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Nuclear pharmaceutical

Yan Zhang, Li-Hong Zhang, Xi Chen, Ning Zhang, Guang Li
Aging is a complex process that is accompanied by neurological damage. Chronic injection of d-galactose (d-gal) can accelerate the aging process similar to natural aging and is commonly used to build an aging model to investigate aging. In the present study, the effects of piceatannol on d-gal-induced aging in mice were evaluated. Piceatannol treatment showed an observable anti-aging effect. Results obtained in vivo showed that piceatannol retained spontaneous motor activity and enhanced spatial learning and memory abilities in mice in which aging was induced by d-gal...
December 7, 2017: Food & Function
Min A Lee, Lingchen Tan, Huiseon Yang, Yeong-Gwan Im, Young Jun Im
Peroxisome proliferator-activator receptor (PPAR) γ is a nuclear hormone receptor that regulates glucose homeostasis, lipid metabolism, and adipocyte function. PPARγ is a target for thiazolidinedione (TZD) class of drugs which are widely used for the treatment of type 2 diabetes. Recently, lobeglitazone was developed as a highly effective TZD with reduced side effects by Chong Kun Dang Pharmaceuticals. To identify the structural determinants for the high potency of lobeglitazone as a PPARγ agonist, we determined the crystal structures of the PPARγ ligand binding domain (LBD) in complex with lobeglitazone and pioglitazone at 1...
December 4, 2017: Scientific Reports
Li Zhao, Arthur C Pinon, Lyndon Emsley, Aaron J Rossini
Solid-state NMR has become a valuable tool for the characterization of both pure and formulated active pharmaceutical ingredients (APIs). However, NMR generally suffers from poor sensitivity that often restricts NMR experiments to nuclei with favorable properties, concentrated samples and acquisition of 1D NMR spectra. Here we review how dynamic nuclear polarization (DNP) can be applied to routinely enhance the sensitivity of solid-state NMR experiments by one to two orders of magnitude for both pure and formulated APIs...
November 28, 2017: Magnetic Resonance in Chemistry: MRC
Alex O Okaru, Tobias S Brunner, Svenja M Ackermann, Thomas Kuballa, Stephan G Walch, Matthias Kohl-Himmelseher, Dirk W Lachenmeier
A simple, rapid, and selective quantitative nuclear magnetic resonance spectroscopic method was evaluated for the determination of the content of fluorinated pharmaceuticals. 19F NMR spectra were either obtained in dimethylsulfoxide-d6 or aqueous buffer, using trifluoroacetic acid as internal standard. Quantification of 13 fluorine-containing pharmaceuticals spanning various pharmacological classes was accomplished using the proposed method. The method was found to be fit for purpose (interday precision 1.2% relative standard deviation) and may thus be applied for routine analysis and quality control of fluorine-containing pharmaceuticals due to its simplicity, nondestructive sample measurement, reliability, and high specificity...
2017: Journal of Analytical Methods in Chemistry
Minsup Lee, Seohyeon Yun, Hyesook Lee, Jaewook Yang
Retinal vascular endothelial growth factor (VEGF) increased by neovascularization is well known as a pathogenic factor in ocular neovascular diseases. However, it is still unclear how retinal neurons are damaged by VEGF. The aims of this study are to demonstrate the inflammatory protein expression regulated by VEGF using mouse photoreceptor-derived cells and the protective effect of quercetin against VEGF-induced inflammatory response. Expression and phosphorylation of protein and expression of mRNA were detected by immunoblot and reverse transcriptase polymerase chain reaction...
November 22, 2017: International Journal of Molecular Sciences
Joseph Lau, Kuo-Shyan Lin, François Bénard
Theranostics is the integration of diagnostic information with pharmaceuticals to increase effectiveness and safety of cancer treatments. Nuclear medicine provides a non-invasive means to visualize drug target expression across primary and metastatic sites, and assess pharmacokinetics and efficacy of companion therapeutic agents. This is significant given the increasing recognition of the importance of clonal heterogeneity in treatment response and resistance. Carbonic anhydrase IX (CA-IX) has been advocated as an attractive diagnostic and therapeutic biomarker for targeting hypoxia in solid malignancies...
2017: Theranostics
A J Fenwick, J L Wevrett, K M Ferreira, A M Denis-Bacelar, A P Robinson
In External Beam Radiotherapy, National Metrology Institutes (NMIs) play a critical role in the delivery of accurate absorbed doses to patients undergoing treatment. In contrast for nuclear medicine the role of the NMI is less clear and although significant work has been done in order to establish links for activity measurement, the calculation of administered absorbed doses is not traceable in the same manner as EBRT. Over recent decades the use of novel radiolabelled pharmaceuticals has increased dramatically...
November 11, 2017: Applied Radiation and Isotopes
Boris Itin, Ivan V Sergeyev
Solid-state NMR (SSNMR) is a powerful tool for the elucidation of structure and dynamics in biological macromolecules. Over the years, SSNMR spectroscopists have developed an array of techniques enabling the measurement of internuclear correlations, distances, and torsional angles; these have been applied to the study of a number of biological systems that are difficult to study by X-ray crystallography and solution NMR, including key biological targets such as membrane proteins and amyloid fibrils. Applications of SSNMR to other topic areas, including materials science, pharmaceuticals, and small molecules, have also flourished in recent years...
2018: Methods in Molecular Biology
Katherine Noel Clayton, Gregory D Berglund, Jacqueline C Linnes, Tamara L Kinzer-Ursem, Steven T Wereley
Analytical characterization of DNA microviscosity provides critical biophysical insights into nuclear crowding, nucleic acid-based pharmaceutical development, and nucleic acid-based biosensor device design. However, most viscosity characterization methods require large sample volumes and destructive testing. In contrast, particle diffusometry, permits in situ analysis of DNA microviscosity with short measurement times (8 seconds) using small volumes (< 3L) which are compatible with DNA preparatory procedures...
November 17, 2017: Analytical Chemistry
Tawona N Chinembiri, Minja Gerber, Lissinda H du Plessis, Jan L du Preez, Josias H Hamman, Jeanetta du Plessis
Background: Withania somnifera is a medicinal plant native to India and is known to have anticancer properties. It has been investigated for its anti-melanoma properties, and since melanoma presents on the skin, it is prudent to probe the use of W. somnifera in topical formulations. To enhance topical drug delivery and to allow for controlled release, the use of niosomes and solid lipid nanoparticles (SLNs) as delivery vesicles were explored. Objective: The objective of this study is to determine the stability and topical delivery of W...
October 2017: Pharmacognosy Magazine
Shilin Zhu, Siyuan Tang, Feng Su
Diosgenin, as an essential natural steroidal saponin, can be extracted from numerous sources, primarily from fenugreek. It is an important raw material for the synthesis of steroid hormone drugs. It exhibits antitumor, anti‑inflammatory, antioxidation and several other significant pharmacologic actions, and is of high pharmaceutical value. In the present study, the activities and underlying mechanisms of dioscin in the inhibition of ischemic stroke in rats were investigated. Inflammatory responses wer analyzed using ELISA kits and caspase‑3 and caspase‑9 activity was analyzed using Caspase‑3 and caspase‑9 activity kits...
October 26, 2017: Molecular Medicine Reports
Ki-Shuk Shim, Bohyoung Lee, Jin Yeul Ma
BACKGROUND: Rumex crispus root has traditionally been used in Asian medicine for the treatment of hemorrhage and dermatolosis. The aim of this study was to explore the pharmaceutical effects of water extract of Rumex crispus (WERC) on osteoblast and osteoclast differentiation. We also studied the effect of WERC on the receptor activator of nuclear factor kappa-B ligand (RANKL)-induced trabecular bone destruction mice model. METHODS: High performance liquid chromatography analysis was used to identify three compounds (emodin, chrysophanol, and physcion) of WERC...
October 26, 2017: BMC Complementary and Alternative Medicine
Tae-Yong Jeong, Dahye Yoon, Suhkmann Kim, Hyun Young Kim, Sang Don Kim
Studies are underway to gather information about the mode of action (MOA) of emerging pollutants that could guide practical environmental decision making. Previously, we showed that propranolol, an active pharmaceutical ingredient, had adverse effects on Daphnia magna that were similar to its pharmaceutical action. In order to characterize the mode of action of propranolol in D. magna, which is suspected to be organ-specific pharmaceutical action or baseline toxicity, we performed time-series monitoring of behavior along with heart rate measurements and nuclear magnetic resonance (NMR) based metabolite profiling...
October 20, 2017: Environmental Pollution
Yuki Toyama, Yoko Mase, Hanaho Kano, Mariko Yokogawa, Masanori Osawa, Ichio Shimada
The gating of potassium ion (K(+)) channels is regulated by various kinds of protein-protein interactions (PPIs). Structural investigations of these PPIs provide useful information not only for understanding the gating mechanisms of K(+) channels, but also for developing the pharmaceutical compounds targeting K(+) channels. Here, we describe a nuclear magnetic resonance spectroscopic method, termed the cross saturation (CS) method, to accurately determine the binding surfaces of protein complexes, and its application to the investigation of the interaction between a G protein-coupled inwardly rectifying K(+) channel and a G protein α subunit...
2018: Methods in Molecular Biology
Jun Liu, Ruyu Bai, Yunpeng Liu, Xin Zhang, Juan Kan, Changhai Jin
In recent years, several medicinal plants have been demonstrated as valuable resources of naturally occurring polysaccharide-polyphenolic conjugates. For the first time, this article introduces recent advances of polysaccharide-polyphenolic conjugates isolated from different medicinal plants. The isolation, purification, structural characterization and biological activities of polysaccharide-polyphenolic conjugates are introduced in details. In general, polysaccharide-polyphenolic conjugates can be isolated by hot water or alkaline extraction followed by purification through anion exchange chromatography or gel filtration chromatography...
October 16, 2017: International Journal of Biological Macromolecules
Dae-Sung Lee, Chang-Min Lee, Seong Kook Park, Mi-Jin Yim, Jeong Min Lee, Grace Choi, Jong Su Yoo, Won-Kyo Jung, Saegwang Park, Su-Kil Seo, Won Sun Park, Il-Whan Choi
Marine algae are rich sources of biologically active compounds that may present useful leads in the development of pharmaceuticals, nutraceuticals, and functional foods. The main aim of this study was to identify the possible anti-inflammatory effects of Distromium decumbens in nasal polyp-derived fibroblasts (NPDFs) and its associated mechanism of action. NPDFs were stimulated by Pseudomonas aeruginosa lipopolysaccharide (PA-LPS) and treated with an ethanolic extract of Distromium decumbens (DDE). The production of interleukin-6 (IL-6) and IL-8 in the supernatant, the phosphorylation of mitogen-activated protein kinase (MAPK) molecules [extracellular signal-related kinase 1/2 (ERK1/2), c-Jun N-terminal kinase and p38 MAPK] and Akt, and the activation of nuclear factor-κB (NF-κB) were assayed in the PA-LPS-stimulated NPDFs untreated or treated with DDE...
October 11, 2017: International Journal of Molecular Medicine
Rosalynn Quiñones, Robbie J Iuliucci, Grayce Behnke, Ryanne Brown, Deben Shoup, Taylor M Riedel, Christine Plavchak, Brooke E Lininger, Jonathan M Spehar
Solid-state nuclear magnetic resonance (SS-NMR) spectroscopy has become a common technique to study polymorphism in pharmaceutical solids at high-resolution. However, high-throughput application of high resolution SS-NMR spectroscopy is severely limited by the long (1)H spin-lattice relaxation (T1) that is common to solid phase compounds. Here, we demonstrate the use of paramagnetic relaxation reagents such as chromium (III) acetylacetonate (Cr(acac)3) and nickel (II) acetylacetonate (Ni(acac)2) for fast data acquisition by significantly reducing the T1 value for carbamazepine Forms I, II, III, and dihydrate, cimetidine Forms A and B, nabumetone Form I, and acetaminophen Form I polymorphs...
October 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
Nicholas C Pflug, Madeline K Hankard, Stephanie M Berg, Meghan O'Connor, James B Gloer, Edward P Kolodziej, David M Cwiertny, Kristine H Wammer
Potent trienone and dienone steroid hormones undergo a coupled photohydration (in light)-thermal dehydration (in dark) cycle that ultimately increases their environmental persistence. Here, we studied the photolysis of dienogest, a dienone progestin prescribed as a next-generation oral contraceptive, and used high resolution mass spectrometry and both 1D and 2D nuclear magnetic resonance spectroscopy to identify its phototransformation products. Dienogest undergoes rapid direct photolysis (t1/2 ∼ 1-10 min), forming complex photoproduct mixtures across the pH range examined (pH 2 to 7)...
November 15, 2017: Environmental Science. Processes & Impacts
Miri Zilka, Simone Sturniolo, Steven P Brown, Jonathan R Yates
In this article, we introduce and apply a methodology, based on density functional theory and the gauge-including projector augmented wave approach, to explore the effects of packing interactions on solid-state nuclear magnetic resonance (NMR) parameters. A visual map derived from a so-termed "magnetic shielding contribution field" can be made of the contributions to the magnetic shielding of a specific site-partitioning the chemical shift to specific interactions. The relation to the established approaches of examining the molecule to crystal change in the chemical shift and the nuclear independent chemical shift is established...
October 14, 2017: Journal of Chemical Physics
Ruge Cao, Yali Zhao, Zhongkai Zhou, Xiaoyu Zhao
BACKGROUND: Hesperidin is a natural product and a strong antioxidant with potential applications in various food and pharmaceutical products. However, its poor water solubility greatly limits its applications. RESULTS: In this study, chitooligosaccharide (COS) was applied to prepare a stable complex with hesperidin (Hesp-COS) via spray-drying method at 100 °C for 20 min. The resultant complex was characterized by Fourier transformation infrared spectroscopy, thermogravimetric analysis, scanning electron microscopy, and proton nuclear magnetic resonance spectroscopy...
October 10, 2017: Journal of the Science of Food and Agriculture
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