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https://www.readbyqxmd.com/read/28938743/pharmaceutical-industry-contribution-to-research-is-essential-but-full-transparency-and-guidelines-are-required
#1
Amir Lass
No abstract text is available yet for this article.
October 1, 2017: Human Reproduction
https://www.readbyqxmd.com/read/28938517/green-tea-camellia-sinensis-and-l-theanine-medicinal-values-and-beneficial-applications-in-humans-a-comprehensive-review
#2
REVIEW
Muhammad Saeed, Muhammad Naveed, Muhammad Arif, Mohib Ullah Kakar, Robina Manzoor, Mohamed Ezzat Abd El-Hack, Mahmoud Alagawany, Ruchi Tiwari, Rekha Khandia, Ashok Munjal, Kumaragurubaran Karthik, Kuldeep Dhama, Hafiz M N Iqbal, Maryam Dadar, Chao Sun
Green tea (Camellia sinensis) is a famous herb, and its extract has been extensively used in traditional Chinese medicinal system. In this context, several studies have revealed its health benefits and medicinal potentialities for several ailments. With ever increasing scientific knowledge, search for safer, potential and novel type of health-related supplements quest, scientists are re-directing their research interests to explore natural resources i.e. medicinal herbs/plant derived compounds. Green tea consumption has gained a special attention and popularity in the modern era of changing lifestyle...
September 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28938421/bortezomib-alone-and-in-combination-with-salinosporamid-a-induces-apoptosis-and-promotes-pheochromocytoma-cell-death-in-vitro-and-in-female-nude-mice
#3
Petra Bullova, Antony Cougnoux, Geena Marzouca, Juraj Kopacek, Karel Pacak
Proteasome inhibitors have been frequently used in treating hematologic and solid tumors. They are administered individually or in combination with other regimens, to prevent severe side effects and resistance development. Since they have been shown to be efficient and are pharmaceutically available, we tested the first FDA-approved proteasome inhibitor bortezomib alone and in combination with another proteasome inhibitor, salinosporamid A, in pheochromocytoma cells. Pheochromocytomas/paragangliomas (PHEOs/PGLs) are neuroendocrine tumors for which no definite cure is yet available...
August 15, 2017: Endocrinology
https://www.readbyqxmd.com/read/28937768/lewis-acid-mediated-cascade-friedel-craft-alkyne-indol-2-yl-cation-cyclization-vinyl-cation-trapping-for-the-synthesis-of-n-fused-indole-derivatives
#4
Santosh J Gharpure, Yogesh G Shelke
A Lewis acid promoted cascade Friedel-Craft/alkyne indol-2-yl cation cyclization/vinyl cation trapping for an efficient and divergent synthesis of N-fused indoles is developed. The present study illustrates the first example of an alkyne as a nucleophile on the less explored indol-2-yl cation. The method efficiently affords pharmaceutically important pyrrolizino-quinolines and complex fused indole derivatives in high yields.
September 22, 2017: Organic Letters
https://www.readbyqxmd.com/read/28937665/a-reductive-aminase-from-aspergillus-oryzae
#5
Godwin A Aleku, Scott P France, Henry Man, Juan Mangas-Sanchez, Sarah L Montgomery, Mahima Sharma, Friedemann Leipold, Shahed Hussain, Gideon Grogan, Nicholas J Turner
Reductive amination is one of the most important methods for the synthesis of chiral amines. Here we report the discovery of an NADP(H)-dependent reductive aminase from Aspergillus oryzae (AspRedAm, Uniprot code Q2TW47) that can catalyse the reductive coupling of a broad set of carbonyl compounds with a variety of primary and secondary amines with up to >98% conversion and with up to >98% enantiomeric excess. In cases where both carbonyl and amine show high reactivity, it is possible to employ a 1:1 ratio of the substrates, forming amine products with up to 94% conversion...
October 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28937621/the-development-of-a-melt-extruded-shellac-carrier-for-the-targeted-delivery-of-probiotics-to-the-colon
#6
Noel M Gately, James E Kennedy
Hot melt extrusion (HME) is considered an efficient technique in developing solid molecular dispersions, and has been demonstrated to provide sustained, modified and targeted drug delivery resulting in improved bioavailability. However, most commercial enteric or pH-responsive polymers are relatively difficult to process or have high Glass Transition Temperature (Tg) values, making their use with temperature-sensitive drugs, probiotics or biologics not viable. Shellac is a natural thermoplastic, and after a review of current literature on the pharmaceutical HME process, a possible gap in the knowledge of the use of shellac to produce dosage forms by means of HME was identified...
September 22, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28937591/metabolic-engineering-of-escherichia-coli-for-producing-astaxanthin-as-the-predominant-carotenoid
#7
Qian Lu, Yi-Fan Bu, Jian-Zhong Liu
Astaxanthin is a carotenoid of significant commercial value due to its superior antioxidant potential and wide applications in the aquaculture, food, cosmetic and pharmaceutical industries. A higher ratio of astaxanthin to the total carotenoids is required for efficient astaxanthin production. β-Carotene ketolase and hydroxylase play important roles in astaxanthin production. We first compared the conversion efficiency to astaxanthin in several β-carotene ketolases from Brevundimonas sp. SD212, Sphingomonas sp...
September 22, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28937226/diblock-terpolymers-are-tunable-and-ph-responsive-vehicles-to-increase-hydrophobic-drug-solubility-for-oral-administration
#8
Swapnil Tale, Anatolii A Purchel, Molly C Dalsin, Theresa M Reineke
Synthetic polymers offer tunable platforms to create new oral drug delivery vehicles (excipients) to increase solubility, supersaturation maintenance, and bioavailability of poorly aqueous soluble pharmaceutical candidates. Five well-defined diblock terpolymers were synthesized via reversible addition-fragmentation chain transfer polymerization (RAFT) and consist of a first block of either poly(ethylene-alt-propylene) (PEP), poly(N-isopropylacrylamide) (PNIPAm), or poly(N,N-diethylaminoethyl methacrylate) (PDEAEMA) and a second hydrophilic block consisting of a gradient copolymer of N,N-dimethylacrylamide (DMA) and 2-methacrylamidotrehalose (MAT)...
September 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28937217/visible-light-mediated-aerobic-oxidation-of-n-alkylpyridinium-salts-under-organic-photocatalysis
#9
Yunhe Jin, Lunyu Ou, Haijun Yang, Hua Fu
Quinolones and isoquinolones exhibit diverse biological and pharmaceutical activities, and their synthesis is highly desirable under mild conditions. Here, a highly efficient and environmentally friendly visible light-mediated aerobic oxidation of readily available N-alkylpyridinium salts has been developed with Eosin Y as the organic photocatalyst and air as the terminal oxidant, and the reaction provided quinolones and isoquinolones in good yields. The method shows numerous advantages including mild and environmentally friendly conditions, high efficiency, tolerance of wide functional groups and low cost...
September 22, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28936936/-treatment-of-dementia
#10
K Blom, G A H van den Elsen, H L Koek, J B Sanders, H C Kruithof, J A H R Claassen
- Treatment options for patients with dementia are limited. This article provides an overview of possible interventions, both pharmaceutical and non-pharmaceutical, for Alzheimer's disease, vascular dementia and mixed dementia.- Pharmaceutical treatment options include cholinesterase inhibitors, memantine and experimental medication. Cholinesterase inhibitors are only recommended for Alzheimer's disease and mixed dementia, not for vascular dementia or mild cognitive impairment. There is no proof of effectiveness for the other pharmaceutical options...
2017: Nederlands Tijdschrift Voor Geneeskunde
https://www.readbyqxmd.com/read/28936788/isorhamnetin-derivatives-and-piscidic-acid-for-hypercholesterolemia-cholesterol-permeability-hmg-coa-reductase-inhibition-and-docking-studies
#11
Asma Ressaissi, Nebil Attia, Pedro Luis Falé, Rita Pacheco, Bruno L Victor, Miguel Machuqueiro, Maria Luísa M Serralheiro
Bioactive compounds, such as isorhamnetin and piscidic acid, were obtained from decoctions of cladodes (stem pads from Opuntia ficus-indica). The effect of these phenolic compounds, in a fiber-free extract, were evaluated as inhibitors of cholesterol permeation through a Caco-2 cell monolayer and as 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. A reduction of 38% in cholesterol permeation through the Caco-2 cell monolayer was obtained, and the phenolic compounds all permeated between 6 and 9%. A mixture of these compounds showed an IC50 of 20...
September 21, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28936609/a-hierarchical-testing-strategy-for-micropollutants-in-drinking-water-regarding-their-potential-endocrine-disrupting-effects-towards-health-related-indicator-values
#12
Jochen Kuckelkorn, Regine Redelstein, Timon Heide, Jennifer Kunze, Sibylle Maletz, Petra Waldmann, Tamara Grummt, Thomas-Benjamin Seiler, Henner Hollert
In Germany, micropollutants that (may) occur in drinking water are assessed by means of the health-related indicator value (HRIV concept), developed by the German Federal Environment Agency. This concept offers five threshold values (≤ 0.01 to ≤ 3 μg l(-1)) depending on availability and completeness of data regarding genotoxicity, neurotoxicity, and germ cell-damaging potential. However, the HRIV concept is yet lacking integration of endocrine disruptors as one of the most prominent toxicological concerns in water bodies, including drinking water...
September 21, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28936330/pyridine-sulfinates-as-general-nucleophilic-coupling-partners-in-palladium-catalyzed-cross-coupling-reactions-with-aryl-halides
#13
Tim Markovic, Benjamin N Rocke, David C Blakemore, Vincent Mascitti, Michael C Willis
Pyridine rings are ubiquitous in drug molecules; however, the pre-eminent reaction used to form carbon-carbon bonds in the pharmaceutical industry, the Suzuki-Miyaura cross-coupling reaction, often fails when applied to these structures. This phenomenon is most pronounced in 2-substituted pyridines, and results from the difficulty in preparing, the poor stability of, and low efficiency in reactions of pyridine-2-boronates. We demonstrate that by replacing these boronates with pyridine-2-sulfinates, a cross-coupling process of unrivalled scope and utility is realized...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28936329/3-cyanoallyl-boronates-are-versatile-building-blocks-in-the-synthesis-of-polysubstituted-thiophenes
#14
Wenjie Shao, Sherif J Kaldas, Andrei K Yudin
We report the preparation of hitherto unprecedented 3-cyanoallyl boronates using condensation of the parent α-boryl aldehyde and nitriles. The resulting allyl boronates have been used to generate a wide range of borylated thiophenes, which represent a valuable class of heterocycles in modern drug discovery. Subsequent Suzuki-Miyaura cross-coupling enabled the synthesis of pharmaceutically important 3,5-disubstituted aminothiophenes. Moreover, late stage functionalization gave access to borylated bromothiophene and thieno[2,3-b]pyridines...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28935769/mof-derived-cobalt-nanoparticles-catalyze-a-general-synthesis-of-amines
#15
Rajenahally V Jagadeesh, Kathiravan Murugesan, Ahmad S Alshammari, Helfried Neumann, Marga-Martina Pohl, Jörg Radnik, Matthias Beller
The development of base metal catalysts for the synthesis of pharmaceutically relevant compounds remains an important goal of chemical research. Here, we report that cobalt nanoparticles encapsulated by a graphitic shell are broadly effective reductive amination catalysts. Their convenient and practical preparation entailed template assembly of cobalt-diamine-dicarboxylic acid metal organic frameworks on carbon and subsequent pyrolysis under inert atmosphere. The resulting stable and reusable catalysts were active for synthesis of primary, secondary, tertiary and N-methylamines (>140 examples)...
September 21, 2017: Science
https://www.readbyqxmd.com/read/28935728/draft-genome-sequence-of-pantoea-agglomerans-jm1-a-strain-isolated-from-soil-polluted-by-industrial-production-of-beta-lactam-antibiotics-that-exhibits-valacyclovir-like-hydrolase-activity
#16
Jiří Zahradník, Martina Plačková, Andrea Palyzová, Helena Marešová, Eva Kyslíková, Pavel Kyslík
Strain Pantoea agglomerans JM1 was isolated from the soil of a microbiome that had been exposed to polluting pharmaceuticals. The bacterium exhibited enzymatic activities useful for the biotransformation of beta-lactams. The genome of the strain was assembled and described, and the gene encoding valacyclovir-like hydrolase was identified.
September 21, 2017: Genome Announcements
https://www.readbyqxmd.com/read/28935596/animal-models-for-evaluation-of-oral-delivery-of-biopharmaceuticals
#17
REVIEW
Stine Harloff-Helleberg, Line Hagner Nielsen, Hanne Mørck Nielsen
Biopharmaceuticals are increasingly important for patients and the pharmaceutical industry due to their ability to treat and, in some cases, even cure chronic and potentially life-threatening diseases. Most biopharmaceuticals are administered by injection, but intensive focus on development of systems for oral delivery of biopharmaceuticals may result in new treatment modalities to increase patient compliance and reduce product cost. In the preclinical development phase, use of experimental animal models is essential for evaluation of new formulation designs...
September 18, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28935592/manufacture-of-fibrous-dosage-forms-by-wet-micro-patterning-and-drying
#18
Aron H Blaesi, Nannaji Saka
Recently, we have introduced fibrous dosage forms prepared by the predictable deposition, or 3D-micro-patterning, of a drug-laden fibrous melt on a surface. Such dosage forms enable precisely controlled microstructures and drug release rates, and can be manufactured by an efficient, continuous melt process. However, the applicability of melt-processing to manufacture pharmaceutical dosage forms is limited because the temperatures at which suitable excipients plasticize by melting are greater than the degradation or melting temperatures of many kinds of drugs...
September 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28935405/composted-biosolids-and-treated-wastewater-as-sources-of-pharmaceuticals-and-personal-care-products-for-plant-uptake-a-case-study-with-carbamazepine
#19
Evyatar Ben Mordechay, Jorge Tarchitzky, Yona Chen, Moshe Shenker, Benny Chefetz
Irrigation with treated wastewater (TWW) and application of biosolids to arable land expose the agro-environment to pharmaceuticals and personal care products (PPCPs) which can be taken up by crops. In this project, we studied the effect of a carrier medium (e.g., biosolids and TWW) on plant (tomato, wheat and lettuce) uptake, translocation and metabolism of carbamazepine as a model for non-ionic PPCPs. Plant uptake and bioconcentration factors were significantly lower in soils amended with biosolids compared to soils irrigated with TWW...
September 19, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28935257/tetrac-conjugated-polymersomes-for-integrin-targeted-delivery-of-camptothecin-to-colon-adenocarcinoma-in-vitro-and-in-vivo
#20
Mona Alibolandi, Rouhollah Rezvani, Sara Amel Farzad, Seyed Mohammad Taghdisi, Khalil Abnous, Mohammad Ramezani
In this study, we prepared tetraiodothyroacetic acid (tetrac) conjugated PEG-PLGA polymersomes for the targeted delivery of camptothecin to colon adenocarcinoma. Tetrac, which binds to integrin αvβ3 with high affinity and specificity, was covalently conjugated to the surface of the PEGylated polymersomal formulation of camptothecin (CPT). The hydrodynamic and morphological properties of the prepared system were evaluated using TEM (transmission electron microscopy), SEM (scanning electron microscopy) and DLS (dynamic light scattering) experiments...
September 18, 2017: International Journal of Pharmaceutics
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