gebhart/patrepeval huggingface dataset:
A promising codrug of nicotinic acid and ibuprofen for managing dyslipidemia. I: Synthesis and<i>in vitro</i>evaluation (2011)

Nicotinic acid is therapeutically the optimum antihyperlipidemic agent, yet its intolerable cutaneous flushing hinders its wide clinical implication. The codrug of nicotinic acid and ibuprofen (IBP) was synthesized in the aim of overcoming the troublesome side effect of nicotinic acid by blockade of prostaglandin synthesis through released IBP, thus enhance patient's compliance. The physico-chemical properties of codrug namely solubility, partition coefficient, and pKa were determined. Its solubility in aqueous and organic solvents was highest in 0.1 M HCl and isopropanol, respectively. The kinetics of hydrolysis of the codrug and IBP 2-hydroxyethyl ester was studied in aqueous phosphate buffer solution in pH 1.2, 6.8, and 7.4 at 70°C, 80°C, and 90°C. The hydrolysis was found to be pH dependent and followed Arrhenius equation. The half-life of codrug and IBP 2-hydroxyethyl ester at 25°C in pH 7.4 was 218 days and 3 years, respectively. In vitro enzymatic hydrolysis of codrug and IBP 2-hydroxyethyl ester was studied in human plasma and rat liver homogenate. Codrug and IBP 2-hydroxyethyl ester exhibited faster in vitro enzymatic hydrolysis than in vitro chemical hydrolysis. The pseudo-first-order rate constants were 0.0113, 0.177 min(-1) for codrug and 0.0006, 0.0569 min(-1) for IBP 2-hydroxyethyl ester in human plasma and rat liver homogenate, respectively. Thus, nicotinic acid will be rapidly released from codrug to manage dyslipidemia, followed by the later release of IBP from IBP 2-hydroxyethyl ester to alleviate nicotinic acid cutaneous flushing.
The TDP‐43 N‐terminal domain structure at high resolution (2016)

Structural data have been deposited in the Protein Data Bank under accession code: 2n4p. The NMR assignments have been deposited in the BMRB database under access code: 25675.
Two-dimensional wavelet processor (1996)

An optical implementation of the two-dimensional (2-D) wavelet transform and inverse wavelet transform is performed in real time by the exploitation of a new multichannel system that processes the different daughter wavelets separately. The so-coined wavelet-processor system relies on a multichannel replication array generated that uses a Dammann grating and is able to handle every wavelet function. All channels process in parallel using a conventional 2-D correlator. Experimental results applying the Mexican-hat wavelet-decomposition technique are presented.
Treatment of Preterm Labor with the Oxytocin Antagonist Atosiban (1996)

The purpose of this study was to describe the course of preterm labor in patients receiving a standard intravenous infusion of the oxytocin antagonist atosiban. An open-labeled, non-randomized study was conducted at 4 sites. Successful tocolysis was defined as delay of delivery larger than 48 hours from starting atosiban and no need for an alternate tocolytic. Atosiban was administered by continuous intravenous infusion at a rate of 300 micrograms per minute until uterine contractions were absent for 6 hours, or up to a maximum infusion time of 12 hours. Sixty-two patients of between 20 and 36 weeks' gestation were enrolled over 6 months. One had rupture of membranes and was excluded. Successful tocolysis was noted in 43 of 61 (70.5%). Four delivered spontaneously within 48 hours and 14 (23.0%) required an alternate tocolytic agent. The chance of successful tocolysis was related to the degree of cervical dilation at the start of therapy. Cessation of uterine contractions was noted in 38 patients (62.3%). A decrease in uterine contraction frequency of 50% or more was noted in 50 of 61 patients (82.0%). Four patients reported side effects (nausea, vomiting, headache, dysguesia, chest pain), but in no case did side effects require discontinuation of the medication. Intravenous administration of atosiban is associated with a delay in delivery comparable to that seen with other tocolytics. If this effect is confirmed in planned placebo-controlled trials, its favorable side effect profile may give it a place in the armamentarium.
Constitutive expression of functional P‐glycoprotein in rat hepatoma cells (1994)

P-glycoprotein is a plasma-membrane glycoprotein involved in multidrug resistance. P-glycoprotein overexpression has been demonstrated to occur in tumor cells after cytotoxic drug exposure, but also in some cancers including hepatocellular carcinomas before any chemotherapeutic treatment. In order to better analyze this constitutive type of tumoral drug resistance, we have investigated P-glycoprotein expression and function in rat liver tumors induced experimentally by administration of diethylnitrosamine and in two cell clones derived from one of these tumors designated as RHC1 and RHC2. High levels of P-glycoprotein mRNAs were found in both liver tumor samples and the two hepatoma cell clones as assessed by Northern blotting; both RHC1 and RHC2 cells displayed altered liver functions commonly observed in rat hepatoma cells, particularly the decreased expression of albumin and overexpression of the fetal glutathione S-transferase 7-7. The use of specific multidrug resistance (mdr) probes revealed a major induction of the mdr1 gene in liver tumor samples while RHC1 and RHC2 cells expressed both mdr1 and mdr3 genes without displaying a major alteration in the number of mdr gene copies as assessed by Southern blotting. High amounts of P-glycoprotein were also demonstrated in RHC1 and RHC2 cells by Western blotting. These cells were strongly resistant to doxorubicin and vinblastine, two anticancer drugs transported by P-glycoprotein. Doxorubicin intracellular retention was low in RHC1 and RHC2 cells, but was strongly enhanced in the presence of verapamil, a known modulator agent of P-glycoprotein; low retention appeared to occur via a drug efflux mechanism, indicating that P-glycoprotein was fully active. These results show that rat hepatoma cells can display elevated levels of functional P-glycoprotein without any prior cytotoxic drug selection and suggest that these cells represent a useful model for analyzing P-glycoprotein regulation in intrinsically clinical drug-resistant cancers.
Modification of platelet proteins by malondialdehyde: prevention by dicarbonyl scavengers (2015)

The thromboxane synthase converts prostaglandin H(2) to thromboxane A(2) and malondialdehyde (MDA) in approximately equimolar amounts. A reactive dicarbonyl, MDA forms covalent adducts of amino groups, including the ε-amine of lysine, but the importance of this reaction in platelets was unknown. Utilizing a novel LC/MS/MS method for analysis of one of the MDA adducts, the dilysyl-MDA cross-link, we demonstrated that dilysyl-MDA cross-links in human platelets are formed following platelet activation via the cyclooxygenase (COX)-1/thromboxane synthase pathway. Salicylamine and analogs of salicylamine were shown to react with MDA preferentially, thereby preventing formation of lysine adducts. Dilysyl-MDA cross-links were measured in two diseases known to be associated with increased platelet activation. Levels of platelet dilysyl-MDA cross-links were increased by 2-fold in metabolic syndrome relative to healthy subjects, and by 1.9-fold in sickle cell disease (SCD). In patients with SCD, the reduction of platelet dilysyl-MDA cross-links following administration of nonsteroidal anti-inflammatory drug provided evidence that MDA modifications of platelet proteins in this disease are derived from the COX pathway. In summary, MDA adducts of platelet proteins that cross-link lysines are formed on platelet activation and are increased in diseases associated with platelet activation. These protein modifications can be prevented by salicylamine-related scavengers.
High spatial resolution reflectometry by synthesis of optical coherence function for measuring reflectivity distribution at a long distance (2005)

A high-spatial resolution reflectometry by synthesis of the optical coherence function is proposed for testing optical devices and circuits at the far end of optical subscriber networks. The system can measure the reflectivity distribution at a long dis- tance without performance degradation resulting from the phase fluctuation in a long-length optical fiber. Reflectivity distribution at a distance of 5 km is measured successfully with the spatial resolution of 6 cm.
An electromyographic index for localized muscle fatigue (1977)

A new method for objective quantification of localized muscle fatigue is described. The method is based on power spectrum analysis of myoelectric signals obtained from the fatigued muscle. It permits real-time investigations and yields statistically based criteria for the occurrence of fatigue. The findings are interpreted in terms of muscle action potential conduction velocity changes and rate of the fatigue development.
Purification or contamination? The effect of sorbents on ionic liquids (2008)

Commonly used for purification, alumina and silica are found to contaminate ionic liquids with particles; these particles cannot be removed easily and can have a non-negligible impact on the electrochemical, spectroscopic and physical properties of an ionic liquid, including its nucleation and crystallisation kinetics.
S‐Sulfonation: a Reversible Chemical Modification of Human Immunoglobulins Permitting Intravenous Application (1983)

The generation and release of mediators of inflammation and anaphylaxis via activation of complement or of Fc receptor-bearing cells is held responsible for adverse reactions observed upon intravenous administration of standard immunoglobulins. They are caused by immunoglobulin G (IgG) effector functions predominantly located in the Fc region of the molecule and 'activated' by aggregate formation. Their functional activity depends on the correct conformation of the C gamma 2 domains of Fc and are therefore impaired or even abrogated by S-sulfonation of the hinge disulfide bonds, as demonstrated in this communication: S-sulfonated IgG (S-IgG) has no anticomplementary activity and does not interact with Fc-receptors anymore. After antigen binding, i.e. immune complex (IC) formation, sulfonated IgG is about half as potent as standard IgG in complement activation or phagocyte stimulation (human monocytes and granulocytes). The two activities synergize, however, so that in the presence of complement S-IgG IC are as effective phagocyte activators as standard IC. Moreover, S-sulfonation being the only chemical modification of immunoglobulins that is reversible, it can be demonstrated that all IgG effector functions important for antigen removal are regained by reconstitution of the disulfide bonds.
Synthesis of Monodisperse Iron Oxide and Iron/Iron Oxide Core/Shell Nanoparticles via Iron-Oleylamine Complex (2006)

Monodisperse magnetic nanoparticles are of great scientific and technical interests. This paper reports a single-step synthesis of monodisperse magnetite nanoparticles with particle size of 8 nm. Iron/maghaemite core/shell nanoparticles with particle size of 11 nm were obtained by reducing the concentration of oleylamine. TEM and in-situ FTIR results suggested that iron-oleylamine intermediate was generated in-situ and decomposed at higher temperature. Oleylamine was also found on the surface of nanoparticles, indicating its role as capping agent which provided steric protection of as-synthesized nanoparticles from agglomeration. Both magnetite and iron/maghaemite core/shell nanoparticles were superparamagnetic at room temperature with a blocking temperature at 80 K and 67 K, respectively.
Putative virulence factors of <i>Aspergillus fumigatus</i> (2000)

Various putative virulence factors of Aspergillus fumigatus have been studied over the past decades. A. fumigatus gliotoxin is a potent inhibitor of the mucociliary system. Several fungal metabolites interfere with phagocytosis and opsonization including toxins, 'conidial inhibitory factor', 'A. fumigatus diffusible product' and 'complement inhibitory factor'. A. fumigatus can bind specifically to different host tissues components, whereas toxins give a general and significant immunosuppressive effect on host defences. Circumstantial evidence links the production of elastinolytic proteases with the ability to cause disease. However, none of the reports demonstrates conclusively a decisive role for any of the virulence factors described thus far. It is conceivable that proteolytic enzyme activities such as those expressed by AFAlp are one of a number of factors, each with a minor effect, that combine to facilitate disease progression.
New Potential Therapeutic Approaches by Targeting Rad51- Dependent Homologous Recombination (2013)

International audience
Virtual design and kinematic simulation for cutter of corn harvester (2008)

The 3D model of vertical shaft spindle cutter of corn harvester is established by UG software and the mechanical dynamic software ADAMS is used to establish the 3D kinematic simulation model of the vertical shaft spindle cutter. Kinematic simulation for spindle cutter and cutting off corn stalk is accomplished with ADAMS. The simulation results demonstrate that the movement of blades in initial stages is instable and the variable number of the blades has no obvious effect on the state of motion of the vertical shaft spindle cutter. However, with the increasing number of blades, the force on pin shaft of blade imposed by the blades and the force on rotation pin imposed by knife plate are reducing.The force of cutting off corn stalk is true and credible.
BOWED STRING PHYSICAL MODEL VALIDATION THROUGH USE OF A BOW CONTROLLER AND EXAMINATION OF BOW STROKES (2003)

Combining a physical model with a bow controller, we propose a technique to validate bow strokes in a virtual instrument. 1.
Comparison of quantitative parameters in cervix cancer measured by dynamic contrast–enhanced MRI and CT (2010)

Cervical tumors of 38 cervix cancer patients were scanned by T(1)-weighted dynamic contrast enhanced (DCE) MRI and then by DCE-CT on the same day. Gadodiamide and iohexol were respectively used as the low-molecular-weight contrast agent in DCE-MRI and DCE-CT. Under an extended Tofts model, DCE-MRI data were analyzed using either individual arterial input functions estimated by a multiple reference tissue method or a population arterial input function by Parker et al., whereas DCE-CT data were analyzed using the arterial input function directly measured from the external iliac arteries. The derived quantitative parameters of cervical tumors were compared between DCE-MRI and DCE-CT. When using the individual multiple reference tissue method arterial input functions to analyze the DCE-MRI data, the correlation coefficients between DCE-MRI- and DCE-CT-derived parameters were, respectively, back-flux rate constant (r = 0.80), extravascular extracellular fractional volume (r = 0.73), contrast agent transfer rate (r = 0.62), and blood plasma volume (r = 0.32); when using the Parker population arterial input function, the correlation coefficients were back-flux rate constant (r = 0.79), extravascular extracellular fractional volume (r = 0.77), contrast agent transfer rate (r = 0.63), and blood plasma volume (r = 0.58). Tumor parametric maps derived by DCE-MRI and DCE-CT had very similar morphologies. However, the means of most derived quantitative parameters were significantly different between the two imaging methods. Close correlation of quantitative parameters derived from two independent imaging modalities suggests both are measuring similar tumor physiologic variables.
Preparation of ( <scp> <i>S</i> </scp> )‐4‐Isopropyl‐ <scp> <i>N</i> </scp> ‐Propanoyl‐1,3‐Thiazolidine‐2‐Thione (2009)

Abstract ( S )‐Valinol Carbon disulfide ( S)‐ 4‐Isopropyl‐1,3‐thiazolidine‐2‐thione n‐ Butyllithium Propanoyl chloride ( S)‐ 4‐Isopropyl‐ N‐ propanoyl‐1,3‐thiazolidine‐2‐thione
Evaluation of the Modified Mini-Mental State Examination in a General Psychiatric Population (1991)

Studies of clinical cognitive screening tests began in the 1960s, and ten instruments have been reported in the English literature. In this study, we have compared the widely used Mini-Mental State Examination developed by Folstein with a reportedly enhanced version, the Modified Mini-Mental State Examination devised by Teng, using a sample of 250 patients (inpatients, outpatients, emergency). We have come to the conclusion that the modifications brought about by Teng result in a minor improvement of the validity of the Mini-Mental State Examination in a psychiatric patients in a general hospital.
Three-Dimensional Simulation of a Magnitude 7.75 Earthquake on the San Andreas Fault (1995)

Simulation of 2 minutes of long-period ground motion in the Los Angeles area with the use of a three-dimensional finite-difference method on a parallel supercomputer provides an estimate of the seismic hazard from a magnitude 7.75 earthquake along the 170-kilometer section of the San Andreas fault between Tejon Pass and San Bernardino. Maximum ground velocities are predicted to occur near the fault (2.5 meters per second) and in the Los Angeles basin (1.4 meters per second) where large amplitude surface waves prolong shaking for more than 60 seconds. Simulated spectral amplitudes for some regions within the Los Angeles basin are up to 10 times larger than those at sites outside the basin at similar distances from the San Andreas fault.
Recursive Least Squares with Linear Constraints (2007)

Recursive Least Squares (RLS) algorithms have wide-spread applications in many areas, such as real-time signal processing, control and communications. This paper shows that the unique solutions to linear-equality constrained and the unconstrained LS problems, respectively, always have exactly the same recursive form. Their only difference lies in the initial values. Based on this, a recursive algorithm for the linear-inequality constrained LS problem is developed. It is shown that these RLS solutions converge to the true parameter that satisfies the constraints as the data size increases. A simple and easily implementable initialization of the RLS algorithm is proposed.
A new metric to measure shape differences in fMRI activity (2011)

We present a novel shape metric for quantification of shape differences between the spatial components obtained from independent component analysis (ICA) of group functional magnetic resonance imaging (fMRI) data. This metric is utilized to measure the difference in shapes of the activation regions obtained from different subjects within a group (healthy controls or patients). The parameters comprising the metric are computed for each pixel on the outermost contour (edge) of an activation region for each slice. These parameters are in the form of (r, θ) pairs that may be interpreted as the length and orientation of a vector originating from the centroid of the activation region to the pixel belonging to the boundary contour. Using this information we extract three features that quantify the shape difference between the two shapes under observation. The reference and observation shapes may be selected in two ways: (a) activation maps from two different subjects or (b) mean activation map compared against subject-wise activations, as obtained from group ICA. We present different methods to visualize the shape differences, thus providing a tool to observe the spatial differences within a group or across groups. In addition to the above results, we also address a few special cases where two or more activation contours are present in a single slice and present potential solutions for accounting for these regions as special measures. Our results show that this metric has utility in creating a better understanding of the variability in brain activity among different groups of subjects performing the same task.
The Development of a Novel Image Quality Metric and a Synthetic Colour Test Image for Objective Quality Assessment of Digital Codecs (2005)

This paper proposes a novel image quality metric for colour codecs and a novel colour test image. The degree of colour error (bleeding) due to image compression is evaluated with a special colour test image designed to emphasise colour artefacts. The known reference approach, which is used in this research, offers swift and accurate measurements. The proposed test image replaces the full field static colour bar test signal used in analogue television and video engineering. The proposed test image can be used to evaluate the performance of digital video and television broadcasting facilities. The objective quality measure can also be used in the codec development process and in benchmarking codec performance. The efficacy of the new metric and test image is assessed using a JPEG codec at a range of compression levels.
Microscopy Image Analysis: Blob Segmentation using Geodesic Active Contours (2009)

An Insight Toolkit (ITK) processing framework for blob segmentation with applications to microscopy images is presented in this paper. Our algorithm is a reﬁnement of the work of Mosaliganti et al. [3] for splitting cell clusters. The basic idea is to incorporate as many cues as possible into developing a suitable level-set speed function so that an evolving contour exactly segments a cell/nuclei blob. We use image gradients, distance maps, multiple channel information and a shape model to drive the evolution. The framework consists of a linear pipeline of 6 new ITK ﬁlters which are applied in succession to generate the segmentation. The ﬁlters extract the cell foreground, construct the speed image, ﬁnd seed points for evolution and collect cell statistics from the segmentation. We include 2D/3D example code, parameter settings and show the results generated on confocal images of the zebraﬁsh embryo.
Adult Stem Cells for Cardiac Repair: A Choice Between Skeletal Myoblasts and Bone Marrow Stem Cells (2006)

The real promise of a stem cell-based approach for cardiac regeneration and repair lies in the promotion of myogenesis and angiogenesis at the site of the cell graft to achieve both structural and functional benefits. Despite all of the progress and promise in this field, many unanswered questions remain; the answers to these questions will provide the much-needed breakthrough to harness the real benefits of cell therapy for the heart in the clinical perspective. One of the major issues is the choice of donor cell type for transplantation. Multiple cell types with varying potentials have been assessed for their ability to repopulate the infarcted myocardium; however, only the adult stem cells, that is, skeletal myoblasts (SkM) and bone marrow-derived stem cells (BMC), have been translated from the laboratory bench to clinical use. Which of these two cell types will provide the best option for clinical application in heart cell therapy remains arguable. With results pouring in from the long-term follow-ups of previously conducted phase I clinical studies, and with the onset of phase II clinical trials involving larger population of patients, transplantation of stem cells as a sole therapy without an adjunct conventional revascularization procedure will provide a deeper insight into the effectiveness of this approach. The present article discusses the pros and cons of using SkM and BMC individually or in combination for cardiac repair, and critically analyzes the progress made with each cell type.