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https://www.readbyqxmd.com/read/28441731/polyphenolic-compounds-and-digestive-enzymes-in-vitro-non-covalent-interactions
#1
REVIEW
Alejandra I Martinez-Gonzalez, Ángel G Díaz-Sánchez, Laura A de la Rosa, Claudia L Vargas-Requena, Ismael Bustos-Jaimes, And Emilio Alvarez-Parrilla
The digestive enzymes-polyphenolic compounds (PCs) interactions behind the inhibition of these enzymes have not been completely studied. The existing studies have mainly analyzed polyphenolic extracts and reported inhibition percentages of catalytic activities determined by UV-Vis spectroscopy techniques. Recently, pure PCs and new methods such as isothermal titration calorimetry and circular dichroism have been applied to describe these interactions. The present review focuses on PCs structural characteristics behind the inhibition of digestive enzymes, and progress of the used methods...
April 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28441657/involvement-of-the-multidrug-and-toxic-compound-extrusion-transporter-in-testosterone-release-from-cultured-pig-leydig-cells
#2
Mitsuhiro Goda, Kana Oda, Atsuko Oda, Naoki Kobayashi, Masato Otsuka
Testosterone is considered to be released from Leydig cells via passive diffusion because of its hydrophobicity; however, the exact mechanism underlying testosterone secretion and the transporter involved are both unknown. Multidrug and toxic compound extrusion (MATE) transporters are predominantly found in the kidneys and liver and are thought to function in the elimination of metabolic organic cations during the final step of excretion in the kidney. In contrast, mMATE2 has been shown to be predominantly expressed in testicular Leydig cells...
April 26, 2017: Pharmacology
https://www.readbyqxmd.com/read/28441580/the-computer-aided-discovery-of-novel-family-of-the-5-ht6-serotonin-receptor-ligands-among-derivatives-of-4-benzyl-1-3-5-triazine
#3
Dorota Łażewska, Rafał Kurczab, Małgorzata Więcek, Katarzyna Kamińska, Grzegorz Satała, Magdalena Jastrzębska-Więsek, Anna Partyka, Andrzej J Bojarski, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
The work describes a discovery of new chemical family of potent ligands for the 5-HT6 serotonin receptors. During the search for new histamine H4 receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, weakly active for the H4 receptor but fitted in 3/4 of pharmacophore features of the 5-HT6R ligand, occurred to be a moderate 5-HT6R agent, useful as a lead structure for further modifications. A series of new derivatives (3-19) of the lead 2 was synthesized, evaluated in the radioligand binding assay (RBA) and explored in comprehensive molecular modelling, including both pharmacophore- and structure-based approaches with docking to the homology model of 5-HT6R...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28441541/molecular-interaction-of-2-4-diacetylphloroglucinol-dapg-with-human-serum-albumin-hsa-the-spectroscopic-calorimetric-and-computational-investigation
#4
Pragna Lakshmi T, Moumita Mondal, Krishna Ramadas, Sakthivel Natarajan
Drug molecule interaction with human serum albumin (HSA) affects the distribution and elimination of the drug. The compound, 2,4-diacetylphloroglucinol (DAPG) has been known for its antimicrobial, antiviral, antihelminthic and anticancer properties. However, its interaction with HSA is not yet reported. In this study, the interaction between HSA and DAPG was investigated through steady-state fluorescence, time-resolved fluorescence (TRF), circular dichroism (CD), Fourier transform infrared (FT-IR) spectroscopy, isothermal titration calorimetry (ITC), molecular docking and molecular dynamics simulation (MDS)...
April 18, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28441473/assembly-of-macrocycle-dye-derivatives-into-particles-for-fluorescence-and-photoacoustic-applications
#5
Hoang Dung Lu, Tristan L Lim, Shoshana Javitt, Andrew Heinmiller, Robert K Prud'homme
Optical imaging is a rapidly progressing medical technique that can benefit from the development of new and improved optical imaging agents suitable for use in vivo. However, the molecular rules detailing what optical agents can be processed and encapsulated into in vivo presentable forms are not known. We here present the screening of series of highly hydrophobic porphyrin, phthalocyanine, and naphthalocyanine dye macrocycles through a self-assembling Flash NanoPrecipitation process to form a series of water dispersible dye nanoparticles (NPs)...
April 25, 2017: ACS Combinatorial Science
https://www.readbyqxmd.com/read/28441360/erythromycin-modification-that-improves-its-acidic-stability-while-optimizing-it-for-local-drug-delivery
#6
Erika L Cyphert, Jaqueline D Wallat, Jonathan K Pokorski, Horst A von Recum
The antibiotic erythromycin has limited efficacy and bioavailability due to its instability and conversion under acidic conditions via an intramolecular dehydration reaction. To improve the stability of erythromycin, several analogs have been developed-such as azithromycin and clarithromycin-which decrease the rate of intramolecular dehydration. We set out to build upon this prior work by developing a conjugate of erythromycin with improved pH stability, bioavailability, and preferential release from a drug delivery system directly at the low pH of an infection site...
April 25, 2017: Antibiotics
https://www.readbyqxmd.com/read/28441023/hydrophobic-nanoparticles-modify-the-thermal-release-behavior-of-liposomes
#7
Matthew Ryan Preiss, Ashley E Hart, Christopher L Kitchens, Geoffrey D Bothun
Understanding the effect of embedded nanoparticles on the characteristics and behavior of lipid bilayers is critical to the development of lipid-nanoparticle assemblies (LNAs) for biomedical applications. In this work we investigate the effect of hydrophobic nanoparticle size and concentration on liposomal thermal release behavior. Decorated LNAs (D-LNAs) were formed by embedding 2 nm (GNP2) and 4 nm (GNP4) dodecanethiol-capped gold nanoparticles into DPPC liposomes at lipid to nanoparticle ratios (L:N) of 25,000:1, 10,000:1, and 5,000:1...
April 25, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28441012/rgb-switchable-porous-electrospun-nanofiber-chemoprobe-filter-prepared-from-multifunctional-copolymers-for-versatile-sensing-of-ph-and-heavy-metals
#8
Fang-Cheng Liang, Chi Ching Kuo, Bo-Yu Chen, Chia-Jung Cho, Chih-Chien Hung, Wen-Chang Chen, Redouane Borsali
Novel red-green-blue (RGB) switchable probes based on fluorescent porous electrospun (ES) nanofibers exhibiting high sensitivity to pH and mercury ions (Hg2+) were prepared with one type of copolymer (poly(methyl methacrylatete-co-1, 8-naphthalimide derivatives-co-rhodamine derivative); poly(MMA-co-BNPTU-co-RhBAM)) by using a single-capillary spinneret. The MMA, BNPTU, and RhBAM moieties were designed to (i) permit formation of porous fibers, (ii) fluoresce for Hg2+ detection, and (iii) fluoresce for pH, respectively...
April 25, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28441004/insights-into-the-mechanisms-by-which-clostridial-neurotoxins-discriminate-between-gangliosides
#9
Joshua R Burns, Gregory S Lambert, Michael R Baldwin
Botulinum neurotoxins (BoNTs) and Tetanus neurotoxin (TeNT) are the causative agents of the paralytic diseases botulism and tetanus, respectively. Entry of toxins into neurons is mediated through initial interactions with gangliosides, followed by binding to a protein co-receptor. Herein we aimed to understand the mechanism through which individual neurotoxins recognize the carbohydrate motif of gangliosides. Using cell-based and in vitro binding assays, in conjunction with structure-driven site directed mutagenesis, a conserved hydrophobic residue within the BoNTs that contributes to both affinity and specificity towards Sia5-containing gangliosides was identified...
April 25, 2017: Biochemistry
https://www.readbyqxmd.com/read/28440962/designed-heme-cage-%C3%AE-sheet-miniproteins
#10
Areetha D'Souza, Xiangyang Wu, Edwin Kok Lee Yeow, Surajit Bhattacharjya
The structure and function of naturally occurring proteins are governed by a large number of amino acids (≥100). The design of miniature proteins with desired structures and functions not only substantiates our knowledge about proteins but can also contribute to the development of novel applications. Excellent progress has been made towards the design of helical proteins with diverse functions. However, the development of functional β-sheet proteins remains challenging. Herein, we describe the construction and characterization of four-stranded β-sheet miniproteins made up of about 19 amino acids that bind heme inside a hydrophobic binding pocket or "heme cage" by bis-histidine coordination in an aqueous environment...
April 25, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28440951/concluding-the-trilogy-the-interaction-of-2-2-dihydroxy-benzophenones-and-their-carbonyl-n-analogues-with-human-glutathione-transferase-m1-1-face-to-face-with-the-p1-1-and-a1-1-isoenzymes-involved-in-mdr
#11
Nikolaos D Georgakis, Dionisis A Karagiannopoulos, Trias N Thireou, Elias E Eliopoulos, Nikolaos E Labrou, Petros G Tsoungas, Michael N Koutsilieris, Yannis D Clonis
The conjugation of intracellular glutathione (GSH) with several electrophilic, predominantly hydrophobic, endogenous and xenobiotic compounds, such as chemotherapeutics and carcinogenics, agrochemicals and other drugs, is catalyzed by the multigene enzyme family of glutathione transferases (GSTs). The mammalian family of GSTs comprises three groups: cytosolic, mitochondrial and microsomal. Human cytosolic GSTs constitute the largest family, which is classified in seven distinct classes named Alpha (Α), Mu (M), Pi (P), Theta (T), Sigma (S), Zeta (Z) and Omega (O)...
April 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28440948/novel-reduction-sensitive-micellar-nanoparticles-assembled-from-rituximab-doxorubicin-conjugates-as-smart-and-intuitive-drug-delivery-systems-for-the-treatment-of-non-hodgkin-s-lymphoma
#12
Huabin Yin, Tong Meng, Ling Shu, Min Mao, Lei Zhou, Haiyan Chen, Dianwen Song
In this study, a novel reduction-sensitive drug delivery system, the Rituximab-Doxorubicin (RTX-DOX) micellar nanoparticle (RDMN), was specially designed for targeted delivery and release of DOX in Non-Hodgkin's Lymphoma (NHL) cells. The RDMN was fabricated by self-assembling of amphiphilic RTX-DOX conjugates (RDCs), which were synthesized by conjugating the hydrophilic Fab fragments of RTX (an anti-CD20 monoclonal antibody) and hydrophobic DOXs by a reduction-responsive linker, 3-(2-Pyridyldithio) propionyl hydrazide (PDPH)...
April 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28440943/microplastics-as-a-vector-of-hydrophobic-contaminants-importance-of-hydrophobic-additives
#13
Jung-Hwan Kwon, Sein Chang, Sang Hee Hong, Won Joon Shim
Despite a recent boom in research on the environmental fate, distribution, and harmful effects of chemical substances associated with marine plastic debris, no consensus has been reached on whether chemicals originating from microplastics cause serious environmental harm. For the risk assessment of chemical contaminants associated with microplastics, it would be useful to group organic chemicals into 2 categories: additives and nonadditives. Whereas plastic particles are not likely to be diffuse sources of chemicals that are not intentionally added to plastic products, continuous leaching of additives would result in higher concentrations, at least at a local scale...
May 2017: Integrated Environmental Assessment and Management
https://www.readbyqxmd.com/read/28440931/microplastics-as-vectors-for-environmental-contaminants-exploring-sorption-desorption-and-transfer-to-biota
#14
Nanna B Hartmann, Sinja Rist, Julia Bodin, Louise Hs Jensen, Stine N Schmidt, Philipp Mayer, Anders Meibom, Anders Baun
The occurrence and effects of microplastics (MPs) in the aquatic environment are receiving increasing attention. In addition to their possible direct adverse effects on biota, the potential role of MPs as vectors for hydrophobic organic chemicals (HOCs), compared to natural pathways, is a topic of much debate. It is evident, however, that temporal and spatial variations of MP occurrence do (and will) occur. To further improve the estimations of the role of MPs as vectors for HOC transfer into biota under varying MP concentrations and environmental conditions, it is important to identify and understand the governing processes...
May 2017: Integrated Environmental Assessment and Management
https://www.readbyqxmd.com/read/28440865/generation-of-wavy-structure-on-lipid-membrane-by-peripheral-proteins-a-linear-elastic-analysis
#15
Paritosh Mahata, Sovan Lal Das
We carry out a linear elastic analysis to study wavy structure generation on lipid membrane by peripheral membrane proteins. We model the lipid membrane as linearly elastic and anisotropic material. The hydrophobic insertion by proteins into the lipid membrane has been idealized as penetration of rigid rodlike inclusions into the membrane and the electrostatic interaction between protein and membrane has been modeled by a distributed surface traction acting on the membrane surface. With the proposed model we study curvature generation by several binding domains of peripheral membrane proteins containing BAR domains and amphipathic alpha-helices...
April 25, 2017: FEBS Letters
https://www.readbyqxmd.com/read/28440819/amphiphilic-carbon-dots-as-versatile-vectors-for-nucleic-acid-and-drug-delivery
#16
Hai-Jiao Wang, Xi He, Tian-Ying Luo, Ji Zhang, Yan-Hong Liu, Xiao-Qi Yu
Carbon dot (CD)-based multifunctional delivery systems have shown great potential in both drug/gene delivery and bio-imaging. In this work, we present a strategy to simply construct amphiphilic CDs (ACDs) by conjugating hydrophobic alkyl epoxide to the surface amino groups of PEI 600-derived CDs. ACDs could well dissolve in water or organic solvents and emit bright fluorescence both in solutions and cells. (1)HNMR also suggested that ACDs may form micelle-like structures in water, and their CMC could be determined...
April 25, 2017: Nanoscale
https://www.readbyqxmd.com/read/28440650/comprehensive-computational-and-experimental-analysis-of-biomaterial-towards-the-behavior-of-imidazolium-based-ionic-liquids-an-interplay-between-hydrophilic-and-hydrophobic-interactions
#17
Reddicherla Umapathi, Suresh B Vepuri, Pannuru Venkatesu, Mahmoud E S Soliman
To provide insights into the aggregation behavior, hydration tendency and variation in phase transition temperature produced by the addition of ionic liquids (ILs) to poly(N-isopropylacrylamide) (PNIPAM) aqueous solution, systematic physicochemical studies, and molecular dynamic simulations were carried out. The influence of ILs possessing same [Cl]- anion and a set of cation [Cnmim]+ with increasing alkyl chain length such as 1-ethyl-3-methylimidazolium ([Emim]+), 1-allyl-3-methylimidazolium ([Amim]+), 1-butyl-3-methylimidazolium ([Bmim]+), 1-hexyl-3-methylimidazolium ([Hmim]+), 1-benzyl-3-methylimidazolium ([Bzmim]+), and 1- decyl-3-methylimidazolium ([Dmim] +) on the phase transition of PNIPAM was monitored by the aid of UV-visible absorption spectra, fluorescence intensity spectra, viscosity (ɳ), dynamic light scattering (DLS) and Fourier transform infrared (FTIR) spectroscopy...
April 25, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28440640/nucleic-acid-nanocapsules-for-enzyme-triggered-drug-release
#18
Joseph K Awino, Saketh Gudipati, Alyssa K Hartmann, Joshua J Santiana, Dominic F Cairns-Gibson, Nicole Gomez, Jessica L Rouge
Herein we describe a nucleic acid functionalized nanocapsule in which nucleic acid ligands are assembled and disassembled in the presence of enzymes. The particles are fully degradable in response to esterases due to an embedded ester cross-linker in the particle's core. During synthesis the nanocapsules can be loaded with hydrophobic small molecules and post self-assembly undergo covalent cross-linking using copper catalyzed click chemistry. They can then be functionalized with thiolated DNA through stepwise thiolyne chemistry using UV light irradiation...
April 25, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28440410/a-novel-notch3-mutation-identified-in-patients-with-oral-cancer-by-whole-exome-sequencing
#19
Yanjun Yi, Zhuowei Tian, Houyu Ju, Guoxin Ren, Jingzhou Hu
Oral cancer is a serious disease caused by environmental factors and/or susceptible genes. In the present study, in order to identify useful genetic biomarkers for cancer prediction and prevention, and for personalized treatment, we detected somatic mutations in 5 pairs of oral cancer tissues and blood samples using whole exome sequencing (WES). Finally, we confirmed a novel nonsense single-nucleotide polymorphism (SNP; chr19:15288426A>C) in the NOTCH3 gene with sanger sequencing, which resulted in a N1438T mutation in the protein sequence...
April 25, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28440205/in-vitro-collapsing-colon-cancer-cells-by-selectivity-of-disulfiram-loaded-charge-switchable-nanoparticles-against-cancer-stem-cells
#20
Marwa Muhammad Abu-Serie, Fatma Hassan El-Rashidy
BACKGROUND: Different strategies against colon cancer are accompanied by treatment failure, because of drug toxicity toward normal cells and cancer stem cells (CSCs) resistance. However, previous patent evaluated liposome that encapsulated inhibitor of CSCs' aldehyde dehydrogenase (ALDH)1; disulfiram, for targeting breast CSCs. Liposome has disadvantages due to its hydrophobicity. OBJECTIVES: Designing hydrophilic nanoparticles have selectivity to release disulfiram in CC cells rather than in normal colonocytes based on variation in microenvironment between normal and cancer cells...
April 24, 2017: Recent Patents on Anti-cancer Drug Discovery
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