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https://www.readbyqxmd.com/read/28814780/adaptive-simulations-towards-interactive-protein-ligand-modeling
#1
Daniel Lecina, Joan F Gilabert, Victor Guallar
Modeling the dynamic nature of protein-ligand binding with atomistic simulations is one of the main challenges in computational biophysics, with important implications in the drug design process. Although in the past few years hardware and software advances have significantly revamped the use of molecular simulations, we still lack a fast and accurate ab initio description of the binding mechanism in complex systems, available only for up-to-date techniques and requiring several hours or days of heavy computation...
August 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28800465/oil-based-cyclo-oligosaccharide-nanodevices-for-drug-encapsulation
#2
Jennifer Noro, Ana Loureiro, Filipa Gonçalves, Nuno G Azoia, Seunho Jung, Carla Silva, Artur Cavaco-Paulo
New encapsulation nanodevices were synthesized by emulsification of cyclo-oligosaccharides fully substituted by hydrophobic palmitic chains. These highly hydrophobic compounds, acquire oily-like behaviour at moderate temperatures (∼50°C) and when submitted to ultrasound (US) can undergo emulsification. The improved emulsifying properties of modified cyclo-oligosaccharides are suitable to produce small and narrow sized nanoemulsions with ability to encapsulate amphiphilic molecules. Both encapsulation and delivery of a therapeutic drug, methotrexate (MTX), with amphiphilic character was assessed...
July 25, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28780322/reduction-of-oxidative-damages-induced-by-titanium-dioxide-nanoparticles-correlates-with-induction-of-the-nrf2-pathway-by-gspe-supplementation-in-mice
#3
Linpeng Niu, Mengjiao Shao, Yuan Liu, Jinfeng Hu, Ruofan Li, Heran Xie, Lixiao Zhou, Lei Shi, Rong Zhang, Yujie Niu
Titanium dioxide nanoparticles (TiO2 NPs) are widely used to additives in cosmetics, pharmaceuticals, paints and foods. Recent studies have demonstrated that TiO2 NPs increased the risk of cancer and the mechanism might relate with oxidative stress. Grape seed procyanidin extract (GSPE) is a natural compound which has been demonstrated to possess a wide array of pharmacological and biochemical actions, including anti-inflammatory, anti-carcinogenic, and antioxidant properties. Our data show that GSPE prevents the changes of histopathology and biomarkers in heart, liver and kidney that occur in mice exposed to TiO2 NPs...
August 2, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28764904/photosensitized-methyl-paraben-induces-apoptosis-via-caspase-dependent-pathway-under-ambient-uvb-exposure-in-human-skin-cells
#4
Divya Dubey, Deepti Chopra, Jyoti Singh, Ajeet K Srivastav, Smita Kumari, Ankit Verma, Ratan Singh Ray
Methyl paraben (MP), is a widely used preservative in pharmaceutical, food and cosmetic products. Its molecular mechanism under ambient ultraviolet radiation is not well understood. We investigated photosensitizing mechanism of MP under ambient UVB (0.6 mW/cm(2)) intensity. MP showed dose dependent decrease in cell viability of human keratinocyte cell line (HaCaT) by MTT and NRU assays. Study showed 40% reduction in antimicrobial activity of UVB irradiated MP through E. coli culture. Photosensitized MP (25 μg/ml) significantly enhanced lipid peroxidation, intracellular ROS generation and disrupted mitochondrial membrane integrity...
July 29, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28762740/in-situ-characterization-of-pharmaceutical-formulations-by-dynamic-nuclear-polarization-enhanced-mas-nmr
#5
Qing Zhe Ni, Fengyuan Yang, Thach V Can, Ivan V Sergeyev, Suzanne M D'Addio, Sudheer K Jawla, Yongjun Li, Maya P Lipert, Wei Xu, R Thomas Williamson, Anthony Leone, Robert G Griffin, Yongchao Su
A principal advantage of magic angle spinning (MAS) NMR spectroscopy lies in its ability to determine molecular structure in a noninvasive and quantitative manner. Accordingly, MAS should be widely applicable to studies of the structure of active pharmaceutical ingredients (API) and formulations. However, the low sensitivity encountered in spectroscopy of natural abundance APIs present at low concentration has limited the success of MAS experiments. Dynamic nuclear polarization (DNP) enhances NMR sensitivity and can be used to circumvent this problem provided that suitable paramagnetic polarizing agent can be incorporated into the system without altering the integrity of solid dosages...
August 17, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28758845/diloxanide-furoate-binary-complexes-with-%C3%AE-methyl-%C3%AE-and-hydroxypropyl-%C3%AE-cyclodextrins-inclusion-mode-characterization-in-solution-and-in-solid-state-and-in-vitro-dissolution-studies
#6
Carolina Aloisio, Marcela Longhi
The purpose of this study was to investigate the effect on solubility and dissolution rate of binary complexes of β-(βCD), methyl-(MβCD) and hydroxypropyl-β-cyclodextrin (HPβCD) with diloxanide furoate (DF). The complexation in solution was evaluated by phase solubility studies and (1)H nuclear magnetic resonance (NMR). Enhanced water solubility of DF was obtained with the DF:MβCD system (61-fold). The mode of inclusion was supported by NMR experiments, which indicated that real inclusion complexes were formed between DF and MβCD or HPβCD...
August 16, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28757565/the-pharmaceutical-device-prisma-%C3%A2-skin-promotes-in-vitro-angiogenesis-through-endothelial-to-mesenchymal-transition-during-skin-wound-healing
#7
Raffaella Belvedere, Valentina Bizzarro, Luca Parente, Francesco Petrella, Antonello Petrella
Glycosaminoglycans are polysaccharides of the extracellular matrix supporting skin wound closure. Mesoglycan is a mixture of glycosaminoglycans such as chondroitin-, dermatan-, heparan-sulfate and heparin and is the main component of Prisma(®) Skin, a pharmaceutical device developed by Mediolanum Farmaceutici S.p.a. Here, we show the in vitro effects of this device in the new vessels formation by endothelial cells, since angiogenesis represents a key moment in wound healing. We found a strong increase of migration and invasion rates of these cells treated with mesoglycan and Prisma(®) Skin which mediate the activation of the pathway triggered by CD44 receptor...
July 25, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28750313/imidazo-1-2-a-pyrazine-imidazo-1-5-a-quinoxaline-and%C3%A2-pyrazolo-1-5-a-quinoxaline-derivatives-as-ikk1-and-ikk2-inhibitors
#8
Cindy Patinote, Nour Bou Karroum, Georges Moarbess, Carine Deleuze-Masquefa, Kamel Hadj-Kaddour, Pierre Cuq, Mona Diab-Assaf, Issam Kassab, Pierre-Antoine Bonnet
The transcription nuclear factor NF-κB plays a pivotal role in chronic and acute inflammatory diseases. Among the several and diverse strategies for inhibiting NF-κB, one of the most effective approach considered by the pharmaceutical industry seems to be offered by the development of IKK inhibitors. In a former study, two potential IKK2 inhibitors have been highlighted among a series of imidazo[1,2-a]quinoxaline derivatives. In order to enhance this activity, we present herein the synthesis of twenty-one new compounds based on the imidazo[1,2-a]pyrazine, imidazo[1,5-a]quinoxaline or pyrazolo[1,5-a]quinoxaline structures...
July 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28736501/design-of-radioiodinated-pharmaceuticals-structural-features-affecting-metabolic-stability-towards-in-vivo-deiodination
#9
REVIEW
Lorenzo Cavina, Dion van der Born, Peter H M Klaren, Martin C Feiters, Otto C Boerman, Floris P J T Rutjes
Radioiodinated pharmaceuticals are convenient tracers for clinical and research investigations because of the relatively long half-lives of radioactive iodine isotopes (i.e., (123)I, (124)I, and (131)I) and the ease of their chemical insertion. Their application in radionuclide imaging and therapy may, however, be hampered by poor in vivo stability of the C-I bond. After an overview of the use of iodine in biology and nuclear medicine, we present here a survey of the catabolic pathways for iodinated xenobiotics, including their biodistribution, accumulation, and biostability...
June 30, 2017: European Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28735742/genotoxicity-of-gemfibrozil-in-the-gilthead-seabream-sparus-aurata
#10
A Barreto, L G Luis, A M V M Soares, P Paíga, L H M L M Santos, C Delerue-Matos, K Hylland, S Loureiro, M Oliveira
Widespread use of pharmaceuticals and suboptimal wastewater treatment have led to increased levels of these substances in aquatic ecosystems. Lipid-lowering drugs such as gemfibrozil, which are among the most abundant human pharmaceuticals in the environment, may have deleterious effects on aquatic organisms. We examined the genotoxicity of gemfibrozil in a fish species, the gilthead seabream (Sparus aurata), which is commercially important in southern Europe. Following 96-h waterborne exposure, molecular (erythrocyte DNA strand breaks) and cytogenetic (micronuclei and other nuclear abnormalities in cells) endpoints were measured...
September 2017: Mutation Research
https://www.readbyqxmd.com/read/28724165/cytogenotoxicity-of-inclusion-complexes-of-diazepam-with-2-hydroxypropyl-%C3%AE-cyclodextrin
#11
Jasmina Hadžiabdić, Nevenka Kopjar, Davor Želježić, Selma Špirtović-Halilović, Davorka Završnik
Background Diazepam, as one of the most frequent prescribed drug from 1,4-benzodiazepine group, has certain limitations in pharmaceutical technology due to its poor solubility in water. By forming inclusion complexes with 2-hydroxypropyl-β-cyclodextrin, diazepam's biopharmaceutical properties can be greatly improved. Aim Aim of this research was to in vitro evaluate genotoxicity of prepared novel complexes of diazepam and their influence on proliferation of human peripheral blood lymphocytes. Methods For identification of possible genotoxicity of diazepam inclusion complexes, cytokinesis-block micronucleus assay has been chosen...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28721737/a-new-water-soluble-nanomicelle-formed-through-self-assembly-of-pectin-curcumin-conjugates-preparation-characterization-and-anticancer-activity-evaluation
#12
Feng Bai, Jiajing Diao, Ying Wang, Shixin Sun, Hongmei Zhang, Yunyun Liu, Yanqing Wang, Jian Cao
Curcumin is a dominating active component of Curcuma longa and has been studied widely because of its prominent biological activities. The extremely low aqueous solubility, stability, and bioavailability of curcumin limit its application in the field of medicine. In this study, we developed pectin-curcumin (PEC-CCM) conjugates that could self-assemble water-soluble nanomicelles in aqueous solution. The structure of PEC-CCM conjugates was characterized by ultraviolet-visible spectra, fluorescence spectra, Fourier transform infrared spectroscopy, and (1)H nuclear magnetic resonance spectroscopy...
August 16, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28719814/enantiomeric-separation-of-seven-%C3%AE-agonists-by-nace-study-of-chiral-selectivity-with-diacetone-d-mannitol-boric-acid-complex
#13
Lili Lv, Lijuan Wang, Jun Li, Yajun Jiao, Shengnan Gao, Jiachang Wang, Hongyuan Yan
A rapid and effective nonaqueous capillary electrophoresis (NACE)-ultraviolet (UV) method was developed for the enantiomeric separation of seven β-agonists. Diacetone-d-mannitol-boric acid complex was used as a new chiral selector. It was in situ synthesized by the reaction of diacetone-d-mannitol and boric acid in methanol medium containing triethylamine. The effects of diacetone-d-mannitol, boric acid, and triethylamine concentrations on the enantioseparation were carefully investigated. Under the optimized conditions, baseline enantioseparation could be obtained for six of the tested β-agonists within 12min...
July 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28704687/antimicrobial-polyketide-furanoterpenoids-from-seaweed-associated-heterotrophic-bacterium-bacillus-subtilis-mtcc-10403
#14
Kajal Chakraborty, Bini Thilakan, Vamshi Krishna Raola
Brown seaweed Anthophycus longifolius (Turner) Kützing (family Sargassaceae) associated heterotrophic bacterium Bacillus subtilis MTCC 10403 was found to be a potent isolate with broad range of antibacterial activity against important perceptive food pathogens Vibrio parahaemolyticus, V. vulnificus, and Aeromonas hydrophila. This bacterium was positive for polyketide synthetase gene (KC589397), and therefore, was selected to bioprospect specialized metabolites bearing polyketide backbone. Bioactivity-guided chromatographic fractionation of the ethyl acetate extract of the seaweed-associated bacterium segregated four homologous polyketide furanoterpenoids with potential antibacterial activities against clinically important pathogens...
July 10, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28703594/preparation-of-curcumin-piperazine-co-amorphous-phase-and-fluorescence-spectroscopic-and-dft-simulation-studies-on-the-interaction-with-bovine-serum-albumin
#15
Wenzhe Pang, Jie Lv, Shuang Du, Jiaojiao Wang, Jing Wang, Yanli Zeng
In present study, new co-amorphous phase (CAP) of bioactive herbal ingredient curcumin (CUR) with high solubilitythe was screened with pharmaceutically acceptable co-formers. Besides, in order to provide basic information for the best practice of physiological and pharmaceutical preparations of CUR-based CAP, the interaction between CUR-based CAP and bovine serum albumin (BSA) was studied at the molecular level in this paper. CAP of CUR and piperazine with molar ratio of 1:2 was prepared by EtOH-assisted grinding...
July 13, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28682217/simvastatin-modulates-gene-expression-of-key-receptors-in-zebrafish-embryos
#16
V Cunha, M M Santos, P Moradas-Ferreira, L F C Castro, M Ferreira
Nuclear receptors (NR) are involved in the regulation of several metabolic processes and it is well known that these constituents may be modulated by different chemicals classes, including pharmaceuticals that may activate or antagonize NR. In mammals, some pharmaceuticals modulate the transcription of pregnane X receptor, Pxr, peroxisome proliferator activated receptor, Ppars, and aryl hydrocarbon receptor, Ahr, affecting mRNA expression of genes belonging to various regulatory pathways, including lipid metabolism and detoxification mechanisms...
July 6, 2017: Journal of Toxicology and Environmental Health. Part A
https://www.readbyqxmd.com/read/28673196/magnetic-resonance-and-ultrastructural-characterization-of-pegylation-associated-vacuolation-in-nonclinical-models
#17
Thomas Forest, Qiuwei Xu, Sabu Kuruvilla, Heather Vu, Katerina Vlasakova, Warren E Glaab, Cathy Hines, Song Xun
Conjugation with polyethylene glycol (PEG) is a strategy for improving the pharmaceutical properties of therapeutic proteins. In nonclinical studies of PEGylated compounds, microscopic tissue vacuolation is often observed, characterized ultrastructurally in this report by lysosomal distension. Although PEGylation-associated vacuolation appears to be of limited toxicologic concern when alternative therapies are limited, the risk-benefit considerations may be impacted by uncertainty about reversibility, lack of methods for monitoring PEG accumulation in vivo without biopsy, and the variability in tissues affected depending on species studied...
January 1, 2017: Toxicologic Pathology
https://www.readbyqxmd.com/read/28668295/chemometrics-assisted-solid-state-characterization-of-pharmaceutically-relevant-materials-polymorphic-substances
#18
REVIEW
Natalia L Calvo, Rubén M Maggio, Teodoro S Kaufman
Current regulations command to properly characterize pharmaceutically relevant solid systems. Chemometrics comprise a range of valuable tools, suitable to process large amounts of data and extract valuable information hidden in their structure. This review aims to detail the results of the fruitful association between analytical techniques and chemometrics methods, focusing on those which help to gain insight into the characteristics of drug polymorphism as an important aspect of the solid state of bulk drugs and drug products...
June 13, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28657406/a-review-of-radiation-countermeasures-focusing-on-injury-specific-medicinals-and-regulatory-approval-status-part-ii-countermeasures-for-limited-indications-internalized-radionuclides-emesis-late-effects-and-agents-demonstrating-efficacy-in-large-animals-with
#19
Vijay K Singh, Melissa Garcia, Thomas M Seed
PURPOSE: The threat of a radiological/nuclear event is a critical concern for all government agencies involved in national security and public health preparedness. Countermeasures that are safe, easily administered, and effective at diminishing or eliminating adverse health effects to individuals and the overall public health impact of radiation exposure are urgently needed. Radiation countermeasures included in this three-part series have been classified under various subheadings based specifically on their developmental stages for United States Food and Drug Administration (FDA) approval...
June 28, 2017: International Journal of Radiation Biology
https://www.readbyqxmd.com/read/28653896/ganoderma-lucidum-targeting-lung-cancer-signaling-a-review
#20
REVIEW
Balraj Singh Gill, Navgeet, Sanjeev Kumar
Lung cancer causes huge mortality to population, and pharmaceutical companies require new drugs as an alternative either synthetic or natural targeting lung cancer. The conventional therapies cause side effects, and therefore, natural products are used as a therapeutic candidate in lung cancer. Chemical diversity among natural products highlights the impact of evolution and survival of fittest. One such neglected natural product is Ganoderma lucidum used for promoting health and longevity for a longer time...
June 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
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