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https://www.readbyqxmd.com/read/28214631/discovery-of-quinone-directed-antitumor-agents-selectively-bioactivated-by-nqo1-over-cpr-with-improved-safety-profile
#1
Jinlei Bian, Xiang Li, Nan Wang, Xingsen Wu, Qidong You, Xiaojin Zhang
In this work, we mainly focused on discovering compounds with good selectivity for NQO1 over CPR. The NQO1-mediated two-electron reduction of compounds would kill cancer cells selectively, while CPR-mediated one-electron reduction would induce potential hepatotoxicity. Several novel quinone-directed antitumor agents were discovered as specific NQO1 substrates through structure-activity relationship studies. Among them, compound 3,7,8-trimethylnaphtho[1,2-b]furan-4,5-dione (12b) emerged as the most specific substrate of the two-electron oxidoreductase NQO1 and could hardly be reduced by CPR...
February 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28214521/neuroprotective-effect-of-salvianolic-acid-b-against-cerebral-ischemic-injury-in-rats-via-the-cd40-nf-%C3%AE%C2%BAb-pathway-associated-with-suppression-of-platelets-activation-and-neuroinflammation
#2
Shixin Xu, Aiqin Zhong, Huining Ma, Dan Li, Yue Hu, Yingzhi Xu, Junping Zhang
Neuroinflammation plays a critical role in the pathogenesis of ischemia/reperfusion (I/R) injury. Activated platelets are increasingly regarded as initiators and/or amplifiers of inflammatory processes in cerebral I/R injury. Salvianolic acid B (SAB) is the most abundant bioactive compound of Salviae miltiorrhizae, a well-known Chinese herb used to promote blood circulation and eliminating blood stasis. S. miltiorrhizae has been used clinically in Asia for the treatment of ischemic cerebrovascular diseases...
February 15, 2017: Brain Research
https://www.readbyqxmd.com/read/28214075/asymmetric-total-synthesis-of-tetrahydroprotoberberine-derivatives-and-evaluation-of-their-binding-affinities-at-dopamine-receptors
#3
David Y W Lee, Jing Liu, Shuzhen Zhang, Peng Huang, Lee-Yuan Liu-Chen
Cocaine addiction remains a serious challenge for clinical and medical research because there is no effective pharmacological treatment. l-THP, a natural product isolated from Corydalis yanhusuo W.T. Wang, is one of the most frequently used traditional herbs to treat drug addiction in China. Our laboratory first reported that its demethylated metabolites l-ICP, l-CD, and l-CP had high affinity at dopamine D1, D2, and D5 receptors. Here we report the chemical synthesis of these metabolites and other derivatives and their binding affinities at dopamine receptors...
January 31, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28214059/pharmacokinetic-alterations-of-rhubarb-anthraquinones-in-experimental-colitis-induced-by-dextran-sulfate-sodium-in-the-rat
#4
Wen-Jin Wu, Ru Yan, Ting Li, Ya-Ping Li, Rui-Na Zhou, Yi-Tao Wang
ETHNOPHARMACOLOGICAL RELEVANCE: Rhubarb (Rhei Rhizoma et Radix) is used for the treatment of digestive diseases in traditional medicinal practice in China. Recent studies also support its beneficial activities in alleviating ulcerative colitis (UC). AIM OF THE STUDY: This study aimed to characterize the oral pharmacokinetics of rhubarb anthraquinones, the main bioactive components of this herb, in the experimental chronic colitis rat model induced by dextran sulfate sodium (DSS) and to identify the factors causing the pharmacokinetic alterations...
February 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28213824/an-approach-to-the-research-on-ion-and-water-properties-in-the-interphase-between-the-plasma-membrane-and-bulk-extracellular-solution
#5
REVIEW
Hiroshi Hibino, Madoka Takai, Hidenori Noguchi, Seishiro Sawamura, Yasufumi Takahashi, Hideki Sakai, Hitoshi Shiku
In vivo, cells are immersed in an extracellular solution that contains a variety of bioactive substances including ions and water. Classical electrophysiological analyses of epithelial cells in the stomach and small intestine have revealed that within a distance of several hundred micrometers above their apical plasma membrane, lies an extracellular layer that shows ion concentration gradients undetectable in the bulk phase. This "unstirred layer", which contains stagnant solutes, may also exist between the bulk extracellular solution and membranes of other cells in an organism and may show different properties...
February 17, 2017: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28213548/effects-of-gelling-agent-and-extracellular-signaling-molecules-on-the-culturability-of-marine-bacteria
#6
Anita Mac Rygaard, Mariane Schmidt Thøgersen, Kristian Fog Nielsen, Lone Gram, Mikkel Bentzon-Tilia
Only 1 % of marine bacteria are currently culturable using standard laboratory procedures and this is a major obstacle for our understanding of the biology of marine microorganisms and for the discovery of novel microbial natural products. Therefore, the purpose of the present study was to investigate if improved cultivation conditions, including the use of an alternative gelling agent, and supplementation with signaling molecules, could improve the culturability of bacteria from seawater. Substituting agar with gellan gum improved viable counts 3 - 40-fold, depending on medium composition and incubation conditions, with a maximum of 6...
February 17, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28213539/critical-concentration-of-lecithin-enhances-the-antimicrobial-activity-of-eugenol-against-escherichia-coli
#7
Haoshu Zhang, Edward G Dudley, P Michael Davidson, Federico Harte
Lecithin is a natural emulsifier used in a wide range of food and non-food applications to improve physical stability with no known bioactive effects. In this study, the effect of lecithin on the antimicrobial performance of a constant eugenol concentration was tested against three Escherichia coli strains (C600, 0.1229, and O157:H7 strain ATCC 700728). This was the first study focusing on lecithin at concentrations below those commonly used in foods to improve the stability of oil in water emulsions (≤ 10mg/100ml)...
February 17, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28213269/protective-effects-of-morin-on-lipopolysaccharide-d-galactosamine-induced-acute-liver-injury-by-inhibiting-tlr4-nf-%C3%AE%C2%BAb-and-activating-nrf2-ho-1-signaling-pathways
#8
Ye Tian, Zheng Li, Bingyu Shen, Qiaoling Zhang, Haihua Feng
Morin, a bioactive flavonoid extracted from the bark of Moraceae plants and many medicinal herbs, has anti-inflammatory and antioxidative effects. In this research, we explored the protective effects of morin against lipopolysaccharide (LPS) and d-galactosamine (D-GalN) induced acute liver injury in mice. Mice were given an intraperitoneal injection of morin before LPS and D-GalN treatment and the HepG2 cells were only given morin to investigate its effects. The results showed that morin markedly inhibited the production of serum alanine transaminase (ALT), aspartate aminotransferase (AST), interleukin-6 (IL-6), tumor necrosis factor (TNF-α) and hepatic TNF-α, IL-6, and myeloperoxidase (MPO) induced by LPS/D-GalN...
February 14, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28213218/dynamic-flow-through-approach-to-evaluate-readily-bioaccessible-antioxidants-in-solid-food-samples
#9
Miguel A Maia, Tânia R P Soares, Ana I P Mota, María Rosende, Luís M Magalhães, Manuel Miró, Marcela A Segundo
Release of bioactive compounds from food matrices is regarded as the first step towards their human bioavailability. The objective of this work was the implementation of an affordable and robust flow-through device for expedient dynamic leaching experiments aiming at the assessment of readily bioaccessible antioxidant compounds in solid food commodities. A simple configuration is proposed using commercially available devices containing regenerated cellulose filters placed in polypropylene holders to entrap the solid sample, featuring a disposable, single use extraction chamber...
May 1, 2017: Talanta
https://www.readbyqxmd.com/read/28213211/application-of-2d-hplc-coupled-with-principal-component-analysis-to-study-an-industrial-opiate-processing-stream
#10
Paul G Stevenson, Niki K Burns, Stuart D Purcell, Paul S Francis, Neil W Barnett, Fiona Fry, Xavier A Conlan
Principal component analysis (PCA) loading plots were used to elucidate key differences between two-dimensional high performance liquid chromatography (2D-HPLC) fingerprint data from samples collected from stages along the Papaver somniferum industrial process chemistry workflow. Data reduction was completed using a 2D-HPLC peak picking approach as a precursor to chemometric analysis. Using comparisons of the final stages of product extraction as an example, PCA analysis of characteristic 2D-HPLC fingerprints accounted for 84...
May 1, 2017: Talanta
https://www.readbyqxmd.com/read/28213108/intestinal-transport-and-absorption-of-bioactive-phenolic-compounds-from-a-chemically-characterized-aqueous-extract-of-athrixia-phylicoides
#11
Sandra L Bowles, Yonela Ntamo, Christiaan J Malherbe, Abidemi M P Kappo, Johan Louw, Christo J F Muller
ETHNOPHARMACOLOGICAL RELEVANCE: Athrixia phylicoides (A. phylicoides), popularly known as "bush tea", is an indigenous aromatic shrub found in mountainous and grassland areas of the northern and eastern parts of southern Africa. The plant is traditionally used for the treatment of several ailments, including coughing, treating infected wounds, treating boils and sore throat, hypertension and heart disease. Potential anti-diabetic effects have also been demonstrated in vitro. AIM OF THE STUDY: To investigate the intestinal transport of prominent phenolic constituents, across a fully differentiated Caco-2 monolayer, using a characterized aqueous extract of A...
February 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28212817/in-vivo-toxicity-of-copper-oxide-lead-oxide-and-zinc-oxide-nanoparticles-acting-in-different-combinations-and-its-attenuation-with-a-complex-of-innocuous-bio-protectors
#12
Ilzira A Minigalieva, Boris A Katsnelson, Vladimir G Panov, Larisa I Privalova, Anatoly N Varaksin, Vladimir B Gurvich, Marina P Sutunkova, Vladimir Ya Shur, Ekaterina V Shishkina, Irene E Valamina, Ilya V Zubarev, Oleg H Makeyev, Ekaterina Y Meshtcheryakova, Svetlana V Klinova
Stable suspensions of metal oxide nanoparticles (Me-NPs) obtained by laser ablation of 99.99% pure copper, zinc or lead under a layer of deionized water were used separately, in three binary combinations and a triple combination in two independent experiments on rats. In one of the experiments the rats were instilled with Me-NPs intratracheally (i.t.) (for performing a broncho-alveolar lavage in 24hrs to estimate the cytological and biochemical indices of the response of the lower airways), while in the other, Me-NPs were repeatedly injected intraperitoneally (i...
February 14, 2017: Toxicology
https://www.readbyqxmd.com/read/28212702/flavoalkaloids-isolation-biological-activity-and-total-synthesis
#13
Lachlan M Blair, Matthew B Calvert, Jonathan Sperry
The flavoalkaloids possess unique molecular frameworks that contain both a flavonoid and alkaloid component. Flavoalkaloids result from the convergence of distinct biosynthetic pathways, affording natural products that display a wide range of interesting biological activities that would not be expected for flavonoids or alkaloids alone. This chapter collates all the known flavoalkaloids up until early 2016, detailing their isolation, bioactivity, and successful total syntheses.
2017: Alkaloids. Chemistry and Biology
https://www.readbyqxmd.com/read/28212574/the-combined-action-of-mast-cell-chymase-tryptase-and-carboxypeptidase-a3-protects-against-melanoma-colonization-of-the-lung
#14
Mirjana Grujic, Aida Paivandy, Ann-Marie Gustafson, Allan R Thomsen, Helena Öhrvik, Gunnar Pejler
Mast cell secretory granules are densely packed with various bioactive mediators including proteases of chymase, tryptase and CPA3 type. Previous studies have indicated that mast cells can affect the outcome of melanoma but the contribution of the mast cell granule proteases to such effects has not been clear. Here we addressed this issue by assessing mice lacking either the chymase Mcpt4, the tryptase Mcpt6 or carboxypeptidase A3 (Cpa3), as well as mice simultaneously lacking all three proteases, in a model of melanoma dissemination from blood to the lung...
February 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28212342/a-review-on-the-phytochemistry-pharmacology-and-pharmacokinetics-of-amentoflavone-a-naturally-occurring-biflavonoid
#15
REVIEW
Sheng Yu, Hui Yan, Li Zhang, Mingqiu Shan, Peidong Chen, Anwei Ding, Sam Fong Yau Li
Amentoflavone (C30H18O10) is a well-known biflavonoid occurring in many natural plants. This polyphenolic compound has been discovered to have some important bioactivities, including anti-inflammation, anti-oxidation, anti-diabetes, and anti-senescence effects on many important reactions in the cardiovascular and central nervous system, etc. Over 120 plants have been found to contain this bioactive component, such as Selaginellaceae, Cupressaceae, Euphorbiaceae, Podocarpaceae, and Calophyllaceae plant families...
February 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28212329/enzyme-assisted-discovery-of-antioxidant-peptides-from-edible-marine-invertebrates-a-review
#16
REVIEW
Tsun-Thai Chai, Yew-Chye Law, Fai-Chu Wong, Se-Kwon Kim
Marine invertebrates, such as oysters, mussels, clams, scallop, jellyfishes, squids, prawns, sea cucumbers and sea squirts, are consumed as foods. These edible marine invertebrates are sources of potent bioactive peptides. The last two decades have seen a surge of interest in the discovery of antioxidant peptides from edible marine invertebrates. Enzymatic hydrolysis is an efficient strategy commonly used for releasing antioxidant peptides from food proteins. A growing number of antioxidant peptide sequences have been identified from the enzymatic hydrolysates of edible marine invertebrates...
February 16, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28212315/developmental-programming-of-adult-disease-reprogramming-by-melatonin
#17
REVIEW
You-Lin Tain, Li-Tung Huang, Chien-Ning Hsu
Adult-onset chronic non-communicable diseases (NCDs) can originate from early life through so-called the "developmental origins of health and disease" (DOHaD) or "developmental programming". The DOHaD concept offers the "reprogramming" strategy to shift the treatment from adulthood to early life, before clinical disease is apparent. Melatonin, an endogenous indoleamine produced by the pineal gland, has pleiotropic bioactivities those are beneficial in a variety of human diseases. Emerging evidence support that melatonin is closely inter-related to other proposed mechanisms contributing to the developmental programming of a variety of chronic NCDs...
February 16, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28212038/iridium-catalyzed-asymmetric-hydrogenation-of-%C3%AE-%C3%AE-unsaturated-%C3%AE-lactams-scope-and-mechanistic-studies
#18
Qianjia Yuan, Delong Liu, Wanbin Zhang
An efficient asymmetric hydrogenation of β,γ-unsaturated γ-lactams using an iridium-phosphoramidite complex is reported. The chiral γ-lactams were obtained in excellent yields and enantioselectivities (up to 99% yield and 99% ee). The mechanistic studies indicated that the reduced products were obtained via the hydrogenation of the N-acyliminium cations, generated from β,γ-unsaturated γ-lactams, which was verified by (1)H NMR analysis. The reaction was carried out at a reduced catalyst loading of 0.1 mol %, and the reduced products can be transformed to two potential bioactive compounds...
February 17, 2017: Organic Letters
https://www.readbyqxmd.com/read/28211996/alternating-current-electrophoretic-deposition-for-the-immobilization-of-antimicrobial-agents-on-titanium-implant-surfaces
#19
Annabel Braem, Katrijn De Brucker, Nicolas Delattin, Manuela Sonja Killian, Maarten B J Roeffaers, Tomohiko Yoshioka, Satoshi Hayakawa, Patrik Schmuki, Bruno P A Cammue, Sannakaisa Virtanen, Karin Thevissen, Bram Neirinck
One prominent cause of implant failure is infection, therefore research is focusing on developing surface coatings that render the surface resistant to colonization by micro-organisms. Permanently attached coatings of antimicrobial molecules are of particular interest because of the reduced cytoxicity and lower risk of developing resistance compared to controlled release coatings. In this study, we focus on the chemical grafting of bioactive molecules on titanium. To concentrate the molecules at the metallic implant surface, we propose electrophoretic deposition (EPD) applying alternating current (AC) signals with an asymmetrical wave shape...
February 17, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28211933/enhanced-bone-tissue-regeneration-using-a-3d-printed-microstructure-incorporated-with-a-hybrid-nano-hydrogel
#20
Dong Nyoung Heo, Nathan J Castro, Se-Jun Lee, Hanaul Noh, Wei Zhu, Lijie Grace Zhang
Three-dimensional (3D) functional constructs with biomimetic mechanical and chemical properties are ideal for various regenerative medicine applications. These properties of 3D fabricated constructs mainly depend on the intrinsic characteristics of the materials and fabrication method. In this respect, the current use of hydrogels for musculoskeletal tissue repair is not ideal due to the lack of suitable mechanical properties, as well as the high biomimetic requirement for success. To overcome this limitation, we developed a novel functionalized hydrogel with bioactive gold nanoparticles (GNPs), reinforcing a 3D printed microstructure via fused deposition modeling (FDM) for bone tissue regeneration...
February 17, 2017: Nanoscale
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