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Nuclear pharmaceutical

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https://www.readbyqxmd.com/read/29035811/moving-towards-fast-characterization-of-polymorphic-drugs-by-solid-state-nmr-spectroscopy
#1
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
https://www.readbyqxmd.com/read/29034382/environmental-photochemistry-of-dienogest-phototransformation-to-estrogenic-products-and-increased-environmental-persistence-via-reversible-photohydration
#2
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)...
October 16, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/29031269/visualising-crystal-packing-interactions-in-solid-state-nmr-concepts-and-applications
#3
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
https://www.readbyqxmd.com/read/29023808/enhancement-of-the-water-solubility-and-antioxidant-activity-of-hesperidin-by-chitooligosaccharide
#4
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
https://www.readbyqxmd.com/read/29022618/enhancing-the-resolution-of-1-h-and-13-c-solid-state-nmr-spectra-by-reduction-of-anisotropic-bulk-magnetic-susceptibility-broadening
#5
Michael P Hanrahan, Amrit Venkatesh, Scott L Carnahan, Julie L Calahan, Joseph W Lubach, Eric J Munson, Aaron J Rossini
We demonstrate that natural isotopic abundance 2D heteronuclear correlation (HETCOR) solid-state NMR spectra can be used to significantly reduce or eliminate the broadening of (1)H and (13)C solid-state NMR spectra of organic solids due to anisotropic bulk magnetic susceptibility (ABMS). ABMS often manifests in solids with aromatic groups, such as active pharmaceutical ingredients (APIs), and inhomogeneously broadens the NMR peaks of all nuclei in the sample. Inhomogeneous peaks with full widths at half maximum (FWHM) of ∼1 ppm typically result from ABMS broadening and the low spectral resolution impedes the analysis of solid-state NMR spectra...
October 12, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28992598/global-transcriptomic-analysis-of-zebrafish-in-response-to-embryonic-exposure-to-three-antidepressants-amitriptyline-fluoxetine-and-mianserin
#6
Minghong Wu, Shuai Liu, Lei Hu, Haidong Qu, Chenyuan Pan, Penghui Lei, Yingjia Shen, Ming Yang
Antidepressants are among the most commonly detected pharmaceuticals in aqueous systems, and, as emerging organic pollutants, may exert negative effects on non-target aquatic organisms. Previously, it has been revealed that antidepressant exposure significantly inhibits the growth and development of fish during their early developmental stages. Thus, in the present study, we aimed to identify and compare the underlying mechanisms of action of different antidepressants at the transcriptional level using zebrafish (Danio rerio) embryos...
September 28, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28991760/centenary-of-the-birth-of-academician-prof-dr-isak-tadzer-founder-of-the-pathophysiology-and-nuclear-medicine-in-macedonia
#7
Borislav Karanfilski
Academician Prof. Dr. Isak Tadzer was born a hundred years ago on December 24, 1916 in Sofia. He completed the primary and secondary education at the German College in Sofia. In 1935 he began his studies at the Medical Faculty in Vienna, which he had to stop because of the annexation of Austria to Germany in 1938. He returned to Bulgaria where he continued his studies and graduated from the Medical Faculty in Sofia in 1941. During the War, 1941-1944, he was forcedly mobilized and he worked as a doctor in several villages...
September 1, 2017: Prilozi (Makedonska Akademija Na Naukite i Umetnostite. Oddelenie za Medicinski Nauki)
https://www.readbyqxmd.com/read/28966222/evaluation-for-standardization-of-1-h-quantitative-nuclear-magnetic-resonance-spectroscopy-by-round-robin-test
#8
Toru Miura, Naoki Sugimoto, Ryuichi Watanabe, Takako Suematsu, Yoichiro Takayanagi, Yoshinobu Ito, Naoki Saito, Ryuichi Sawa, Tsuyoshi Kato, Yoshinori Fujimine, Ryo Koike, Yuko Ohfuku, Yuko Yamada, Hiroaki Utsumi, Toshiyuki Suzuki
  (1)H quantitative Nuclear Magnetic Resonance ((1)H qNMR) is known as a powerful tool for determination of analytes without the need for their identical standards, which is eligible to a primary rate method. (1)H qNMR has been already stipulated to an assay for purity determination in Japanese Pharmacopoeia (JP), and then this technique has been also applied in several fields such as pharmaceutical and food sciences. However, there is little information about the accuracy of (1)H qNMR so that the further applications into other fields such as industrial chemistry could be constricted...
September 29, 2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28946185/cytotoxic-effect-of-cyperus-rotundus-rhizome-extract-on-human-cancer-cell-lines
#9
Prabu Mannarreddy, Maghil Denis, Durgadevi Munireddy, Ranjani Pandurangan, Kalaichelvan Puthupalayam Thangavelu, Kaviyarasan Venkatesan
The wild weed Cyperus rotundus is commonly used as traditional medicine in different parts of the world. Sequential extraction of C. rotundus rhizome with solvents of different polarity namely hexane, chloroform, ethyl acetate, methanol and water were prepared and the free radical scavenging activity was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Based on high antioxidant activity of methanolic extract of C. rotundus rhizome (MRCr) was further investigated for its cytotoxic effect on different human cancer cell lines-breast (MCF-7), cervical (HeLa), liver (Hep G2), prostate (PC-3), colorectal (HT-29) and normal cell line (MCF-12A) by 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT) assay evaluated as 50% inhibition of growth (IC50)...
September 19, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28923766/development-of-stability-enhanced-ternary-solid-dispersions-via-combinations-of-hpmcp-and-soluplus-%C3%A2-processed-by-hot-melt-extrusion
#10
Ahmad B Albadarin, Catherine B Potter, Mark T Davis, Javed Iqbal, Sachin Korde, Sudhir Pagire, Anant Paradkar, Gavin Walker
The aim of this study was to evaluate a novel combination of hydroxypropyl methylcellulose phthalate (HPMCP-HP-50) and Soluplus(®) polymers for enhanced physicochemical stability and solubility of the produced amorphous solid dispersions (ASDs). This was achieved using hot melt extrusion (HME) to convert the crystalline active pharmaceutical ingredient (API) into a more soluble amorphous form within the ternary systems. Itraconazole (ITZ), a Biopharmaceutics Classification System class II (BCS II) API, was selected as the model drug...
September 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28922619/identification-of-angiogenesis-inhibitors-using-a-co-culture-cell-model-in-a-high-content-and-high-throughput-screening-platform
#11
Shuaizhang Li, Chia-Wen Hsu, Srilatha Sakamuru, Chaozhong Zou, Ruili Huang, Menghang Xia
Angiogenesis is an important hallmark of cancer, contributing to tumor formation and metastasis. In vitro angiogenesis models for analyzing tube formation serve as useful tools to study these processes. However, current in vitro co-culture models using primary cells have limitations in usefulness and consistency. Therefore, in the present study, an in vitro co-culture assay system was optimized in a 1536-well format for high-throughput screening using human telomerase reverse transcriptase (hTERT)-immortalized mesenchymal stem cells and aortic endothelial cells...
September 1, 2017: SLAS Technology
https://www.readbyqxmd.com/read/28919470/preparation-and-characterization-of-amorphous-ciprofloxacin-amino-acid-salts
#12
Hanah Mesallati, Daryl Conroy, Sarah Hudson, Lidia Tajber
The amorphization of the poorly soluble drug ciprofloxacin (CIP) may be facilitated by the use of a suitable stabilizer. In this study seven amino acids, with various side chain properties, were evaluated in this regard. Solid dispersions were prepared by ball milling 1:1 molar ratios of CIP with the amino acids, and their solid-state and pharmaceutical properties were then examined. Fully X-ray amorphous solid dispersions were obtained with aspartic acid, glutamic acid, cysteine and arginine. In each case, evidence of salt formation between the drug and amino acids was found via Fourier transform infrared spectroscopy and solid-state nuclear magnetic resonance...
September 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28901514/multimodal-actions-of-the-phytochemical-sulforaphane-suppress-both-ar-and-ar-v7-in-22rv1-cells-advocating-a-potent-pharmaceutical-combination-against-castration-resistant-prostate-cancer
#13
Namrata Khurana, Hogyoung Kim, Partha K Chandra, Sudha Talwar, Pankaj Sharma, Asim B Abdel-Mageed, Suresh C Sikka, Debasis Mondal
Prostate cancer (PCa) cells expressing full-length androgen receptor (AR-FL) are susceptible to androgen deprivation therapy (ADT). However, outgrowth of castration-resistant prostate cancer (CRPC) can occur due to the expression of constitutively active (ligand-independent) AR splice variants, particularly AR-V7. We previously demonstrated that sulforaphane (SFN), an isothiocyanate phytochemical, can decrease AR-FL levels in the PCa cell lines, LNCaP and C4-2B. Here, we examined the efficacy of SFN in targeting both AR-FL and AR-V7 in the CRPC cell line, CWR22Rv1 (22Rv1)...
August 30, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28898054/synthesis-radiolabeling-and-characterization-of-plasma-protein-binding-ligands-potential-tools-for-modulation-of-the-pharmacokinetic-properties-of-radio-pharmaceuticals
#14
Cristina Müller, Renáta Farkas, Francesca Borgna, Raffaella M Schmid, Martina Benešová, Roger Schibli
The development of (radio)pharmaceuticals with favorable pharmacokinetic profiles is crucial for allowing the optimization of the imaging or therapeutic potential and the minimization of undesired side effects. The aim of this study was, therefore, to evaluate and compare three different plasma protein binders (PPB-01, PPB-02, and PPB-03) that are potentially useful in combination with (radio)pharmaceuticals to enhance their half-life in the blood. The entities were functionalized with a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator via a l-lysine and β-alanine linker moiety using solid-phase peptide chemistry and labeled with (177)Lu (T1/2 = 6...
September 20, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28891958/the-application-of-quantitative-%C3%A2-h-nmr-for-the-determination-of-orlistat-in-tablets
#15
Shanshan Sun, Mengxia Jin, Xia Zhou, Jinghua Ni, Xiangju Jin, Hongyue Liu, Yinghong Wang
A quantitative nuclear magnetic resonance (qNMR) method to measure the content of Orlistat in tablets was studied and found to be efficient, accurate, reliable, and simple. In this paper, phloroglucinolanhydrous and dimethylsulfoxide-d₆ (DMSO-d₆) served as the internal standard and solvent, respectively. The qNMR methodology, including the linearity, range, the limit of detection (LOD) and quantification (LOQ), stability, precision, and accuracy, was validated seriatim, and the results were very favorable...
September 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28891335/development-of-dna-tetrahedron-based-drug-delivery-system
#16
Yue Hu, Zhou Chen, He Zhang, Mingkai Li, Zheng Hou, Xiaoxing Luo, Xiaoyan Xue
Nanocarriers of drugs have attracted significant attention to tackle the problems of drug resistance or nucleic acid drug delivery, which can optimize pharmaceutical parameters and enhance the cellular uptake efficiency. Nowadays, DNA nanostructure presents an opportunity in the field of nanomaterial due to its precise control in shape and size, excellent biocompatibility, as well as multiple sites for targeting decoration. DNA tetrahedron, which is stable and easily synthesized, is used for various applications, including nuclear magnetic resonance imaging, molecular diagnosis, targeting drug delivery, and so on...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28890206/unraveling-the-nuclear-and-chloroplast-genomes-of-an-agar-producing-red-macroalga-gracilaria-changii-rhodophyta-gracilariales
#17
Chai-Ling Ho, Wei-Kang Lee, Ee-Leen Lim
Agar and agarose have wide applications in food and pharmaceutical industries. Knowledge on the genome of red seaweeds that produce them is still lacking. To fill the gap in genome analyses of these red algae, we have sequenced the nuclear and organellar genomes of an agarophyte, Gracilaria changii. The partial nuclear genome sequence of G. changii has a total length of 35.8Mb with 10,912 predicted protein coding sequences. Only 39.4% predicted proteins were found to have significant matches to protein sequences in SwissProt...
September 7, 2017: Genomics
https://www.readbyqxmd.com/read/28873280/a-biomimetic-escape-strategy-for-cytoplasm-invasion-by-synthetic-particles
#18
Nerea Iturrioz-Rodríguez, Elena González-Domínguez, Eloisa González-Lavado, Laura Marín-Caba, Belén Vaz, Moisés Pérez-Lorenzo, Miguel A Correa-Duarte, Monica L Fanarraga
The translocation of nanomaterials or complex delivery systems into the cytosol is a major challenge in nanobiotechnology. After receptor-mediated endocytosis, most nanomaterials are sequestered and undergo degradation, therapy inactivation, or exocytosis. Herein we explore a novel surface particle coating made of adsorbed carbon nanotubes that provides coated materials with new properties that reproduce the viral cell-invasive mechanisms, namely, receptor-mediated endocytosis, endolysosomal escape, and cytosolic particle release preserving cell viability...
September 5, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28872126/application-and-methodology-of-the-non-destructive-19f-time-domain-nmr-technique-to-measure-the-content-in-fluorine-containing-drug-products
#19
Maria Victoria Silva Elipe, Lan Li, Karthik Nagapudi, Alan M Kook, Carlos Cobas, Isaac Iglesias, Chen Peng
Here, we describe a protocol developed by our group that uses low-field fluorine-19 ((19)F) time-domain (TD) nuclear magnetic resonance (NMR) to measure the average content of fluorinated drugs in their formulated drug product forms: tablets or capsules. This method is specific to fluorinated drugs because it detects only the content of fluorine, avoiding interference from the excipients that lack fluorine. The advantages of measuring the active content of fluorinated drugs using low-field (19)F TD-NMR versus high-field (19)F solid-state (SS) NMR are the simplicity of the method; the low cost; and the non-destructive nature of the technique, with all samples recoverable in intact forms (e...
August 22, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28858907/nucleoligands-repurposing-gpcr-ligands-to-modulate-nuclear-localized-gpcrs-in-the-cardiovascular-system
#20
Nicolas Audet, Rabah Dabouz, Bruce G Allen, Terence E Hébert
There is significant evidence that internal pools of GPCRs exist and may be affected by both endogenous signaling molecules and hydrophobic pharmaceutical ligands, once assumed to only affect cell surface versions of these receptors. Here, we discuss evidence that the biology of nuclear GPCRs in particular is complex, rich and highly interactive with GPCR signalling from the cell surface. Caging existing GPCR ligands may be an excellent means of further stratifying the phenotypic effects of known pharmacophores such as β-adrenergic, angiotensin II and type B endothelin receptor ligands in the cardiovascular system...
August 29, 2017: Journal of Cardiovascular Pharmacology
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