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https://www.readbyqxmd.com/read/28724165/cytogenotoxicity-of-inclusion-complexes-of-diazepam-with-2-hydroxypropyl-%C3%AE-cyclodextrin
#1
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-nano-micelle-through-self-assembly-pectin-curcumin-conjugates-preparation-characterization-and-anti-cancer-activity-evaluation
#2
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. Extremely low aqueous solubility, stability and bioavailability of curcumin limits its application in the field of medicine. In this study, we developed pectin-curcumin (PEC-CCM) conjugates which could self-assemble water-soluble nano-micelles in aqueous solution. The structure of PEC-CCM conjugates was characterized by ultraviolet and visible spectra (UV-Vis), fluorescence spectra, Fourier transform infrared (FTIR) spectroscopy and 1H nuclear magnetic resonance (NMR) spectroscopy...
July 19, 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
#3
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
#4
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/28682217/simvastatin-modulates-gene-expression-of-key-receptors-in-zebrafish-embryos
#5
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
#6
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
#7
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
#8
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
#9
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
https://www.readbyqxmd.com/read/28653347/preliminary-evaluation-of-pleurotus-ostreatus-for-the-removal-of-selected-pharmaceuticals-from-hospital-wastewater
#10
Laura Palli, Francesc Castellet-Rovira, Miriam Pérez-Trujillo, Donatella Caniani, Montserrat Sarrà-Adroguer, Riccardo Gori
The fungus Pleurotus ostreatus was investigated to assess its ability to remove diclofenac, ketoprofen and atenolol spiked at 10 mg/L each one in hospital wastewater. The degradation test was carried out in a fluidized bed bioreactor testing both the batch and the continuous mode (hydraulic retention time in the range 1.63-3 d). In batch mode, diclofenac disappeared in less than 24 h, ketoprofen was degraded up to almost 50% in 5 d while atenolol was not removed. In continuous mode, diclofenac and ketoprofen removals were about 100% and 70% respectively; atenolol degradation was negligible during the first 20 d but it increased up to 60% after a peak of laccase production and notable biomass growth...
June 27, 2017: Biotechnology Progress
https://www.readbyqxmd.com/read/28644553/structural-insights-into-the-inclusion-complexes-between-clomiphene-citrate-and-%C3%AE-cyclodextrin-the-mechanism-of-preferential-isomeric-selection
#11
Arti Maheshwari, Harish Saraswat, Santosh Kumar Upadhyay
A major challenge in pharmaceuticals for clinical applications is to alter the solubility, stability, and toxicity of drug molecules in living systems. Cyclodextrins (CDs) have the ability to form host-guest inclusion complexes with pharmaceuticals for further development of new drug formulations. The inclusion complex of clomiphene citrate (CL), a poorly water-soluble drug, with native β-cyclodextrin (β-CD) was characterized by a one and two-dimensional nuclear magnetic resonance (NMR) spectroscopic approach and also by molecular docking techniques...
June 23, 2017: Chirality
https://www.readbyqxmd.com/read/28625724/the-binary-system-of-ibuprofen-nicotinamide-under-nanoscale-confinement-from-cocrystal-to-coamorphous-state
#12
Yanping Bi, Deli Xiao, Shuai Ren, Shuyan Bi, Jianzhu Wang, Fei Li
Coamorphous systems have gained success in stabilizing amorphous drugs and improving their solubility and dissolution. Here we proposed to confine a binary mixture of drug and coformer (CF) within nanopores to obtain a nano-confined coamorphous (NCA) system. For proving feasibility of this proposal, a poorly water-soluble drug (ibuprofen, IBP) and a frequently used pharmaceutical CF (nicotinamide, NIC) were loaded into nanopores of mesoporous silica microspheres (MSMs). The solid state of NCA system was characterized by differential scanning calorimetry, X-ray powder diffraction, infrared spectrum and solid state nuclear magnetic resonance...
June 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28624088/nootkatone-encapsulation-by-cyclodextrins-effect-on-water-solubility-and-photostability
#13
Miriana Kfoury, David Landy, Steven Ruellan, Lizette Auezova, Hélène Greige-Gerges, Sophie Fourmentin
Nootkatone (NO) is a sesquiterpenoid volatile flavor, used in foods, cosmetics and pharmaceuticals, possessing also insect repellent activity. Its application is limited because of its low aqueous solubility and stability; this could be resolved by encapsulation in cyclodextrins (CDs). This study evaluated the encapsulation of NO by CDs using phase solubility studies, Isothermal Titration Calorimetry, Nuclear Magnetic Resonance spectroscopy and molecular modeling. Solid CD/NO inclusion complex was prepared and characterized for encapsulation efficiency and loading capacity using UV-Visible...
December 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28600832/investigation-of-drug-products-received-for-analysis-in-the-swedish-strida-project-on-new-psychoactive-substances
#14
Matilda Bäckberg, Karl-Henrik Jönsson, Anders Helander, Olof Beck
The web-based open sale of unregulated new psychoactive substances (NPS) has shown a steady increase over the past years. Analysis of drug products sold as NPS is useful to confirm the true chemical contents, for comparison with the substances detected in corresponding body fluids, but also to study drug trends. This work describes the examination of 251 drug products that were randomly submitted for analysis in 173 cases of suspected NPS-related intoxications in the Swedish STRIDA project in 2010-2015. Of the products, 39% were powders/crystals, 32% tablets/capsules, 16% herbal materials, 8% liquids, 1% blotters, and 4% others...
June 9, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28584912/new-cryptotanshinone-derivatives-with-anti-influenza-a-virus-activities-obtained-via-biotransformation-by-mucor-rouxii
#15
Wenni He, Yao Li, Yuejie Qin, Xiaomei Tong, Zhijun Song, Yu Zhao, Ran Wei, Li Li, Huanqin Dai, Wenzhao Wang, Houwei Luo, Xin Ye, Lixin Zhang, Xueting Liu
This paper provides an efficient platform to diversify the structure and pharmaceutical potentials of known natural products. Seven metabolites were obtained via the biotransformation of cryptotanshinone by the fungus Mucor rouxii AS 3.3447, and assigned as 13R-14R-hydroxy-anhydride of 16R-cryptotanshinone (1), 1S-hydroxy-anhydride of 16R-cryptotanshinone (2), 1R-hydroxy-anhydride of 16R-cryptotanshinone (3), 3S-hydroxy-epicryptoacetalide (4), 3S-hydroxy-cryptoacetalide (5), epicryptoacetalide (6), and cryptoacetalide (7)...
June 5, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28583765/current-role-and-future-perspectives-of-multivariate-chemometric-methods-in-nmr-spectroscopic-analysis-of-pharmaceutical-products
#16
REVIEW
Yulia B Monakhova, Ulrike Holzgrabe, Bernd W K Diehl
Nuclear magnetic resonance (NMR) is a fast and accurate analytical method. Associated with chemometrics, it gradually becomes more important tool for the pharmaceutical industry. In this review studies dealing with the applications of multivariate analysis to NMR spectroscopic profiles were grouped and discussed according to the analytical problem solved. The following topics were covered: authenticity of medicines according to variety, seasonal and geographical differences of herbal plants; quantitative prediction of pharmacologically relevant parameters; production and batches approval; investigation of drug structure modifications; site-specific natural isotope fractionation (SNIF-NMR) fingerprinting for origin and manufacturer tracking and others...
May 27, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28578058/toralactone-glycoside-in-cassia-obtusifolia-mediates-hepatoprotection-via-an-nrf2-dependent-anti-oxidative-mechanism
#17
Yongtaek Seo, Jae-Sook Song, Young-Mi Kim, Young Pyo Jang
Cassia obtusifolia L. (Leguminosae) seeds are a well-known medicinal food in East Asia and are used to clear liver heat, sharpen vision, lubricate the intestines, and promote bowel movement. The aims of the present study were to identify the hepatoprotective components of C. obtusifolia seeds by bioactivity-guided isolation and to elucidate their mechanisms of action. Ten phenolic glycosides were isolated from the most active ethyl acetate fraction, and their chemical structures were elucidated by spectroscopic analyses...
July 2017: Food Research International
https://www.readbyqxmd.com/read/28544938/sex-steroids-and-metabolic-responses-in-mussels-mytilus-galloprovincialis-exposed-to-drospirenone
#18
Tiziana Cappello, Denise Fernandes, Maria Maisano, Andrea Casano, Marta Bonastre, Maria João Bebianno, Angela Mauceri, Salvatore Fasulo, Cinta Porte
Drospirenone (DRO) is a synthetic progestin derived from 17α-spironolactone with a pharmacological mechanism of action similar to progesterone. Despite its wide use as pharmaceutical and consequent continuous release into the aquatic environment, DRO effects have been poorly investigated on aquatic biota. In order to unravel the toxicity mechanisms of DRO, mussels Mytilus galloprovincialis were exposed for 7 days to different concentrations of DRO, namely 20ng/L (Low; L), 200ng/L (Medium; M), 2000ng/L (High; H) and 10μg/L (Super High; SH) nominal doses...
May 22, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28537194/an-investigation-into-the-potential-role-of-brain-angiogenesis-inhibitor-protein-3-bai3-in-the-tumorigenesis-of-small-cell-carcinoma-a-review-of-the-surrounding-literature
#19
Michael Thomas, David Snead, Daniel Mitchell
Brain angiogenesis inhibitor protein 3 (BAI3) is from the adhesion group of seven-transmembrane spanning G protein-coupled receptors (GPCRs) and has been identified via gene expression profiling as being upregulated in small-cell lung cancer (SCLC) tumors. It has subsequently been validated as a sensitive and specific immunohistochemical marker for SCLC, helping to differentiate these tumors from morphologically similar large-cell neuroendocrine (LCNEC) malignancies. It is, however, still unclear as to the role BAI3 proteins might play in SCLC and indeed how they might contribute to tumorigenesis...
May 24, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28528487/role-of-medicines-of-unknown-identity-in-adverse-drug-reaction-related-hospitalizations-in-developing-countries-evidence-from-a-cross-sectional-study-in-a-teaching-hospital-in-the-lao-people-s-democratic-republic
#20
Céline Caillet, Chanvilay Sichanh, Gaëtan Assemat, Myriam Malet-Martino, Agnès Sommet, Haleh Bagheri, Noudy Sengxeu, Niphonh Mongkhonmath, Mayfong Mayxay, Lamphone Syhakhang, Maryse Lapeyre-Mestre, Paul N Newton, Anne Roussin
INTRODUCTION: The health dangers of medicines of unknown identity (MUIs) [loose pharmaceutical units repackaged in individual bags without labelling of their identity] have been suspected in L/MICs. Using visual and analytical tools to identify MUIs, we investigated the frequency of, and factors associated with, adverse drug reaction (ADR)-related hospitalizations in a central hospital in Vientiane Capital, Lao People's Democratic Republic (PDR). METHODS: All unplanned admissions, except for acute trauma and intentional overdose, were prospectively recorded during a 7-week period in 2013, leading to include 453 adults hospitalized for ≥24 h...
May 20, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
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