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Nuclear pharmaceutical

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https://www.readbyqxmd.com/read/28319010/exploring-protein-peptide-recognition-pathways-using-a-supervised-molecular-dynamics-approach
#1
Veronica Salmaso, Mattia Sturlese, Alberto Cuzzolin, Stefano Moro
Peptides have gained increased interest as therapeutic agents during recent years. The high specificity and relatively low toxicity of peptide drugs derive from their extremely tight binding to their targets. Indeed, understanding the molecular mechanism of protein-peptide recognition has important implications in the fields of biology, medicine, and pharmaceutical sciences. Even if crystallography and nuclear magnetic resonance are offering valuable atomic insights into the assembling of the protein-peptide complexes, the mechanism of their recognition and binding events remains largely unclear...
March 10, 2017: Structure
https://www.readbyqxmd.com/read/28315689/in-silico-prediction-of-hpxr-activators-using-structure-based-pharmacophore-modeling
#2
Nao Torimoto-Katori, Ruili Huang, Harutoshi Kato, Rikiya Ohashi, Menghang Xia
The activation of pregnane X receptor (PXR), a member of the nuclear receptor superfamily, can mediate potential drug-drug interactions by regulating the expression of several drug- mediated enzymes and transporters, resulting in reduced therapeutic efficacy or increased toxicity by producing reactive metabolites. Therefore, in the early stage of drug development, it is important to predict these risks using an in silico approach. We constructed a human PXR (hPXR) pharmacophore model based on known structural information of compounds that activate PXR...
March 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28301521/lysosomal-adaptation-how-cells-respond-to-lysosomotropic-compounds
#3
Shuyan Lu, Tae Sung, Nianwei Lin, Robert T Abraham, Bart A Jessen
Lysosomes are acidic organelles essential for degradation and cellular homoeostasis and recently lysosomes have been shown as signaling hub to respond to the intra and extracellular changes (e.g. amino acid availability). Compounds including pharmaceutical drugs that are basic and lipophilic will become sequestered inside lysosomes (lysosomotropic). How cells respond to the lysosomal stress associated with lysosomotropism is not well characterized. Our goal is to assess the lysosomal changes and identify the signaling pathways that involve in the lysosomal changes...
2017: PloS One
https://www.readbyqxmd.com/read/28300771/inhibitors-of-brd4-protein-from-a-marine-derived-fungus-alternaria-sp-nh-f6
#4
Hui Ding, Dashan Zhang, Biao Zhou, Zhongjun Ma
Bromodomains (BRD) are readers of the epigenetic code that regulate gene transcription through their recognition of acetyl-lysine modified histone tails. Recently, bromodomain-containing proteins such as BRD4 have been demonstrated to be druggable through the discovery of potent inhibitors. These protein-protein interaction inhibitors have the potential to modulate multiple diseases by their profound anti-inflammatory and antiproliferative effects. In order to explore new BRD4 inhibitors as well as lead compounds for the development of new drugs, the secondary metabolites of Alternaria sp...
March 16, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28298102/rotational-spectra-of-two-six-membered-heterocyclic-n-methyl-piperidinol-compounds-conformations-by-oh-rotation-n-methyl-inversion-and-ring-puckering
#5
Javix Thomas, Eric Mariona, Yunjie Xu
Rotational spectra of two nitrogen containing six-membered heterocycles which are commonly used in syntheses of pharmaceuticals, namely, N-methyl-3-piperidinol (NMP3) and N-methyl-4-piperidinol (NMP4), were measured using a broadband chirped pulse and a cavity based Fourier transform microwave spectrometer. The possible conformers due to the OH rotation, N-methyl inversion, and ring puckering were investigated theoretically for these two heterocycles. The substituent position of the hydroxyl group with respective to the N atom in the heterocyclic ring has a strong influence on the preferred conformations...
March 14, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28295588/facilitating-the-performance-of-qnmr-analysisusing-automated-quantification-and-results-verification
#6
Yulia B Monakhova, Bernd W K Diehl
Quantitative nuclear magnetic resonance (qNMR) is considered as a powerful tool for measuring the absolute amount of small molecules in complex mixtures. However, verification of the accuracy of such quantification is not a trivial task. In particular, preprocessing and integration steps are particularly challenging and potentially erroneous.A script was developed in Matlab environment to automate qNMR analysis. Verification of the results is based on two evolving integration profiles. The analysis of binary mixtures of internal standards as well as pharmaceutical products has shown that all common artifacts (phase and baseline distortion, impurities) can be easily recognized in routine qNMR experiments...
March 10, 2017: Magnetic Resonance in Chemistry: MRC
https://www.readbyqxmd.com/read/28295562/locked-nucleic-acid-lna-based-single-stranded-oligonucleotides-are-not-genotoxic
#7
Guérard Melanie, Zeller Andreas, Koller Erich, Marchand Christine, Müller B Martina, Weile Christian, Schuler Franz, Singer Thomas, Tessier Yann
Over the last decade, single stranded oligonucleotides (ON) have gained increased attention as a new drug modality. Because the assessment of genotoxicity risk during early development of pharmaceuticals is essential, we evaluated the potential of locked nucleic acids (LNA)-ONs to induce DNA damage in L5178Y tk(+/-) cells both with the mouse lymphoma assay (MLA) and the micronucleus test (MNT). Further, the MLA was performed to assess gene and chromosome mutation over 3 and 24h (± metabolic activation). In addition, the MNT was performed to assess, in addition, a potential aneugenic liability...
March 10, 2017: Environmental and Molecular Mutagenesis
https://www.readbyqxmd.com/read/28293120/glucocorticoid-receptor-expression-in-20-solid-tumor-types-using-immunohistochemistry-assay
#8
Thaddeus S Block, Tiffany I Murphy, Pamela N Munster, Dat P Nguyen, Frank J Lynch
BACKGROUND: Glucocorticoid receptor (GR) activity plays a role in many aspects of human physiology and may play a crucial role in chemotherapy resistance in a wide variety of solid tumors. A novel immunohistochemistry (IHC) based assay has been previously developed and validated in order to assess GR immunoreactivity in triple-negative breast cancer. The current study investigates the standardized use of this validated assay to assess GR expression in a broad range of solid tumor malignancies...
2017: Cancer Management and Research
https://www.readbyqxmd.com/read/28287743/a-systematic-study-of-molecular-interactions-of-anionic-drugs-with-a-dimethylaminoethyl-methacrylate-copolymer-regarding-solubility-enhancement
#9
Wiebke Saal, Alfred Ross, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
The methacrylate-copolymer Eudragit EPO (EPO) has raised interest in solubility enhancement of anionic drugs. Effects on aqueous drug solubility at rather low polymer concentrations are barely known despite their importance upon dissolution and dilution of oral dosage forms. We provide evidence for substantial enhancement (factor 4-230) of aqueous solubility of poorly water-soluble anionic drugs induced by low (0.1-5% (w/w)) concentration of EPO for a panel of seven acidic crystalline drugs. Diffusion data (determined by (1)H nuclear magnetic resonance spectroscopy) indicate that the solubility increasing effect monitored by quantitative ultraperformance liquid chromatography was caused primarily by molecular API polymer interactions in the bulk liquid phase...
March 21, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28287131/separation-of-nuclear-isomers-for-cancer-therapeutic-radionuclides-based-on-nuclear-decay-after-effects
#10
R Bhardwaj, A van der Meer, S K Das, M de Bruin, J Gascon, H T Wolterbeek, A G Denkova, P Serra-Crespo
(177)Lu has sprung as a promising radionuclide for targeted therapy. The low soft tissue penetration of its β(-) emission results in very efficient energy deposition in small-size tumours. Because of this, (177)Lu is used in the treatment of neuroendocrine tumours and is also clinically approved for prostate cancer therapy. In this work, we report a separation method that achieves the challenging separation of the physically and chemically identical nuclear isomers, (177m)Lu and (177)Lu. The separation method combines the nuclear after-effects of the nuclear decay, the use of a very stable chemical complex and a chromatographic separation...
March 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28274662/pharmaceutical-properties-of-two-ethenzamide-gentisic-acid-cocrystal-polymorphs-drug-release-profiles-spectroscopic-studies-and-theoretical-calculations
#11
Agnieszka Sokal, Edyta Pindelska, Lukasz Szeleszczuk, Waclaw Kolodziejski
The aim of this study was to evaluate the stability and solubility of the polymorphic forms of the ethenzamide (ET) - gentisic acid (GA) cocrystals during standard technological processes leading to tablet formation, such as compression and excipient addition. In this work two polymorphic forms of pharmaceutical cocrystals (ETGA) were characterized by (13)C and (15)N solid-state nuclear magnetic resonance and Fourier transformed infrared spectroscopy. Spectroscopic studies were supported by gauge including projector augmented wave (GIPAW) calculations of chemical shielding constants...
March 6, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28263824/suppressive-immunoregulatory-effects-of-three-antidepressants-via-inhibition-of-the-nuclear-factor-%C3%AE%C2%BAb-activation-assessed-using-primary-macrophages-of-carp-cyprinus-carpio
#12
Wenhui Qiu, Minghong Wu, Shuai Liu, Bei Chen, Chenyuan Pan, Ming Yang, Ke-Jian Wang
Antidepressants, having been applied for the treatment of major depressive disorder and other conditions for decades, are among the most commonly detected human pharmaceuticals in the aquatic environment. This study evaluated the immunotoxicity of acute exposure to environmentally relevant concentrations of amitriptyline, fluoxetine and mianserin using an in vitro primary macrophage model isolated from red common carp (Cyprinus carpio), and also explored their potential mechanisms of action. A potential suppressive immunoregulatory effect of antidepressant exposure was suggested based on the observed suppressive effects on oxidative stress parameters, bactericidal activity, NO production, and NO synthase activity, as well as pro-inflammatory cytokine gene expression, and a significant stimulatory effect on anti-inflammatory interleukin-10 and interferon cytokine gene expression and ATPase activities in macrophages after 6h-exposure to three individual antidepressants and a combination thereof...
March 3, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28256039/biotransformation-of-ginsenoside-rb1-to-ginsenoside-rg3-by-endophytic-bacterium-burkholderia-sp-ge-17-7-isolated-from-panax-ginseng
#13
Yu Fu, Zhenhao Yin, Chengri Yin
AIMS: To isolate a novel endophytic bacteriums from Panax ginseng that could have excellent properties on converting ginsenoside Rb1 to ginsenoside Rg3. METHODS AND RESULTS: Based on 16S rDNA gene sequence, the strain named GE 17-7 was identified as Burkholderia sp. This strain have showed the highest activity in convertion ginsenosides Rb1 into 20(S)-ginsenoside Rg3. During the biotransformation of ginsenoside Rb1, the final metabolite was identified by Nuclear Magnetic Resonance (NMR) analysis and the transformation pathway of ginsenoside Rb1 was also identified by Thin-layer chromatography (TLC) and high performance liquid chromatography (HPLC) analysis in this study...
March 3, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28238082/a-novel-bicistronic-expression-system-composed-of-the-intraflagellar-transport-protein-gene-ift25-and-fmdv-2a-sequence-directs-robust-nuclear-gene-expression-in-chlamydomonas-reinhardtii
#14
Bin Dong, He-He Hu, Zhen-Fang Li, Rong-Qiang Cheng, De-Mei Meng, Junping Wang, Zhen-Chuan Fan
Chlamydomonas reinhardtii offers a great promise for large-scale production of multiple recombinant proteins of pharmaceutical and industrial interest. However, the nuclear-encoding transgenes usually are expressed at a low level, which severely hampers the use of this alga in molecular farming. In this study, the promoter of the endogenous intraflagellar transport 25 (IFT25) gene of C. reinhardtii was tested for its ability to drive the expression of green fluorescent protein (GFP), which functions as a readout for target gene expression...
February 25, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28236763/palmatine-inhibits-trif-dependent-nf-%C3%AE%C2%BAb-pathway-against-inflammation-induced-by-lps-in-goat-endometrial-epithelial-cells
#15
Baoqi Yan, Dongsheng Wang, Shuwei Dong, Zhangrui Cheng, Lidong Na, Mengqi Sang, Hongzao Yang, Zhiqiang Yang, Shidong Zhang, Zuoting Yan
Palmatine, a natural pharmaceutical drug, possesses many biological activities. But its clinical application is rarely reported in the veterinary medicine. The aim of this study was to investigate the anti-inflammatory effects of palmatine on lipopolysaccharide (LPS)-induced inflammation in goat endometrial epithelial cells (gEECs), and the possible molecular mechanisms. Palmatine cell toxicity was determined by MTT assay, and the production of inflammatory cytokine in the cultured medium was measured with ELISA, qRT-PCR and Western blotting...
February 21, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28231139/evaluation-of-the-bitterness-masking-effect-of-powdered-roasted-soybeans
#16
Yoshimasa Makita, Tomoko Ishida, Noriko Kobayashi, Mai Fujio, Kyoko Fujimoto, Rina Moritomo, Jun-Ichi Fujita, Shin-Ichi Fujiwara
The masking of bitterness is considered important because many pharmaceutical compounds have a bitter taste. The bitterness-masking effect of powdered roasted soybeans (PRS) was investigated using a bitter taste sensor. PRS was revealed to significantly suppress the bitterness of quinine hydrochloride and denatonium benzoate. Furthermore, the bitterness-masking mechanism of PRS extracts was evaluated using dynamic light scattering. These results showed that the extracted suspension consisted of particles that were several hundreds of nanometers in size...
June 18, 2016: Foods (Basel, Switzerland)
https://www.readbyqxmd.com/read/28215508/biocatalyst-mediated-production-of-11-15-dihydroxy-derivatives-of-androst-1-4-dien-3-17-dione
#17
Yuqian Qiao, Yanbing Shen, Wei Huang, Yanping Wang, Jiajia Ren, Ting Xia, Min Wang
Hydroxylation of steroids at various positions is a powerful tool for the production of valuable pharmaceutical ingredients and precursors. Our paper reported the synchronous dihydroxylation of an efficient strain, i.e., Colletotrichum lini AS3.4486, at two points. C. lini AS3.4486 was selected from 10 strains; this strain can catalyze the dihydroxylation of androst-1,4-dien-3,17-dione at C-11α and C-15α positions. Transformation of ADD(I) by C. lini AS3.4486 produced metabolites II-IV. The structures of these compounds were elucidated by liquid chromatography-mass spectrometry (LC-MS), Fourier Transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), and X-ray as 15-hydroxyandrost-1,4-dien-3,17-dione (15α-OH-ADD; II), 11,15-dihydroxyandrost-1,4-dien-3,17-dione (11,15-diOH-ADD; III), and 15,17β-dihy-droxyandrost-1,4-dien-3-one (15-OH-BD; BD is the abbreviation of boldenone; IV)...
February 17, 2017: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/28214672/evaluation-of-molecular-chaperone-drug-function-regorafenib-and-%C3%AE-cyclodextrins
#18
Xiurong Hu, Mengying Sun, Yang Li, Guping Tang
Regorafenib (RG) was an oral multi-kinase inhibitor with poor water solubility. In order to enhance the drug's solubility, dissolution and bioavailability, the binary molecular chaperone drug between RG and β-cyclodetrin (β-CD) had prepared by co-crystallization. The structure of RG-β-CD was characterized by thermal analysis, powder X-ray diffraction, infrared spectroscopy and nuclear magnetic resonance. Phase-solubility study revealed the higher solubility and complexing ability of β-CDwith RG.The solubility and dissolution of RG-β-CD was significantly enhanced in pH 1...
February 7, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28208662/characterization-molecular-docking-and-in-vitro-dissolution-studies-of-solid-dispersions-of-20-s-protopanaxadiol
#19
Qi Zhang, Yiqiong Pu, Bing Wang, Yuqin Wang, Tina Tingxia Dong, Tao Guo, Tong Zhang, Zhenzhen Cai
In this study, we prepared solid dispersions (SDs) of 20(S)-protopanaxadiol (PPD) using a melting-solvent method with different polymers, in order to improve the solubility and dissolution performance of drugs with poor water solubility. The SDs were characterized via differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), and molecular docking and dynamics study. DSC and PXRD results indicated that PPD crystallinity in SDs was significantly reduced, and that the majority of PPD is amorphous...
February 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28199101/fungal-identification-using-molecular-tools-a-primer-for-the-natural-products-research-community
#20
Huzefa A Raja, Andrew N Miller, Cedric J Pearce, Nicholas H Oberlies
Fungi are morphologically, ecologically, metabolically, and phylogenetically diverse. They are known to produce numerous bioactive molecules, which makes them very useful for natural products researchers in their pursuit of discovering new chemical diversity with agricultural, industrial, and pharmaceutical applications. Despite their importance in natural products chemistry, identification of fungi remains a daunting task for chemists, especially those who do not work with a trained mycologist. The purpose of this review is to update natural products researchers about the tools available for molecular identification of fungi...
February 15, 2017: Journal of Natural Products
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