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https://www.readbyqxmd.com/read/29324705/influence-of-chitosan-treatment-on-surrogate-serum-markers-of-cholesterol-metabolism-in-obese-subjects
#1
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
#2
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/K3PO4 system gave previously unknown ether derivatives (7a-f and 8a-f) in good yields. UV-visible, FTIR, and 1H 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
#3
Aldo Almeida, Lemeng Dong, Bekzod Khakimov, Jean-Etienne André Bassard, Tessa Moses, Frederic Lota, Alain Goossens, Giovanni Appendino, Soren 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 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 bethaminana...
December 4, 2017: 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
#4
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
#5
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)...
November 27, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/29187719/-small-animal-aspergillosis-and-cryptococcosis-in-japan
#6
Rui Kano
 Canine and feline upper respiratory tract (URT) infection due to Aspergillus spp. is considered an emerging disease, with the number of reported cases continuing to rise in Japan. Aspergillus fumigatus has been the most frequently reported etiologic agent of sino-orbital aspergillosis in dogs and cats; the other Aspergillus species, Aspergillus felis, Aspergillus fischeri, Aspergillus udagawae, Aspergillus viridinutans, and A. fumigatus, have also been implicated in feline cases. The minimum inhibitory concentrations (MICs) of antifungal drugs are elevated for these cryptic species compared with A...
2017: Medical Mycology Journal
https://www.readbyqxmd.com/read/29168743/synthesis-and-anticandidal-activity-evaluation-of-new-benzimidazole-thiazole-derivatives
#7
Zafer Asım Kaplancıklı, Serkan Levent, Derya Osmaniye, Begüm Nurpelin Sağlık, Ulviye Acar Çevik, Betül Kaya Çavuşoğlu, Yusuf Özkay, Sinem Ilgın
Azole-based antifungal agents constitute one of the important classes of antifungal drugs. Hence, in the present work, 12 new benzimidazole-thiazole derivatives 3a-3l were synthesized to evaluate their anticandidal activity against C.albicans, C.glabrata, C.krusei, and C.parapsilopsis. The structures of the newly synthesized compounds 3a-3l were confirmed by IR, ¹H-NMR, (13)C-NMR, and ESI-MS spectroscopic methods. ADME parameters of synthesized compounds 3a-3l were predicted by an in-slico study and it was determined that all synthesized compounds may have a good pharmacokinetic profile...
November 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29162893/intrinsic-short-tailed-azole-resistance-in-mucormycetes-is-due-to-an-evolutionary-conserved-aminoacid-substitution-of-the-lanosterol-14%C3%AE-demethylase
#8
Rita Caramalho, Joel D A Tyndall, Brian C Monk, Thomas Larentis, Cornelia Lass-Flörl, Michaela Lackner
Mucormycoses are emerging and potentially lethal infections. An increase of breakthrough infections has been found in cohorts receiving short-tailed azoles prophylaxis (e.g. voriconazole (VCZ)). Although VCZ is ineffective in vitro and in vivo, long-tailed triazoles such as posaconazole remain active against mucormycetes. Our goal was to validate the molecular mechanism of resistance to short-tailed triazoles in Mucorales. The paralogous cytochrome P450 genes (CYP51 F1 and CYP51 F5) of Rhizopus arrhizus, Rhizopus microsporus, and Mucor circinelloides were amplified and sequenced...
November 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29158527/azole-sensitivity-in-leptosphaeria-pathogens-of-oilseed-rape-the-role-of-lanosterol-14%C3%AE-demethylase
#9
Thomas R Sewell, Nichola J Hawkins, Henrik U Stotz, YongJu Huang, Steven L Kelly, Diane E Kelly, Bart Fraaije, Bruce D L Fitt
Lanosterol 14-α demethylase is a key enzyme intermediating the biosynthesis of ergosterol in fungi, and the target of azole fungicides. Studies have suggested that Leptosphaeria maculans and L. biglobosa, the causal agents of phoma stem canker on oilseed rape, differ in their sensitivity to some azoles, which could be driving pathogen frequency change in crops. Here we used CYP51 protein modelling and heterologous expression to determine whether there are interspecific differences at the target-site level...
November 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29156575/synthesis-of-oxadiazole-thiadiazole-hybrids-and-their-anticandidal-activity
#10
Serkan Levent, Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Derya Osmaniye, Ulviye Acar Çevik, Özlem Atlı, Yusuf Özkay, Zafer Asım Kaplancıklı
In the field of infection management, it is a major challenge to discover a potent and safe antifungal agent due to the emergence of resistant strains. Hence, the goal of this paper is to design and synthesize novel oxadiazole-thiadiazole hybrid compounds (6a-6s) and evaluate their antifungal activity. The structures of synthesized compounds were elucidated by various methods including FT-IR, ¹H-NMR, (13)C-NMR and HR-MS spectral data. Compounds were tested against four Candida species by broth microdilution assay...
November 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29142437/docking-based-screening-of-ficus-religiosa-phytochemicals-as-inhibitors-of-human-histamine-h2-receptor
#11
Amit Chaudhary, Birendra Singh Yadav, Swati Singh, Pramod Kumar Maurya, Alok Mishra, Shweta Srivastva, Pritish Kumar Varadwaj, Nand Kumar Singh, Ashutosh Mani
Background: Ficus religiosa L. is generally known as Peepal and belongs to family Moraceae. The tree is a source of many compounds having high medicinal value. In gastrointestinal tract, histamine H2 receptors have key role in histamine-stimulated gastric acid secretion. Their over stimulation causes its excessive production which is responsible for gastric ulcer. Objective: This study aims to screen the range of phytochemicals present in F. religiosa for binding with human histamine H2 and identify therapeutics for a gastric ulcer from the plant...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29115523/characterization-of-cholesterol-metabolism-in-sertoli-cells-and-spermatogenesis-review
#12
Jin-Feng Shi, Yu-Kun Li, Kun Ren, Yuan-Jie Xie, Wei-Dong Yin, Zhong-Cheng Mo
The Sertoli cell, which is the supporting cell of spermatogenesis, has an important role in the endocrine and paracrine control of spermatogenesis. Functionally, it provides the cells of the seminiferous epithelium with nutrition, conveys mature spermatids to the lumen of seminiferous tubules, secretes androgen‑binding protein and interacts with endocrine Leydig cells. In addition, the levels of cholesterol, as well as its intermediates, vary greatly between nongonadal tissues and the male reproductive system...
November 7, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29112162/syntheses-of-novel-4-substituted-n-5-amino-1h-1-2-4-triazol-3-yl-pyridine-3-sulfonamide-derivatives-with-potential-antifungal-activity
#13
Krzysztof Szafrański, Jarosław Sławiński, Anna Kędzia, Ewa Kwapisz
Candidiasis represent a serious threat for patients with altered immune responses. Therefore, we have undertaken the synthesis of compounds comprising a pyridine-3-sulfonamide scaffold and known antifungally active 1,2,4-triazole substituents. Thus a series of novel 4-substituted N-(5-amino-1H-1,2,4-triazol-3-yl)pyridine-3-sulfonamides have been synthesized by multistep reactions starting from 4-chloropyridine-3-sulfonamide via N'-cyano-N-[(4-substitutedpyridin-3-yl)sulfonyl]carbamimidothioates which were further converted with hydrazine hydrate to the corresponding 1,2,4-triazole derivatives 26-36...
November 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29108727/reproducibility-of-serum-oxysterols-and-lanosterol-among-postmenopausal-women-results-from-epic-heidelberg
#14
Da-Lin Lu, Disorn Sookthai, Charlotte Le Cornet, Verena A Katzke, Theron S Johnson, Rudolf Kaaks, Renée T Fortner
BACKGROUND: Circulating oxysterols have been proposed as biological markers of disease risk. However, within-person reproducibility of circulating oxysterols over time is not well established. METHODS: We evaluated the one-year reproducibility of 11 oxysterols and lanosterol among 30 postmenopausal women with repeat blood samples in the European Prospective Investigation into Cancer and Nutrition (EPIC) - Heidelberg, Germany cohort. Liquid chromatography-mass spectrometry (LC/MS) was performed to quantify serum concentrations of 22R-hydroxycholesterol, 2β-hydroxycholesterol, 24S-hydroxycholesterol, 27-hydroxycholesterol, 22S-hydroxycholeterol, 24,2β-epoxycholesterol, 5α,6β-dihydroxycholestanol, 7α-hydroxycholesterol, 5β,6β-epoxycholesterol, 5α,6α-epoxycholesterol, 24-dihydrolanosterol, and lanosterol...
November 3, 2017: Clinical Biochemistry
https://www.readbyqxmd.com/read/29096293/effects-of-the-bioconcentration-and-parental-transfer-of-environmentally-relevant-concentrations-of-difenoconazole-on-endocrine-disruption-in-zebrafish-danio-rerio
#15
Miaomiao Teng, Suzhen Qi, Wentao Zhu, Yao Wang, Dezhen Wang, Kai Dong, Chengju Wang
Difenoconazole, a typical triazole fungicide, inhibits lanosterol-14R-demethylase (CYP51) to prevent fungal sterol synthesis and its residues are frequently detected in the environment due to its wide application. Previous studies have demonstrated that difenoconazole altered the triglyceride levels, and gene expression relevant to cholesterol biosynthesis in zebrafish. However, endocrine-disruption in the hypothalamus-pituitary-gonadal-liver (HPGL) axis, the effects of transferring to offspring, and the underlying mechanisms of difenoconazole in aquatic organisms are still unknown...
October 26, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/29038279/a-ctg-clade-candida-yeast-genetically-engineered-for-the-genotype-phenotype-characterization-of-azole-antifungal-resistance-in-human-pathogenic-yeasts
#16
Isabelle Accoceberry, Amandine Rougeron, Nicolas Biteau, Pauline Chevrel, Valérie Fitton-Ouhabi, Thierry Noël
A strain of the opportunistic pathogenic yeast Candida lusitaniae was genetically modified for its use as a cellular model for assessing by allele replacement the impact of lanosterol C14α-demethylase ERG11 mutations on azole resistance. Candida lusitaniae was chosen because it is susceptible to azole antifungals, it belongs to the CTG clade of yeast which includes most of the Candida species pathogenic for humans, and it is haploid and easily amenable to genetic transformation and molecular modeling. In this work, allelic replacement is targeted at the ERG11 locus by the reconstitution of a functional auxotrophic marker in the 3' intergenic region of ERG11 Homologous and heterologous ERG11 alleles are expressed from the resident ERG11 promoter of C...
October 16, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29036583/characterization-of-moss-ent-kaurene-oxidase-cyp701b1-using-a-highly-purified-preparation
#17
Chisato Noguchi, Sho Miyazaki, Hiroshi Kawaide, Osamu Gotoh, Yuzo Yoshida, Yuri Aoyama
CYP701B1 of the moss, Physcomitrella patents, might be a unique cytochrome P450 having the ent-kaurene oxidase (KO) activity occurring in nonvascular plant. Phylogenetic analysis suggested that the gene encoding CYP701B1 was diverged from a common ancestral gene encoding KO of vascular plants. CYP701B1 expressed in Phichia yeast microsomes was purified and characterized. The purified CYP701B1 catalyzed the oxidation of ent-kaurene to ent-kaurenoic acid through three successive monooxygenations, and the rate-limiting step of this oxidation might be the initial step that forms ent-kaurenol...
September 27, 2017: Journal of Biochemistry
https://www.readbyqxmd.com/read/29016354/congenital-cataract-with-lss-gene-mutations-a-new-case-report
#18
Xiaodan Chen, Li Liu
BACKGROUND: Congenital cataract is one of the major causes of blindness and amblyopia in children. About one-third of the cases are inherited. CASE PRESENTATION: We applied whole exome sequencing for a pediatric patient with congenital cataract, small penis, baldness and absence of eyebrows and detected a compound heterozygous mutation in the lanosterol synthase (LSS) gene. These two mutations were inherited from the patient's parents. Both mutations altered the amino acid coding, at highly conserved amino acid residues...
October 26, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
https://www.readbyqxmd.com/read/28992260/simulations-of-cyp51a-from-aspergillus-fumigatus-in-a-model-bilayer-provide-insights-into-triazole-drug-resistance
#19
Anthony Nash, Johanna Rhodes
Azole antifungal drugs target CYP51A in Aspergillus fumigatus by binding with the active site of the protein, blocking ergosterol biosynthesis. Resistance to azole antifungal drugs is now common, with a leucine to histidine amino acid substitution at position 98 the most frequent, predominantly conferring resistance to itraconazole, although cross-resistance has been reported in conjunction with other mutations. In this study, we create a homology model of CYP51A using a recently published crystal structure of the paralog protein CYP51B...
September 9, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28989971/target-abundance-based-fitness-screening-tafis-facilitates-rapid-identification-of-target-specific-and-physiologically-active-chemical-probes
#20
Arielle Butts, Christian DeJarnette, Tracy L Peters, Josie E Parker, Morgan E Kerns, Karen E Eberle, Steve L Kelly, Glen E Palmer
Traditional approaches to drug discovery are frustratingly inefficient and have several key limitations that severely constrain our capacity to rapidly identify and develop novel experimental therapeutics. To address this, we have devised a second-generation target-based whole-cell screening assay based on the principles of competitive fitness, which can rapidly identify target-specific and physiologically active compounds. Briefly, strains expressing high, intermediate, and low levels of a preselected target protein are constructed, tagged with spectrally distinct fluorescent proteins (FPs), and pooled...
September 2017: MSphere
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