gebhart/patrepeval huggingface dataset:
Methacrylate-Copolymer Eudragit EPO as a Solubility-Enabling Excipient for Anionic Drugs: Investigation of Drug Solubility, Intestinal Permeability, and Their Interplay (2019)

The purpose of this work was to investigate the use of the dimethylaminoethyl methacrylate-copolymer Eudragit EPO (EPO) in oral solubility-enabling formulations for anionic lipophilic drugs, aiming to guide optional formulation design and maximize oral bioavailability. We have studied the solubility, the permeability, and their interplay, using the low-solubility nonsteroidal anti-inflammatory drug mefenamic acid as a model drug. Then, we studied the biorelevant solubility enhancement of mefenamic acid from EPO-based formulations throughout the gastrointestinal tract (GIT), using the pH-dilution dissolution method. EPO allowed a profound and linear solubility increase of mefenamic acid, from 10 μg/mL without EPO to 9.41 mg/mL in the presence of 7.5% EPO (∼940-fold; 37 °C); however, a concomitant decrease of the drug permeability was obtained, both in vitro and in vivo in rats, indicating a solubility-permeability trade-off. In the absence of an excipient, the unstirred water layer (UWL) adjacent to the GI membrane was found to hinder the permeability of the drug, accounting for this UWL effect and revealing that the true membrane permeability allowed good prediction of the solubility-permeability trade-off as a function of EPO level using a direct relationship between the increased solubility afforded by a given EPO level and the consequent decreased permeability. Biorelevant dissolution studies revealed that EPO levels of 0.05 and 0.1% were insufficient to dissolve mefenamic acid dose during the entire dissolution time course, whereas 0.5 and 1% EPO allowed complete solubility with no drug precipitation. In conclusion, EPO may serve as a potent solubility-enabling excipient for BCS class II/IV acidic drugs; however, it should be used carefully. It is prudent to use the minimal EPO amounts just sufficient to dissolve the drug dose throughout the GIT and not more than that. Excess amounts of EPO provide no solubility gain and cause further permeability loss, jeopardizing the overall success of the formulation. This work may help the formulator to hit the optimal solubility-permeability balance, maximizing the oral bioavailability afforded by the formulation.
ChemInform Abstract: Asymmetric Oxidation of Ketones (2002)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Ruthenium tetraoxide phase-transfer-promoted oxidation of secondary alcohols to ketones (1987)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRuthenium tetraoxide phase-transfer-promoted oxidation of secondary alcohols to ketonesPhilip E. Morris Jr. and Donald E. KielyCite this: J. Org. Chem. 1987, 52, 6, 1149–1152Publication Date (Print):March 1, 1987Publication History Published online1 May 2002Published inissue 1 March 1987https://pubs.acs.org/doi/10.1021/jo00382a035https://doi.org/10.1021/jo00382a035research-articleACS PublicationsRequest reuse permissionsArticle Views627Altmetric-Citations61LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Security algorithms in wireless LAN: proprietary or nonproprietary (2004)

Wireless LANs in business and for personal use are becoming common. However, many issues are impeding further adoption of the technology by end-users, in particular the inability or difficulty in providing adequate security between the networks and users. The two issues limiting wider acceptance are Authentication and Encryption. The IEEE 802.1x standard provides a framework for authentication of LAN users, while at the same time providing a base for sophisticated key management procedures. This paper aims to document these issues by comparing proprietary and nonproprietary Authentication and Encryption measures and listing the advantages and disadvantages of each type.
The nature and origin of amyloid fibrils (1996)

The Molecular Structure of Famililal Amyloidotic Polyneuropathy Amyloid Fibrils Refined Fibril Structures: The Hydrophobic Core in Alzheimer's (-amyloid and Prion as Revealed by X-ray Diffraction Modulating Factors in Transthyretin Amyloid Proteoglycans and Amyloid Fibrillogenesis Molecular Mechanisms of Fibrillogenesis and the Protective Role of Amyloid P Component - Two Possible Avenues for Therapy Metabolism of Amyloid Proteins Alzheimer's Disease: Genesis of Amyloid in vivo and in vitro Amyloidogenesis and Apolipoproteins Sequestration of Amyloid ( Protein and Prevention of Amyloid Formation Amyloid and Polymers of the Scarpie Prion Protein Ageing and Fibrillogenesis - Lessons from Apolipoprotein A-1, Transthyretin and Islet Amyloid Polypeptide The Mechanisms of Transthyretin Amyloid Fibril Formation.
JENNA: a jamming evasive network-coding neighbor-discovery algorithm for cognitive radio networks [Dynamic Spectrum Management] (2010)

Cognitive radios operate in a particularly challenging wireless environment. Besides the strict requirements imposed by opportunistic coexistence with licensed users, cognitive radios may have to deal with other concurrent (either malicious or selfish) cognitive radios that aim at gaining access to the available spectrum resources with no regard to fairness or other behavioral etiquettes. By taking advantage of their highly flexible RF front-ends, they are able to mimic a licensed user's behavior or simply jam a given channel with high power. This way these concurrent users (jammers) are capable of interrupting or delaying the neighbor discovery process initiated by a cognitive radio, which is interested in using a portion of the available spectrum for its own data communications. To solve this problem we propose a Jamming Evasive Network-coding Neighbor-Discovery Algorithm (JENNA), which ensures complete neighbor discovery for a cognitive radio network in a distributed and asynchronous way. We compare the proposed algorithm with baseline schemes that represent existing solutions, and validate its feasibility in a single-hop cognitive radio network.
Identification and characterization of human myocardial phospholipase A2 from transplant recipients suffering from end-stage ischemic heart disease. (1992)

Although numerous studies have implicated accelerated phospholipid catabolism during myocardial ischemia as an important contributor to ischemic membrane dysfunction, no information is currently available on the subcellular distribution, physical properties, or kinetic characteristics of human myocardial phospholipase A2. In this report, we demonstrate that the overwhelming majority (98%) of total phospholipase A2 activity in human myocardium (obtained from transplant recipients) is calcium independent, plasmalogen selective, and is distributed between the microsomal (60-70% of total activity) and cytosolic (30-40% of total activity) fractions. Both human myocardial microsomal and cytosolic phospholipase A2 enzymes 1) preferentially hydrolyze plasmalogen molecular species containing arachidonic acid at the sn-2 position, 2) are recalcitrant to chemical inactivation by the indole-reactive agent parabromophenacyl bromide, 3) are irreversibly inhibited by covalent modification of an essential thiol residue by 5,5'-dithio-bis(2-nitrobenzoic acid) (DTNB), and 4) are exquisitely sensitive to mechanism-based inhibition by (E)-6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one (bromoenol lactone). In sharp contrast, human mitochondrial phospholipase A2 1) accounts for only a diminutive amount of total myocardial phospholipase A2 activity (1-2%), 2) is augmented by calcium ion, 3) exhibits a higher reaction velocity using phosphatidylcholine in comparison with plasmenylcholine substrate, and 4) is not substantially inhibited by either DTNB or bromoenol lactone. Collectively, these results demonstrate that the majority of phospholipase A2 activity in human myocardium is catalyzed by a novel class of calcium-independent plasmalogen-selective phospholipases A2 and underscore the potential importance of this class of enzymes in mediating membrane dysfunction during myocardial infarction in humans.
Evaluation of various NIR instruments for estimating grain quality for livestock (2005)

A large national research project in Australia over the past seven years has focused on improving the quality of grains for feeding to livestock. A major expectation of the grain and livestock industries from this project is the adoption of rapid and objective analytical tests for relevant quality criteria of grains, preferably at the point of delivery. NIR spectroscopy obviously has a key role, and calibrations have been derived, or attempted, for 52 different chemical and physical properties, several in vitro or in sacco tests, and in vivo digestibility or energy content for ruminants [1 - 3], pigs and poultry. Final calibrations were developed using over 100 grains, either whole or ground, which were scanned on laboratory-based grating monochromators, namely Foss-NIRSystems models 6500 or 5000 instruments. However, the industry has requested that the appropriate NIR spectroscopy testing procedures be made available on simpler, cheaper and as such, often older, spectrometers. This presents a real challenge for calibration transfer, given the differences in optical configuration, spectral range, sample presentation and software packages among the instrument types. Some instruments also target specific applications and constituents. Due to the nature of many of the tests of interest in this project, it was a difficult task to make direct and fair comparisons between NIR spectrometers in the market-place. The purpose of this study was to compare the accuracy of some NIR spectrometers for estimation of selected indicators of feed grain quality, using whole grain samples.
Tracking Vector Magnetograms with the Magnetic Induction Equation (2008)

The differential affine velocity estimator (DAVE) developed in Schuck (2006) for estimating velocities from line-of-sight magnetograms is modified to directly incorporate horizontal magnetic fields to produce a differential affine velocity estimator for vector magnetograms (DAVE4VM). The DAVE4VM's performance is demonstrated on the synthetic data from the anelastic pseudospectral ANMHD simulations that were used in the recent comparison of velocity inversion techniques by Welsch (2007). The DAVE4VM predicts roughly 95% of the helicity rate and 75% of the power transmitted through the simulation slice. Inter-comparison between DAVE4VM and DAVE and further analysis of the DAVE method demonstrates that line-of-sight tracking methods capture the shearing motion of magnetic footpoints but are insensitive to flux emergence -- the velocities determined from line-of-sight methods are more consistent with horizontal plasma velocities than with flux transport velocities. These results suggest that previous studies that rely on velocities determined from line-of-sight methods such as the DAVE or local correlation tracking may substantially misrepresent the total helicity rates and power through the photosphere.
The use of seawater-neutralised bauxite refinery residues (red mud) in environmental remediation programs (1999)

Seawater-neutralised bauxite refinery residues (red mud) have a very high trace metal trapping capacity (>1000 meq/kg), and a high acid neutralisation capacity (≈3.5 moles/kg) that is due to an abundance of amorphous and finely crystalline phases that form weak bases; trace metals bound to the red mud can not be readily leached off. These properties make the seawater-neutralised red mud suitable for treating acid mine drainage, tailings pond waters, and acid sulphate soils; there are also other potential uses. The red mud can be mixed with contaminated liquids or solids, or used to form permeable subsurface barriers that will not impede subsurface water flow but will neutralise any acid and strip trace metals from contaminated water before it reaches natural waterways. This paper describes the properties of seawater-neutralised red mud and the results of trials involving its use in environmental management and remediation applications.
Impact of TASK-1 in Human Pulmonary Artery Smooth Muscle Cells (2006)

The excitability of pulmonary artery smooth muscle cells (PASMC) is regulated by potassium (K+) conductances. Although studies suggest that background K+ currents carried by 2-pore domain K+ channels are important regulators of resting membrane potential in PASMC, their role in human PASMC is unknown. Our study tested the hypothesis that TASK-1 leak K+ channels contribute to the K+ current and resting membrane potential in human PASMC. We used the whole-cell patch-clamp technique and TASK-1 small interfering RNA (siRNA). Noninactivating K+ current performed by TASK-1 K+ channels were identified by current characteristics and inhibition by anandamide and acidosis (pH 6.3), each resulting in significant membrane depolarization. Moreover, we showed that TASK-1 is blocked by moderate hypoxia and activated by treprostinil at clinically relevant concentrations. This is mediated via protein kinase A (PKA)-dependent phosphorylation of TASK-1. To further confirm the role of TASK-1 channels in regulation of resting membrane potential, we knocked down TASK-1 expression using TASK-1 siRNA. The knockdown of TASK-1 was reflected by a significant depolarization of resting membrane potential. Treatment of human PASMC with TASK-1 siRNA resulted in loss of sensitivity to anandamide, acidosis, alkalosis, hypoxia, and treprostinil. These results suggest that (1) TASK-1 is expressed in human PASMC; (2) TASK-1 is hypoxia-sensitive and controls the resting membrane potential, thus implicating an important role for TASK-1 K+ channels in the regulation of pulmonary vascular tone; and (3) treprostinil activates TASK-1 at clinically relevant concentrations via PKA, which might represent an important mechanism underlying the vasorelaxing properties of prostanoids and their beneficial effect in vivo.
1,2,3-Benzothiadiazoles. Part I. A simplified synthesis of 1,2,3-benzothiadiazoles (1970)

Diazotisation of the benzothiazathiolium salts isolated from the reaction of sulphur monochloride with aromatic amines (Herz reaction) leads to the formation of 1,2,3-benzothiadiazoles. The scope of the reaction is discussed.
Polyuronide Degradation and Hemicellulose Modifications in Ripening Tomato Fruit (1983)

Abstract Hemicelluloses and polyuronides from the cell wall of ripening tomato ( Lycopersicon esculentum Mill. cv. Rutgers) fruit were examined using gel-filtration chromatography. Gel filtration of polyuronides revealed that these polymers were extensively degraded during ripening, as evidenced by the increase in the quantity of polymers that fractionated on the gel. Low molecular weight polyuronides were first evident in fruit harvested at the turning stage and they constituted the major portion of the polyuronides obtained from fruit at more advanced stages of ripening. The appearance of degraded polyuronides corresponded well with the activity of endo-D-galacturonanase, which appeared to be solely responsible for the degradation of these wall polymers. The cell wall hemicelluloses were also affected during ripening; gel-filtration analyses revealed marked changes in the molecular-weight distribution of these polymers. Hemicelluloses from immature green and mature green fruit were similar chromatographically, whereas those from fruit harvested during ripening showed progressively lower quantities of high molecular weight polymers and higher quantities of low molecular weight polymers (<40,000). These changes coincided with the degradation of the pectic polysaccharides; however, in vitro studies using isolated cell wall showed that pectin degradation occurred independently of the changes in hemicelluloses.
Elevated Serum Levels of Antibodies to Carbonic Anhydrase I and II in Patients with Chronic Pancreatitis (2000)

An immune-mediated reaction to pancreatic structures has been postulated for the pathogenesis of chronic pancreatitis (CP). Several reports demonstrate the presence of antibodies to the pancreatic ductal epithelium in some patients suffering from CP. Serum antibodies to carbonic anhydrase I (anti-CA I) and II (anti-CA II) are present in patients affected by idiopathic CP. The aim of this study was to evaluate the presence of anti-CA I and anti-CA II in a series of patients with CP. We studied 78 consecutive CP patients (62 male, 16 female; mean age 48.6 +/- 10.2 years) referred to the Verona University Center for the Study of the Pancreas. As a control group, we studied 26 healthy subjects recruited from among the medical and nursing staff of the center. Serum anti-CA I and anti-CA II levels were quantified by enzyme-linked immunosorbent assay using a standard method with minor modifications. The mean absorbance of antibodies was higher in CP patients than in control subjects (anti-CA I: 0.064 +/- 0.042 vs. 0.047 +/- 0.015, p = 0.051; and anti-CA II: 0.038 +/- 0.02 vs. 0.029 +/- 0.014, p = 0.033). Positive results were arbitrarily defined as absorbance values >0.067 for anti-CA I and 0.047 for anti-CA II. We found anti-CA I and anti-CA II positivity in 21 of 78 (27%) and 20 of 78 (26%) of CP patients, respectively, and in only two of 26 control subjects (7.7%) (p = 0.032 and 0.039). Twenty-two of 26 subjects in the control group (84.6%) and 48 of 78 patients (61.5%) in the CP group tested negative for both antibodies (p = 0.03). None of the control subjects and 12 of 78 (16.6%) of the CP patients tested positive for both anti-CA I and anti-CA II. We observed a significant correlation between anti-CA I and anti-CA II serum levels in control subjects (R = 0.423; p = 0.016) and in CP patients (R = 0.584; p < 0.0001). No correlation was found between serum antibody levels and any of the following variables: length of disease, alcohol consumption, smoking habits, pancreatic surgery, pancreatic calcifications, diabetes, and steatorrhea. Serum levels of anti-CA I and anti-CA II are elevated in some patients suffering from CP.
Evaluation of a new spectral peak coding strategy for the Nucleus 22 Channel Cochlear Implant System. (1994)

Sixty-three postlinguistically deaf adults from four English-speaking countries participated in a 17-week field study of performance with a new speech coding strategy, Spectral Peak (SPEAK), and the most widely used strategy, Multipeak (MPEAK), both of which are implemented on wearable speech processors of the Nucleus 22 Channel Cochlear Implant System; MPEAK is a feature-extraction strategy, whereas SPEAK is a filterbank strategy. Subjects' performance was evaluated with an experimental design in which use of each strategy was reversed and replicated (ABAB). Average scores for speech tests presented sound-only at 70 dB SPL were higher with the SPEAK strategy than with the MPEAK strategy. For tests in quiet, mean scores for medial vowels were 74.8 percent versus 70.1 percent; for medial consonants, 68.6 percent versus 56.6 percent; for monosyllabic words, 33.8 percent versus 24.6 percent; and for sentences, 77.5 percent versus 67.4 percent. For tests in noise, mean scores for Four-Choice Spondees at +10 and +5 dB signal-to-noise ratio (S/N) were 88.5 percent versus 73.6 percent and 80.1 percent versus 62.3 percent, respectively; and for sentences at +15 dB, +10, and +5 dB S/N, 66.5 percent versus 43.4 percent, 61.5 percent versus 37.1 percent, and 60.4 percent versus 31.7 percent, respectively. Subjects showed marked improvement in recognition of sentences in noise with the new SPEAK filterbank strategy. These results agree closely with subjects' responses to a questionnaire on which approximately 80 percent reported they heard best with the SPEAK strategy for everyday listening situations.
Toward Real Time Data Analysis for Smart Grids (2012)

This paper describes the architecture and design of a novel system for supporting large-scale real-time data analysis for future power grid systems. The widespread deployment of renewable generation, smart grid controls, energy storage, plug-in hybrids, and new conducting materials will require fundamental changes in the operational concepts and principal components of the grid. As a result, the whole system becomes highly dynamic and requires constant adjusting based on real time data. Even though millions of sensors such as phase measurement units (PMU) and smart meters are being widely deployed, a data layer that can analyze this amount of data in real time is needed. Unlike the data fabric in other cloud services, the data layer for smart grids has some unique design requirements. First, this layer must provide real time guarantees. Second, this layer must be scalable to allow a large number of applications to access the data from millions of sensors in real time. Third, reliability is critical and this layer must be able to continue to provide service in face of failures. Fourth, this layer must be secure. We address these challenges though a scalable system architecture that integrates the I/O and data processing capability in a devise set of devices. Data process operations can be placed anywhere from sensors, data storage devices, to control centers. We further employ compression to improve performance. We design a lightweight compression customized for power grid data. Our system can reduce end-to-end response time by reduce I/O overhead through compression and overlap compression operations with I/O. The initial prototype of our system was demonstrated with several use cases from PNNL's FPGI and show that our system can provide real time guarantees to a diverse set of applications.
Mating type-like conversion promoted by the 2 micrograms circle site-specific recombinase: implications for the double-strand-gap repair model. (1986)

Double-strand breaks in DNA are known to promote recombination in Saccharomyces cerevisiae. Yeast mating type switching, which is a highly efficient gene conversion event, is apparently initiated by a site-specific double-strand break. The 2 micrograms circle site-specific recombinase, FLP, has been shown to make double-strand breaks in its substrate DNA. By using a hybrid 2 micrograms circle::Tn5 plasmid, a portion of which resembles, in its DNA organization, the active (MAT) and the silent (HML) yeast mating type loci, it is shown that FLP mediates a conversion event analogous to mating type switching. Whereas the FLP site-specific recombination is not dependent on the RAD52 gene product, the FLP-induced conversion is abolished in a rad52 background. The FLP-promoted conversion in vivo can be faithfully reproduced by making a double-stranded gap in vitro in the vicinity of the FLP site and allowing the gap to be repaired in vivo.
Soybean [<i>Glycine max</i> (L.) Merrill]: Importance as A Crop and Pedigree Reconstruction of Korean Varieties (2015)

Chaeyoung Lee, Man-Soo Choi, Hyun-Tae Kim, Hong-Tai Yun, Byungwook Lee, Young-Soo Chung, Ryan W. Kim, and Hong-Kyu Choi. Plant Breeding and Biotechnology -0001;3:179-96. https://doi.org/10.9787/PBB.2015.3.3.179