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https://www.readbyqxmd.com/read/28231139/evaluation-of-the-bitterness-masking-effect-of-powdered-roasted-soybeans
#1
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
#2
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
#3
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
#4
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
#5
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
https://www.readbyqxmd.com/read/28179150/transporter-mediated-nuclear-entry-of-jasmonoyl-isoleucine-is-essential-for-jasmonate-signaling
#6
Qingqing Li, Jian Zheng, Shuaizhang Li, Guanrong Huang, Stephen J Skilling, Lijian Wang, Ling Li, Mengya Li, Lixing Yuan, Pei Liu
To control gene expression directly by hormone concentrations, both animal and plant cells have exploited comparable mechanisms to sense small molecular hormones in nucleus. Whether nuclear entry of these hormones is actively transported or passively diffused, as conventionally postulated, through nuclear pore complex remains enigmatic. Here, we identified and characterized a jasmonate transporter in Arabidopsis thaliana, AtJAT1/ AtABCG16, which exhibits an unexpected dual localization in the nuclear envelope and plasma membrane...
February 4, 2017: Molecular Plant
https://www.readbyqxmd.com/read/28177407/transformation-of-sulfonamides-and-tetracyclines-during-anaerobic-fermentation-of-liquid-manure
#7
Astrid Spielmeyer, Franziska Stahl, Madeleine S Petri, Walter Zerr, Hubertus Brunn, Gerd Hamscher
Liquid manure is frequently used as soil fertilizer due to its high nutrient content. It can also contain residues of pharmaceuticals, such as antibiotics, if farm animals are medicated. The anaerobic fermentation process in biogas plants is discussed as one way to reduce the input of antibiotics into the environment. Therefore, 10 worldwide-applied sulfonamides (sulfachloropyridazine, sulfadiazine, sulfadimethoxine, sulfaguanidine, sulfamerazine, sulfamethazine, sulfamethoxazole, sulfamethoxypyridazine, sulfapyridine, and sulfathiazole) and four frequently used tetracyclines (chlortetracycline, doxycycline, oxytetracycline, and tetracycline) were investigated concerning their elimination pattern during anaerobic fermentation...
January 2017: Journal of Environmental Quality
https://www.readbyqxmd.com/read/28170315/cytoplasmic-irradiation-induces-metabolic-shift-in-human-small-airway-epithelial-cells-via-activation-of-pim-1-kinase
#8
Jinhua Wu, Qin Zhang, Yen-Ruh Wuu, Sirui Zou, Tom K Hei
The unique cellular and molecular consequences of cytoplasmic damage caused by ionizing radiation were studied using a precision microbeam irradiator. Our results indicated that targeted cytoplasmic irradiation induced metabolic shift from an oxidative to glycolytic phenotype in human small airway epithelial cells (SAE). At 24 h postirradiation, there was an increase in the mRNA expression level of key glycolytic enzymes as well as lactate secretion in SAE cells. Using RNA-sequencing analysis to compare genes that were responsive to cytoplasmic versus nuclear irradiation, we found a glycolysis related gene, Pim-1, was significantly upregulated only in cytoplasmic irradiated SAE cells...
February 7, 2017: Radiation Research
https://www.readbyqxmd.com/read/28163224/stem-cell-extracellular-vesicles-as-drug-delivery-systems-new-frontiers-for-silk-curcumin-nanoparticles
#9
Sara Perteghella, Barbara Crivelli, Laura Catenacci, Milena Sorrenti, Giovanna Bruni, Vittorio Necchi, Barbara Vigani, Marzio Sorlini, Maria Luisa Torre, Theodora Chlapanidas
The aim of this work was to develop a novel carrier-in-carrier system based on stem cell-extracellular vesicles loaded of silk/curcumin nanoparticles by endogenous technique. Silk nanoparticles were produced by desolvation method and curcumin has been selected as drug model because of its limited water solubility and poor bioavailability. Nanoparticles were stable, with spherical geometry, 100nm in average diameter and the drug content reached about 30%. Cellular uptake studies, performed on mesenchymal stem cells (MSCs), showed the accumulation of nanoparticles in the cytosol around the nuclear membrane, without cytotoxic effects...
February 2, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28131079/-1-h-nmr-based-metabolomics-reveals-sub-lethal-toxicity-of-a-mixture-of-diabetic-and-lipid-regulating-pharmaceuticals-on-amphibian-larvae
#10
Steven D Melvin, Leesa J Habener, Frederic D L Leusch, Anthony R Carroll
Pharmaceuticals are widely used for the treatment of various physical and psychological ailments. Due to incomplete removal during sewage treatment many pharmaceuticals are frequently detected in aquatic waterways at trace concentrations. The diversity of pharmaceutical contaminants and potential for complex mixtures to occur makes it very difficult to predict the toxicity of these compounds on wildlife, and robust methods are therefore needed to explore sub-lethal effects. Metabolic syndrome is one of the most widespread health concerns currently facing the human population, and various drugs, including anti-diabetic medications and lipid- and cholesterol-lowering fibrates and statins, are widely prescribed as treatment...
March 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28128839/proanthocyanidins-purified-from-fruit-pericarp-of-clausena-lansium-lour-skeels-as-efficient-tyrosinase-inhibitors-structure-evaluation-inhibitory-activity-and-molecular-mechanism
#11
Wei-Ming Chai, Mei-Zhen Lin, Hui-Ling Feng, Zheng-Rong Zou, Ying-Xia Wang
Fruit pericarp of Clausena lansium (Lour.) Skeels, a food waste, was selected as a raw material for proanthocyanidins. The proanthocyanidins' structures were integrally analyzed using three methods: matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS), high performance liquid chromatography electrospray ionization mass spectrometry (HPLC-ESI-MS) and (13)C nuclear magnetic resonance (NMR). The results elucidated that these compounds were composed of prodelphinidin (75%) and procyanidin (25%) with a degree of polymerization (DP) up to the 20-mers...
January 27, 2017: Food & Function
https://www.readbyqxmd.com/read/28118570/conductive-polymeric-ionic-liquid-fe3o4-nanocomposite-as-an-efficient-catalyst-for-the-voltammetric-determination-of-amlodipine-besylate
#12
Fariba Fathirad, Ali Mostafavi, Daryoush Afzali
A novel conductive polymeric ionic liquid (IL)-Fe<sub>3</sub>O<sub>4</sub> nanocomposite (represented as PIL-Fe<sub>3</sub>O<sub>4</sub>) based on inorganic-organic hybrid material was synthesized using two different methods. Nuclear magnetic resonance, Fourier transform infrared, X-ray diffraction, and field emission scanning electron microscopy characterized the structures of IL, Fe<sub>3</sub>O<sub>4</sub> nanoparticles, and PIL-Fe<sub>3</sub>O<sub>4</sub>...
December 20, 2016: Journal of AOAC International
https://www.readbyqxmd.com/read/28110685/a-multi-analytical-approach-to-better-assess-the-keratan-sulfate-contamination-in-animal-origin-chondroitin-sulfate
#13
Odile Francesca Restaino, Rosario Finamore, Paola Diana, Mariacarmela Marseglia, Mario Vitiello, Angela Casillo, Emiliano Bedini, Michelangelo Parrilli, Maria Michela Corsaro, Marco Trifuoggi, Mario De Rosa, Chiara Schiraldi
Chondroitin sulfate is a glycosaminoglycan widely used as active principle of anti-osteoarthritis drugs and nutraceuticals, manufactured by extraction from animal cartilaginous tissues. During the manufacturing procedures, another glycosaminoglycan, the keratan sulfate, might be contemporarily withdrawn, thus eventually constituting a contaminant difficult to be determined because of its structural similarity. Considering the strict regulatory rules on the pureness of pharmaceutical grade chondrotin sulfate there is an urgent need and interest to determine the residual keratan sulfate with specific, sensitive and reliable methods...
March 15, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28068097/characterization-of-phase-separation-propensity-for-amorphous-spray-dried-dispersions
#14
Daniel McNamara, Shawn Yin, Duohai Pan, George Crull, Peter Timmins, Balvinder Vig
A generalized screening approach, applying isothermal calorimetry at 37 °C 100% RH, to formulations of spray dried dispersions (SDDs) for two active pharmaceutical ingredients (APIs) (BMS-903452 and BMS-986034) is demonstrated. APIs 452 and 034, with similar chemotypes, were synthesized and promoted during development for oral dosing. Both APIs were formulated as SDDs for animal exposure studies using the polymer hydroxypropylmethlycellulose acetyl succinate M grade (HPMCAS-M). 452 formulated at 30% (wt/wt %) was an extremely robust SDD that was able to withstand 40 °C 75% RH open storage conditions for 6 months with no physical evidence of crystallization or loss of dissolution performance...
January 20, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28062541/evaluation-of-a-novel-renewable-hepatic-cell-model-for-prediction-of-clinical-cyp3a4-induction-using-a-correlation-based-ris-approach
#15
Rongjun Zuo, Feng Li, Sweta Parikh, Li Cao, Kirsten L Cooper, Yulong Hong, Jin Liu, Ronald A Faris, Daochuan Li, Hongbing Wang
Metabolism enzyme induction-mediated drug-drug interactions need to be carefully characterized in vitro for drug candidates in order to predict in vivo outcomes of safety risk and therapeutic efficiency. Currently, both the FDA and EMA recommend using primary human hepatocytes as the "Gold Standard" in vitro test system for studying the induction potential of candidate drugs on cytochrome P450 (CYP), CYP3A4, CYP1A2, and CYP2B6. However, primary human hepatocytes are known to bear inherent limitations such as limited supply and large lot-to-lot variations which result in an experimental burden to qualify new lots...
January 6, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28049248/nestin-expression-in-the-adult-mouse-retina-with-pharmaceutically-induced-retinal-degeneration
#16
Chan Hee Moon, Heeyoon Cho, Yoon Kyung Kim, Tae Kwann Park
The present study investigated the temporal pattern and cellular localization of nestin in the adult mouse retina with pharmaceutically induced retinal degeneration using N-methyl-N-nitrosourea (MNU). After a single intraperitoneal injection of MNU in 8-week-old C57BL/6 mice, the animals were sacrificed at 1, 3, 5, 7, and 21 days (n = 6, in each stage). The eyes were examined by means of immunohistochemical tests using nestin, ionized calcium-binding adaptor molecule (Iba-1), CD11b, F4/80, and glial fibrillary acidic protein (GFAP)...
February 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/28025997/a-novel-chk1-binding-peptide-that-enhances-genotoxic-sensitivity-through-the-cellular-redistribution-of-nuclear-chk1
#17
Kwang Seok Kim, Kyu Jin Choi, Sangwoo Bae
Since checkpoint kinase 1 (Chk1) is an essential factor for cell viability following DNA damage, the inhibition of Chk1 has been a major focus of pharmaceutical development to enhance the sensitivity of tumor cells to chemo- and radiotherapy that damage DNA. However, due to the off-target effects of conventional Chk1-targeting strategies and the toxicity of Chk1 inhibitors, alternative strategies are required to target Chk1. To facilitate such efforts, in this study, we identified a specific Chk1-binding 12-mer peptide from the screening of a phage display library and characterized the peptide in terms of cellular cytotoxicity, and in terms of its effect on Chk1 activity and sensitivity to genotoxic agents...
November 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28024262/levothyroxine-sodium-revisited-a-wholistic-structural-elucidation-approach-of-new-impurities-via-hplc-hrms-ms-on-line-h-d-exchange-nmr-spectroscopy-and-chemical-synthesis
#18
M Ruggenthaler, J Grass, W Schuh, C G Huber, R J Reischl
The structural elucidation of unknown pharmaceutical impurities plays an important role in the quality control of newly developed and well-established active pharmaceutical ingredients (APIs). The United States Pharmacopeia (USP) monograph for the API Levothyroxine Sodium, a synthetic thyroid hormone, features two high pressure liquid chromatography (HPLC) methods using UV-VIS absorption detection to determine organic impurities in the drug substance. The impurity profile of the first USP method ("Procedure 1") has already been extensively studied, however for the second method ("Procedure 2"), which exhibits a significantly different impurity profile, no wholistic structural elucidation of impurities has been performed yet...
December 14, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28004818/3-d-microwell-array-system-for-culturing-virus-infected-tumor-cells
#19
Rami El Assal, Umut A Gurkan, Pu Chen, Franceline Juillard, Alessandro Tocchio, Thiruppathiraja Chinnasamy, Chantal Beauchemin, Sebnem Unluisler, Serli Canikyan, Alyssa Holman, Srikar Srivatsa, Kenneth M Kaye, Utkan Demirci
Cancer cells have been increasingly grown in pharmaceutical research to understand tumorigenesis and develop new therapeutic drugs. Currently, cells are typically grown using two-dimensional (2-D) cell culture approaches, where the native tumor microenvironment is difficult to recapitulate. Thus, one of the main obstacles in oncology is the lack of proper infection models that recount main features present in tumors. In recent years, microtechnology-based platforms have been employed to generate three-dimensional (3-D) models that better mimic the native microenvironment in cell culture...
December 22, 2016: Scientific Reports
https://www.readbyqxmd.com/read/28004015/influenza-infection-modulates-vesicular-trafficking-and-induces-golgi-complex-disruption
#20
Vibha Yadav, Antonito T Panganiban, Kerstin Honer Zu Bentrup, Thomas G Voss
Influenza A virus (IFV) replicates its genome in the nucleus of infected cells and uses the cellular protein transport system for genome trafficking from the nucleus to the plasma membrane. However, many details of the mechanism of this process, and its relationship to subsequent cytoplasmic virus trafficking, have not been elucidated. We examined the effect of nuclear transport inhibitors Leptomycin B (LB), 5,6 dichloro-1-β-d-ribofuranosyl-benzimidazole (DRB), the vesicular transport inhibitor Brefeldin A (BFA), the caspase inhibitor ZWEHD, and microtubule inhibitor Nocodazole (NOC) on virus replication and intracellular trafficking of viral nucleoprotein (NP) from the nucleus to the ER and Golgi...
December 2016: Virusdisease
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