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Qamar Uddin Ahmed, Murni Nazira Sarian, Siti Zaiton Mat So'ad, Jalifah Latip, Solachuddin Jauhari Arief Ichwan, Nurlaili Najmie Hussein, Muhammad Taher, Alhassan Muhammad Alhassan, Hanisuhana Hamidon, Sharida Fakurazi
Flavonoids have been reported to exert antihyperglycemic effects and have potential to enhance the current therapy options against type 2 diabetes mellitus. However, the structure activity relationships (SAR) studies of flavonoids against this disease have not been thoroughly comprehended. Hence, in the present study, 14 structurally related flavonoids viz. wogonin, techtochrysin, norwogonin, isoscutellarein, hypolaetin, kaempferol, quercetin, methyl ether of wogonin, acetate of wogonin, acetate of norwogonin, 8-hydroxy-7-methoxyflavone, chrysin, (+)-catechin and (-)-epicatechin were taken into account for in vitro antidiabetic evaluation...
November 15, 2018: Biomolecules
Sailen Barik
The dual-family peptidylprolyl cis-trans isomerases (immunophilins) represent a naturally occurring chimera of the classical FK506-binding protein (FKBP) and cyclophilin (CYN), connected by a flexible linker. They are found exclusively in monocellular organisms. The modular builds of these molecules represent two distinct types: CYN-(linker)-FKBP and FKBP-3TPR (tetratricopeptide repeat)-CYN. Abbreviated respectively as CFBP and FCBP, the two classes also exhibit distinct organism preference, the CFBP being found in prokaryotes, and the FCBP in eukaryotes...
November 15, 2018: Biomolecules
Maliha Zahid, Kyle S Feldman, Gabriel Garcia-Borrero, Timothy N Feinstein, Nicholas Pogodzinski, Xinxiu Xu, Raymond Yurko, Michael Czachowski, Yijen L Wu, Neale S Mason, Cecilia W Lo
Our previous work identified a 12-amino acid peptide that targets the heart, termed cardiac targeting peptide (CTP). We now quantitatively assess the bio-distribution of CTP, show a clinical application with the imaging of the murine heart, and study its mechanisms of transduction. Bio-distribution studies of cyanine5.5- N -Hydroxysuccinimide (Cy5.5) labeled CTP were undertaken in wild-type mice. Cardiac targeting peptide was labeled with Technetium 99m (99m Tc) using the chelator hydrazino-nicotinamide (HYNIC), and imaging performed using micro-single photon emission computerized tomography/computerized tomography (SPECT/CT)...
November 14, 2018: Biomolecules
Hyun-Ju Hwang, Jin-Woo Han, Hancheol Jeon, Jong Won Han
Lectin is an important protein in medical and pharmacological applications. Impurities in lectin derived from natural sources and the generation of inactive proteins by recombinant technology are major obstacles for the use of lectins. Expressing recombinant lectin with a tandem repeat structure can potentially overcome these problems, but few studies have systematically examined this possibility. This was investigated in the present study using three distinct forms of recombinant mannose-binding lectin from Bryopsis plumosa (BPL2)-i...
November 14, 2018: Biomolecules
Qishun Zhou, Bao Tram Vu Ngoc, Grazyna Leszczynska, Jean-Luc Stigliani, Geneviève Pratviel
Oxidative RNA damage is linked to cell dysfunction and diseases. The present work focuses on the in vitro oxidation of 5-methylaminomethyl uridine (mnm⁵U), which belongs to the numerous post-transcriptional modifications that are found in tRNA. The reaction of oxone with mnm⁵U in water at pH 7.5 leads to two aldonitrone derivatives. They form by two oxidation steps and one dehydration step. Therefore, the potential oxidation products of mnm⁵U in vivo may not be only aldonitrones, but also hydroxylamine and imine derivatives (which may be chemically more reactive)...
November 14, 2018: Biomolecules
Meraj A Khan, Cecil Pace-Asciak, Jassim M Al-Hassan, Mohammad Afzal, Yuan Fang Liu, Sosamma Oommen, Bincy M Paul, Divya Nair, Nades Palaniyar
Various biomolecules induce neutrophil extracellular trap (NET) formation or NETosis. However, the effect of fatty acids on NETosis has not been clearly established. In this study, we focused on the NETosis-inducing ability of several lipid molecules. We extracted the lipid molecules present in Arabian Gulf catfish ( Arius bilineatus , Val) skin gel, which has multiple therapeutic activities. Gas chromatography⁻mass spectrometry (GC-MS) analysis of the lipid fraction-3 from the gel with NETosis-inducing activity contained fatty acids including a furanoid F-acid (F6; 12,15-epoxy-13,14-dimethyleicosa-12,14-dienoic acid) and common long-chain fatty acids such as palmitic acid (PA; C16:0), palmitoleic acid (PO; C16:1), stearic acid (SA; C18:0), and oleic acid (OA; C18:1)...
November 13, 2018: Biomolecules
Karolina Mitusińska, Tomasz Magdziarz, Maria Bzówka, Agnieszka Stańczak, Artur Gora
Several different approaches are used to describe the role of protein compartments and residues in catalysis and to identify key residues suitable for the modification of the activity or selectivity of the desired enzyme. In our research, we applied a combination of molecular dynamics simulations and a water tracking approach to describe the water accessible volume of Solanum tuberosum epoxide hydrolase. Using water as a molecular probe, we were able to identify small cavities linked with the active site: (i) one made up of conserved amino acids and indispensable for the proper positioning of catalytic water and (ii) two others in which modification can potentially contribute to enzyme selectivity and activity...
November 12, 2018: Biomolecules
Seong Soo Moon, Hye Jin Lee, Ramya Mathiyalagan, Yu Jin Kim, Dong Uk Yang, Dae Young Lee, Jin Woo Min, Zuly Jimenez, Deok Chun Yang
Ginsenosides from Panax ginseng (Korean ginseng) are unique triterpenoidal saponins that are considered to be responsible for most of the pharmacological activities of P. ginseng . However, the various linkage positions cause different pharmacological activities. In this context, we aimed to synthesize new derivatives of ginsenosides with unusual linkages that show enhanced pharmacological activities. Novel α-glycosylated derivatives of ginsenoside F1 were synthesized from transglycosylation reactions of dextrin (sugar donor) and ginsenoside F1 (acceptor) by the successive actions of Toruzyme® 3...
November 10, 2018: Biomolecules
Stefania Costa, Irene Rugiero, Christian Larenas Uria, Paola Pedrini, Elena Tamburini
Valuable biomass conversion processes are highly dependent on the use of effective pretreatments for lignocellulose degradation and enzymes for saccharification. Among the nowadays available treatments, chemical delignification represents a promising alternative to physical-mechanical treatments. Banana is one of the most important fruit crops around the world. After harvesting, it generates large amounts of rachis, a lignocellulosic residue, that could be used for second generation ethanol production, via saccharification and fermentation...
November 9, 2018: Biomolecules
Sharonda J LeBlanc, Prakash Kulkarni, Keith R Weninger
Intrinsically disordered proteins (IDPs) are often modeled using ideas from polymer physics that suggest they smoothly explore all corners of configuration space. Experimental verification of this random, dynamic behavior is difficult as random fluctuations of IDPs cannot be synchronized across an ensemble. Single molecule fluorescence (or Förster) resonance energy transfer (smFRET) is one of the few approaches that are sensitive to transient populations of sub-states within molecular ensembles. In some implementations, smFRET has sufficient time resolution to resolve transitions in IDP behaviors...
November 8, 2018: Biomolecules
Cheng Chi, Sib Sankar Giri, Jin Woo Jun, Hyoun Joong Kim, Sang Wha Kim, Jeong Woo Kang, Se Chang Park
Palmitoleic acid (PA) is an effective algicide against Alexandrium tamarense . However, the toxicological mechanism of PA exposure is unclear. The transcript abundance and differentially expressed genes (DEGs) in gills of bay scallop were investigated following 80 mg/L PA exposure up to 48 h using the Illumina HiSeq 4000 deep-sequencing platform with the recommended read length of 100 bp. De novo assembly of paired-end reads yielded 62,099 unigenes; 5414 genes were identified as being significantly increased, and 4452 were decreased...
November 6, 2018: Biomolecules
Momen S A Abdelaty
Vanillin was used to synthesize a new derivative with an active aldehyde group and response to pH. It is named 2-((diethylamino) methyl)-4-formyl-6-methoxyphenyl acrylate, abbreviated to DEAMVA. The chemical structures were evaluated by ¹H, 13 C nuclear magnetic resonance (NMR), infrared (IR), and UV-Vis-spectroscopy, and all results demonstrated good statement. In order to achieve the dual responsive behavior thermo-pH with functionality, free radical polymerization of N -isopropylacrylamide with DEAMVA in different molar ratios (5, 10, 15 mol%) has been used, with azobisisobutyronitrile (AIBN) as the initiator...
November 6, 2018: Biomolecules
Ying-Jie Yang, Raghvendra Pratap Singh, Xin Lan, Cheng-Sheng Zhang, Yue-Zhong Li, Yi-Qiang Li, Duo-Hong Sheng
Myxococcus xanthus DK1622 is a rich source of novel secondary metabolites, and it is often used as an expression host of exogenous biosynthetic gene clusters. However, the frequency of obtaining large genome-deletion variants by using traditional strategies is low, and progenies generated by homologous recombination contain irregular deletions. The present study aims to develop an efficient genome-engineering system for this bacterium based on the Cre/loxP system. We first verified the functionality of the native cre system that was integrated into the chromosome with an inducible promoter P cuoA ...
November 6, 2018: Biomolecules
Levent Kilic, Abdulsamet Erden, Yusuf Ziya Sener, Berkan Armagan, Alper Sari, Umut Kalyoncu, Omer Karadag, Ali Akdogan, Ismail Dogan, Sule Apras Bilgen, Sedat Kiraz, Ihsan Ertenli
Secondary amyloid A (AA) amyloidosis is a late and serious complication of poorly controlled, chronic inflammatory diseases. Rheumatoid arthritis (RA) patients with poorly controlled, longstanding disease and those with extra-articular manifestations are under risk for the development of AA amyloidosis. Although new drugs have proven to be significantly effective in the treatment of secondary AA amyloidosis, no treatment modality has proven to be ideal. To date, only in small case series preliminary clinical improvement have been shown with rituximab therapy for AA amyloidosis secondary to RA that is refractory to TNF-α inhibitors (TNF-i) therapy...
November 5, 2018: Biomolecules
S Zulkafli Nor Effa, Nik Soriani Yaacob, Norazmi Mohd Nor
Immunomodulation, as a means of immunotherapy, has been studied in major research and clinical laboratories for many years. T-Regulatory (Treg) cell therapy is one of the modulators used in immunotherapy approaches. Similarly, nuclear receptor peroxisome proliferator activated receptor gamma (PPARγ) has extensively been shown to play a role as an immuno-modulator during inflammation. Given their mutual roles in downregulating the immune response, current study examined the influence of PPARγ ligands i.e., thiazolidinedione (TZD) class of drugs on Forkhead Box P3 (Foxp3) expression and possible crosstalk between PPARγ and nTreg cells of Non-Obese Diabetes (NOD) and Non-Obese Diabetes Resistant (NOR) mice...
November 5, 2018: Biomolecules
Diego A Bonilla Ocampo, Andrés F Paipilla, Estevan Marín, Salvador Vargas-Molina, Jorge L Petro, Alexandra Pérez-Idárraga
According to current therapeutic approaches, a nitrate-dietary supplementation with beetroot juice (BRJ) is postulated as a nutritional strategy that might help to control arterial blood pressure in healthy subjects, pre-hypertensive population, and even patients diagnosed and treated with drugs. In this sense, a systematic review of random clinical trials (RCTs) published from 2008 to 2018 from PubMed/MEDLINE, ScienceDirect, and manual searches was conducted to identify studies examining the relationship between BRJ and blood pressure...
November 2, 2018: Biomolecules
Karolina Weinmann, Jakob Werner, Wolfgang Koenig, Wolfgang Rottbauer, Daniel Walcher, Mirjam Keßler
BACKGROUND: Immunoadsorption and intravenous immunoglobulin (IVIG) administration may have beneficial effects in patients with dilated cardiomyopathy with end-stage heart failure. We investigated the effect of immunoadsorption with subsequent IVIG administration on cardiac function and symptoms in patients on optimal medical treatment (OMT) for heart failure (HF) with recent-onset cardiomyopathy during long-term follow-up. METHODS: Thirty-five patients with recent-onset of HF symptoms received intensive guideline-recommended medical HF therapy for 5...
November 2, 2018: Biomolecules
Alina E Perrone, Natalia Milduberger, Alicia G Fuchs, Patricia L Bustos, Jacqueline Bua
Trypanosoma cruzi is the etiological agent of Chagas disease. It affects eight million people worldwide and can be spread by several routes, such as vectorborne transmission in endemic areas and congenitally, and is also important in non-endemic regions such as the United States and Europe due to migration from Latin America. Cyclophilins (CyPs) are proteins with enzymatic peptidyl-prolyl isomerase activity (PPIase), essential for protein folding in vivo. Cyclosporin A (CsA) has a high binding affinity for CyPs and inhibits their PPIase activity...
October 31, 2018: Biomolecules
Esben Jannik Bjerrum, Boris Sattarov
Chemical autoencoders are attractive models as they combine chemical space navigation with possibilities for de novo molecule generation in areas of interest. This enables them to produce focused chemical libraries around a single lead compound for employment early in a drug discovery project. Here, it is shown that the choice of chemical representation, such as strings from the simplified molecular-input line-entry system (SMILES), has a large influence on the properties of the latent space. It is further explored to what extent translating between different chemical representations influences the latent space similarity to the SMILES strings or circular fingerprints...
October 30, 2018: Biomolecules
Celia F Rodrigues, Diana Vilas Boas, Ken Haynes, Mariana Henriques
Candida glabrata biofilms are recognized to have high resistance to antifungals. In order to understand the effect of mannans in the resistance profile of C. glabrata mature biofilms, C. glabrata Δ mnn2 was evaluated. Biofilm cell walls were analysed by confocal laser scanning microscopy (CLSM) and their susceptibility was assessed for fluconazole, amphotericin B, caspofungin, and micafungin. Crystal violet and Alcian Blue methods were performed to quantify the biomass and the mannans concentration in the biofilm cells and matrices, respectively...
October 30, 2018: Biomolecules
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