro, Itziar Lamiquiz-Moneo, Sofía Perez-Calahorra, Ana M Bea, Victoria Marco-Benedí, Estíbaliz Jarauta, Rocío Mateo-Gallego, Fernando Civeira
Primary hypercholesterolemia of genetic origin, negative for mutations in LDLR, APOB, PCSK9 and APOE genes (non-FH GH), and familial combined hyperlipidemia (FCHL) are polygenic genetic diseases that occur with hypercholesterolemia, and both share a very high cardiovascular risk. In order to better characterize the metabolic abnormalities associated with these primary hypercholesterolemias, we used noncholesterol sterols, as markers of cholesterol metabolism, to determine their potential differences. Hepatic cholesterol synthesis markers (desmosterol and lanosterol) and intestinal cholesterol absorption markers (sitosterol and campesterol) were determined in non-FH GH (n=200), FCHL (n=100) and genetically defined heterozygous familial hypercholesterolemia subjects (FH) (n=100) and in normolipidemic controls (n=100)...
March 2018: Journal of Nutritional Biochemistry
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