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Daniel R Whiten, Dezerae Cox, Mathew H Horrocks, Christopher G Taylor, Suman De, Patrick Flagmeier, Laura Tosatto, Janet R Kumita, Heath Ecroyd, Christopher M Dobson, David Klenerman, Mark R Wilson
The aberrant aggregation of α-synuclein is associated with several human diseases, collectively termed the α-synucleinopathies, which includes Parkinson's disease. The progression of these diseases is, in part, mediated by extracellular α-synuclein oligomers that may exert effects through several mechanisms, including prion-like transfer, direct cytotoxicity, and pro-inflammatory actions. In this study, we show that two abundant extracellular chaperones, clusterin and α2 -macroglobulin, directly bind to exposed hydrophobic regions on the surface of α-synuclein oligomers...
June 19, 2018: Cell Reports
Anna Sola Rabada, Monika Michaelis, Daniel J Oliver, Martin Roe, Lucio Colombi Ciacchi, Hendrik Heinz, Carole C Perry
In this contribution, the effect of silica particle size (28 and 210 nm) and surface chemistry (i.e. hydroxyl, methyl or amino groups) on peptide binding response is studied with a specific emphasis on the effect of extent of functionalization on binding. Exhaustive characterization of the silica surfaces was crucial for knowledge of the chemistry and topography of the solid surface under study; and thus, to understand their impact on adsorption and the conformational ensemble of the peptides. The extent of surface functionalization was shown to be particle-size dependent, a higher level of 3-aminopropyl functionality being obtained for smaller particles, while a higher degree of methyl group functionality was found on the larger particles...
June 20, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
Alessio Ausili, Pablo Martinez Valera, Alejandro Torrecillas, Victoria Gómez-Murcia, Ana M deGodos, Senena Corbalan-Garcia, Jose Antonio Teruel, Juan C Gomez-Fernandez
Edelfosine is an anticancer drug with an asymmetric structure because, being a derivative of glycerol, it possesses two hydrophobic substituents of very different lengths. We showed that edelfosine destabilizes liquid ordered membranes formed by either POPC (1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine), SM (sphingomyelin) and cholesterol (1:1:1 molar ratio) or SM and cholesterol (2:1 molar ratio). This was observed by differential scanning calorimetry where a phase transition arises from either of these membrane systems after the addition of edelfosine...
June 20, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
Derek S Frank, Adam J Matzger
Amorphous solid dispersions containing a polymeric component often impart improved stability against crystallization for a small molecule relative to the pure amorphous form. However, the relationship between side chain functionalities on a polymer and the ability of a polymer to stabilize against crystallization is not well understood. To shed light on this relationship, a series of polymers were functionalized from a parent batch of poly(chloromethylstyrene- co-styrene) to investigate the effect of functionality on the stability in amorphous solid dispersions without altering the physical parameters of polymers, such as the average molecular weight or backbone chain chemistry...
June 20, 2018: Molecular Pharmaceutics
Tetsuya Hattori, Toru Itagaki, Hirotaka Uji, Shunsaku Kimura
Two kinds of amphiphilic polypeptides having different types of hydrophilic polypeptoids, poly(sarcosine)-b-(L-Leu-Aib)6 (ML12) and poly(N-ethyl glycine)-b-(L-Leu-Aib)6 (EL12), were self-assembled via two paths to phase-separated nanotubes. One path was via sticking ML12 nanotubes with EL12 nanotubes, and the other was a preparation from a mixture of ML12 and EL12 in solution. In either case, nanotubes showed temperature-induced phase separation along the long axis, which was observed by two methods of labeling one phase with gold nanoparticles and fluorescence resonance energy transfer between the components...
June 20, 2018: Journal of Physical Chemistry. B
Mohamed Khayet, Rong Wang
Electrospinning technique was used successfully to fabricate nanofibers of polysulfone (PSF) in which polytetrafuoroethylene nanoparticles (PTFE NPs) were embedded. The size of the PTFE NPs is only 1.7 to 3.6 times smaller than the nanofiber diameter. The transition from hydrophobic to superhydrophobic character of the bead-free PSF electrospun nanofiber mats occurred with a PTFE NPs loading in the range 12 - 18 % of the PSF weight. Transmission electron microscopy images revealed protruding nanosized asperities on the fiber surface due to the embedded PTFE NPs in the PSF matrix...
June 20, 2018: ACS Applied Materials & Interfaces
Min Zeng, Meng Huo, Yujun Feng, Jinying Yuan
ABC triblock copolymer assemblies with reversible "breathing" behaviors based on poly[oligo(ethylene glycol) methyl ether methacrylate]-b-poly(benzyl methacrylate)-b-poly[2-(diethylamino)ethyl methacrylate] (POEGMA-b-PBnMA-b-PDEA) are fabricated via one-pot sequential reverisble addition-fragmentation chain transfer dispersion polymerization. Using a POEGMA as the macromolecular chain transfer agent, chain extension with BnMA and DEA is conducted in ethanol, where PBnMA acts as the core-forming block, and the PDEA block endows the solvophilicity and CO2 -responsiveness...
June 20, 2018: Macromolecular Rapid Communications
Yun-Ho Jeong, Hyeon-Woo Shin, Ji-Yeong Kwon, Sang-Min Lee
Encapsulation of chemotherapeutic agents inside a nanoscale delivery platform can provide an attractive therapeutic strategy with many pharmaceutical benefits, such as increased plasma solubility, prolonged in vivo circulation, and reduced acute toxicity. Given that the biological activities of polymeric nanoparticles are highly dependent on their colloidal structures, the molecular geometry-regulated programming of self-assembled nanoscale architecture is of great interest for chemical design of an ideal delivery platform...
June 20, 2018: ACS Applied Materials & Interfaces
Xingxing Dai, Ran Wang, Zhimin Wu, Shujuan Guo, Chang Yang, Lina Ma, Liping Chen, Xinyuan Shi, Yanjiang Qiao
Borneol (BO) and menthol (MEN) are two widely used natural permeation enhancers in the transdermal drug delivery system. In previous studies, their permeation enhancement effects and mechanisms of action on the hydrophobic drug osthole (logP=3.8) and hydrophilic drug 5-fluorouracil (logP=-0.9) have been studied. In this study, ligustrazine (LTZ), whose logP is 1.3, was used as a model drug to provide a comprehensive understanding of the influence of its logP on the permeation-enhancing effects of BO and MEN...
June 20, 2018: Chemical Biology & Drug Design
Michael J Haider, Huixi Violet Zhang, Nairiti Sinha, Jeffrey A Fagan, Kristi L Kiick, Jeffery G Saven, Darrin J Pochan
Coiled-coil peptides have proven useful in a range of materials applications ranging from the formation of well-defined fibrils to responsive hydrogels. The ability to design from first principles their oligomerization and subsequent higher order assembly offers their expanded use in producing new materials. Toward these ends, homo-tetrameric, antiparallel, coiled-coil, peptide bundles have been designed computationally, synthesized via solid-phase methods, and their solution behavior characterized. Two different bundle-forming peptides were designed and examined...
June 20, 2018: Soft Matter
Paridhi Gulati, Shangang Jia, Aixia Li, David Richard Holding, Dipak Santra, Devin Jerrold Rose
Thirty-three accessions of proso millet (Panicum miliaceum) with different countries of origin were screened for their pepsin digestibility after cooking to identify samples with high digestibility. The pepsin digestibility of all samples ranged from 26 to 57% (average 32%). There were no apparent differences in protein profiles (SDS-PAGE) of samples with the lowest, intermediate, and highest digestibilities. However, LC-MS/MS analysis revealed a negative correlation between pepsin digestibility and peptides that matched to high molecular weight proteins (24 kDa) from Panicum hallii with regions of contiguous hydrophobic amino acids...
June 20, 2018: Journal of Agricultural and Food Chemistry
Cheng Jin, Hui Zhang, Jianmei Zou, Yan Liu, Lin Zhang, Fengjie Li, Ruowen Wang, Wenjing Xuan, Mao Ye, Weihong Tan
Automated attachment of chemotherapeutic drugs to oligonucleotides through phosphoramidite chemistry and DNA synthesis has emerged as a powerful technology in constructing structure-defined and payload-tunable oligonucleotide-drug conjugates. In practice, however, in vivo delivery of these oligonucleotides remains a challenge. Inspired by the systemic transport of hydrophobic payloads by serum albumin in nature, we report the development of a lipid-conjugated floxuridine homomeric oligonucleotide (LFU20) that "hitchhikes" with endogenous serum albumin for cancer chemotherapy...
June 19, 2018: Angewandte Chemie
Wenfei Xiong, Cong Ren, Jing Li, Bin Li
The objective of this study was to investigate the impact of encapsulating resveratrol in ovalbumin (OVA)-carboxymethylcellulose (CMC) nanocomplexes or nanoparticles on its photostability and bioaccessibility. The nanocomplexes were formed by the electrostatic assembly between OVA and CMC, and the nanoparticles were fabricated through further heating the nanocomplexes at 90 °C for 30 min. The nanocomplexes and nanoparticles both presented a spherical morphology, and the nanoparticles exhibited larger average particle sizes and net zeta potential...
June 20, 2018: Food & Function
Wolfgang Stremmel, Simone Staffer, Nicole Stuhrmann, Hongying Gan-Schreier, Annika Gauss, Nina Burger, Daniel Hornuss
Background: Attack by commensal microbiota is one component of induction of inflammatory episodes in ulcerative colitis (UC). In UC, the mucus layer is intrinsically devoid of phosphatidylcholine (PC) resulting in low hydrophobicity which facilitates bacterial invasion. Colonic ectophospholipase-carrying bacterial strains are likely candidates to further thinning the PC mucus barrier and to precipitate inflammatory episodes. Objective: To evaluate the effect of phospholipase A2 (PLA2 ) inhibitors on inflammation in a genetic UC mouse model...
March 2018: Inflammatory Intestinal Diseases
Mansour Sobeh, Mona F Mahmoud, Rehab A Hasan, Mohamed A O Abdelfattah, Omar M Sabry, Mosad A Ghareeb, Assem M El-Shazly, Michael Wink
The potential hepatoprotective activities of two Lannea species were explored in vivo. Furthermore, the binding activities of their main polyphenols to the antiapoptotic protein Bcl-2 were investigated. Based on HPLC-MS/MS results, 22 secondary metabolites were characterized in L. stuhlmannii (mainly tannins), while 20 secondary metabolites (mainly sulphated tannins) were identified in L. humilis. Both extracts exhibited substantial antioxidant activities in vitro and counteracted D-galactosamine induced intoxication in rats in vivo and increased the total antioxidant capacity (TAC) of liver tissues...
June 19, 2018: Scientific Reports
Jing Li, Chao Qiu, Haoran Fan, Yuxiang Bai, Zhengyu Jin, Jinpeng Wang
A novel cyclodextrin-functionalized hybrid silicon nano-adsorbent material (6-EA-β-CD-Si) was synthesized via the nucleophilic substitution method. The structure was detected by Fourier transform infrared (FT-IR), X-ray, thermogravimetric analysis, and Brunauer-Emmett-Teller (BET) analysis. Results reveal that the BET surface area of 6-EA-β-CD-Si is 240 m²/g and the average pore size is 4.16 nm. The adsorption properties of 6-EA-β-CD-Si onto methylene blue (MB) were studied and fitted with adsorption kinetic models...
June 19, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Li Feng, Shengtao Zhang, Yujie Qiang, Yue Xu, Lei Guo, Loutfy H Madkour, Shijin Chen
The anticorrosion effect of thiazolyl blue (MTT) for copper in 3% NaCl at 298 K was researched by electrochemical methods, scanning electron-microscopy (SEM), and atomic force microscopy (AFM). The results reveal that MTT can protect copper efficiently, with a maximum efficiency of 95.7%. The corrosion inhibition mechanism was investigated by X-ray photoelectron spectroscopy (XPS), Fourier transform infrared spectral (FT-IR), and theoretical calculation. The results suggest that the MTT molecules are adsorbed on metal surface forming a hydrophobic protective film to prevent copper corrosion...
June 19, 2018: Materials
Alessandra Romanelli, Concetta Avitabile, Luca Domenico D'Andrea, Elisabetta D'Aversa, Roberta Milani, Roberto Gambari
New peptides derived from the natural antimicrobial temporin B were obtained. The design, the antimicrobial activity as well as the characterization of the secondary structure of peptides in the presence of bacterial cells is here described. We identified TB_KKG6K (KKLLPIVKNLLKSLL) as the most active analogue against Gram-positive and Gram-negative bacteria as compared to natural temporin B (LLPIVGNLLKSLL) and TB_KKG6A (KKLLPIVANLLKSLL). Acylation with hydrophobic moieties led generally to reduced activity, however, acylation at position 6 of TB_KKG6K led to retained submicromolar activity against Staphylococcus epidermidis...
June 19, 2018: ChemMedChem
Rajan Patel, Neha Maurya, Mehraj Ud Din Parray, Nida Farooq, Abrar Siddique, Kanak Lata Verma, Neeraj Dohare
The present work is a brief overview of the effect of psychostimulant drug mephedrone hydrochloride (4MMC) on a transport protein, bovine serum albumin (BSA). The binding effect of 4MMC on BSA has been investigated by using UV-visible, steady-state fluorescence, time-resolved fluorescence, fluorescence resonance energy transfer, Fourier transform infrared, circular dichroism, and molecular docking method. 4-Methylmephedrone quenched the intrinsic fluorescence of BSA by static quenching mechanism, which was further confirmed by time-resolved fluorescence...
June 19, 2018: Journal of Molecular Recognition: JMR
Hao Wang, Xiaoli Zhao, Xuejiao Han, Zhi Tang, Fanhao Song, Shaoyang Zhang, Yuanrong Zhu, Wenjing Guo, Zhongqi He, Qingwei Guo, Fengchang Wu, Xiaoguang Meng, John P Giesy
Better understanding of the colloidal behaviors of nanomaterials impacted by aquatic chemistry parameters is needed for appropriate evaluation of the environmental risks posed by nanomaterials in natural waters. In the study, the colloidal stability of Fe3 O4 magnetic nanoparticles (Fe-MNPs) was evaluated over a range of chemistry characteristics [e.g., pH, dissolved organic matter (DOM), salt types, cationic strength] in six synthetic water samples. The findings from the synthetic water samples were further examined with eight "real world" environmental water samples...
June 14, 2018: Environmental Pollution
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