gebhart/patrepeval huggingface dataset:
Development of Diclofenac Sodium Controlled Release Solid Dispersions by Spray Drying Using Optimization Strategy I. Powder Formulation (1995)

Diclofenac sodium (DS) controlled release solid dispersions were prepared by spray drying using ethylcellulose (EC), methacrylic acid copolymer (Eudragit), chitosan, hydroxypropyl methylcellulose (HPMC), and carbomer as single carriers and EC-chitosan as combined carriers. Among solid dispersions of 3:1 drugsingle carrier, the system containing chitosan exhibited the slowest dissolution followed by the systems containing Eudragit, EC, HPMC, and carbomer, respectively. Combined carriers of EC-chitosan exhibited more dissolution retarding effect than single carrier of EC or chitosan. An Hadamard matrix H[8] was employed to estimate the main effects of four parameters: spray feeding volume and contents of absolute ethanol, EC, and chitosan. Optimization strategy using multiple linear regression and a feasibility computer program was utilized to obtain the optimum quantities of the four parameters that would result in a required DS controlled release solid dispersion. The validation of the optimum DS solid dispersion was confirmed by statistical analysis. The optimized 10: (2.5+0.02) DS:(EC+chitosan) controlled release solid dispersion exhibited a dissolution profile that was well fitted to Higuchi model.
Poly(ethylene oxide)-Bearing Lipids and Interaction of Functionalized Liposomes with Intact Cells (1997)

The aggregation behavior of poly(ethylene oxide)-bearing lipids (PEO-lipids) in aqueous media or at the air-water interface was investigated. The PEO-lipids have a PEO moiety (average number of PEO units, 5 to 31) on the hydroxy group of 1,3-didodecyloxy-2-propanol. The outer surface of lecithin liposome was functionalized by reconstitution of the PEO-lipids, and the interaction of intact cells with the functionalized liposome was examined. Using fluorescent and biological markers, fusion of the PEO-lipid reconstituted liposome with various intact cells, such as carrot protoplast, Hela, B16 melanoma, and Jurkat cells was demonstrated.
Computation of Extended Suzuki Mobile Fading Channel (Type I) Parameters (2019)

The analysis and modeling of mobile fading communications channels has been an active research topic since early beginnings of mobile radio systems. In mobile wireless communication systems, the multipath propagation in addition to the movement of the receiver and/or the transmitter leads to drastic and random fluctuations of the received signal. For flat fading channels, the extended Suzuki process of type (I) has been proposed as a stochastic model of such received signal fluctuations. In this paper we discuss this stochastic model and an appropriate deterministic model, and subsequently present and analyze simulation results based on these models. In this paper, a method to mitigate the effect of multipath propagation using an adaptive array antenna is presented. It is shown that by controlling a number of active elements and their spacing the array’s capability to eliminate scattered signals can be enhanced in the presence of pointing errors.
Atrial Natriuretic Peptide Polarizes Human Dendritic Cells Toward a Th2-Promoting Phenotype Through Its Receptor Guanylyl Cyclase-Coupled Receptor A (2003)

Atrial natriuretic peptide (ANP) is a cardiovascular hormone secreted mainly by the cardiac atria and regulates the volume-pressure homeostasis. The action of ANP is mediated by its receptor, guanylyl cyclase-coupled receptor A (GC-A). In this study, we explored the possibility that ANP and GC-A may play a role in the dendritic cell (DC)-mediated immune regulation. We first examined the expression of GC-A in human monocyte-derived DCs in comparison with monocytes and found that DCs but not monocytes express GC-A at both the mRNA and protein levels. DCs responded to ANP with an increase in intracellular cGMP in a dose-dependent manner, indicating that GC-A expressed on DCs is functional. Furthermore, treatment of DCs with ANP decreased production of IL-12 and TNF-alpha and conversely increased that of IL-10 upon stimulation with LPS. In accordance with this change of cytokine production, DCs treated with ANP plus LPS promoted differentiation of naive CD4(+) T cells into a Th2 phenotype. Finally, we presented evidence that ANP affected cytokine production of fresh whole blood stimulated with LPS in line with the above-mentioned results. These results indicate that ANP polarizes human DCs toward a Th2-promoting phenotype through GC-A and thus can regulate immune responses.
Stimulation of Platelet Production by Serum of Platelet-Depleted Rats (1961)

Four subcutaneous injections, given during a 2-day period, of serum from platelet-depleted rats into untreated or splenectomized rats caused an increase in the number of circulating platelets to as much as 167% of the initial count. The rise in peripheral platelet count began 2 days after the first injection, reached a peak at 5 days, then declined to control values at 8 days. Equal amounts of serum from untreated donors did not produce this response. The results indicate that the active serum contains an agent (thrombopoietin) that stimulates production of blood platelets.
Mice with Genetically Altered Glucocorticoid Receptor Expression Show Altered Sensitivity for Stress-Induced Depressive Reactions (2005)

Altered glucocorticoid receptor (GR) signaling is a postulated mechanism for the pathogenesis of major depression. To mimic the human situation of altered GR function claimed for depression, we generated mouse strains that underexpress or overexpress GR, but maintain the regulatory genetic context controlling the GR gene. To achieve this goal, we used the following: (1) GR-heterozygous mutant mice (GR+/-) with a 50% GR gene dose reduction, and (2) mice overexpressing GR by a yeast artificial chromosome resulting in a twofold gene dose elevation. GR+/- mice exhibit normal baseline behaviors but demonstrate increased helplessness after stress exposure, a behavioral correlate of depression in mice. Similar to depressed patients, GR+/- mice have a disinhibited hypothalamic-pituitary-adrenal (HPA) system and a pathological dexamethasone/corticotropin-releasing hormone test. Thus, they represent a murine depression model with good face and construct validity. Overexpression of GR in mice evokes reduced helplessness after stress exposure, and an enhanced HPA system feedback regulation. Therefore, they may represent a model for a stress-resistant strain. These mouse models can now be used to study biological changes underlying the pathogenesis of depressive disorders. As a first potential molecular correlate for such changes, we identified a downregulation of BDNF protein content in the hippocampus of GR+/- mice, which is in agreement with the so-called neurotrophin hypothesis of depression.
Cytotoxic effects of acrylates and methacrylates: Relationships of monomer structures and cytotoxicity (1997)

Thirty-nine acrylates and methacrylates that had been used in dental resin materials were evaluated by a cytotoxicity test, and the relationships between their structures and cytotoxicity were studied to predict cytotoxic levels of dental resin materials in order to develop new low-toxic resin materials. All the acrylates evaluated were more toxic than corresponding methacrylates. In both the acrylates and methacrylates, a hydroxyl group seemed to enhance cytotoxicity. Dimethacrylates with 14 or fewer oxyethylene chains showed similar cytotoxicity while dimethacrylates with 23 oxyethylene chains showed lower cytotoxicity. The cytotoxicity ranking of monomers widely used in dental resin materials was bisphenol A bis 2-hydroxypropyl methacrylate (bisGMA) > urethane dimethacrylate (UDMA) > triethyleneglycol dimethacrylate (3G) > 2-hydroxyethyl methacrylate (HEMA) > methyl methacrylate (MMA). In acrylates, methacrylates, and ethylmethacrylates with either substituents, the lipophilicity of substituents affected their cytotoxicity, and an inverse correlation between IC50 and logP was observed. These results will be useful in developing new resin materials with low toxic monomer compositions.
Magnetic resonance imaging of the abdomen: applications in the oncology patient. (2000)

Cross-sectional imaging of the abdomen in oncology patients presents unique challenges and opportunities. A close working relationship between the oncologist and radiologist is essential for the exchange of the clinical and imaging information necessary for optimizing patient diagnosis and management. Compared to helical computed tomography (CT), magnetic resonance imaging (MRI) of the abdomen and pelvis offers important advantages, including superior soft-tissue contrast. The multiplanar capabilities of MRI allow for direct coronal or sagittal imaging, providing a truer anatomic presentation of abdominal and pelvic masses. Recent advances in MRI, including the use of intravenous (i.v.) and oral contrast agents, the development of high-performance imagers, and improved surface coil designs, facilitate more rapid abdominal imaging with superior image quality. All of these features combine to produce a versatile imaging examination with exquisite sensitivity for depicting abdominal and pelvic tumors. In this article, we will review the clinical applications for hepatic and extrahepatic abdominal MRI in the oncology patient. The MRI techniques and protocols described can be applied to most commercially available high-field magnetic resonance imagers.
A Critical Role of Erythropoietin Receptor in Neurogenesis and Post-Stroke Recovery (2006)

Erythropoietin (EPO) is the principal growth factor regulating the production of red blood cells. Recent studies demonstrated that exogenous EPO acts as a neuroprotectant and regulates neurogenesis. Using a genetic approach, we evaluate the roles of endogenous EPO and its classical receptor (EPOR) in mammalian neurogenesis. We demonstrate severe and identical embryonic neurogenesis defects in animals null for either the Epo or EpoR gene, suggesting that the classical EPOR is essential for EPO action during embryonic neurogenesis. Furthermore, by generating conditional EpoR knock-down animals, we demonstrate that brain-specific deletion of EpoR leads to significantly reduced cell proliferation in the subventricular zone and impaired post-stroke neurogenesis. EpoR conditional knockdown leads to a specific deficit in post-stroke neurogenesis through impaired migration of neuroblasts to the peri-infarct cortex. Our results suggest that both EPO and EPOR are essential for early embryonic neural development and that the classical EPOR is important for adult neurogenesis and for migration of regenerating neurons during post-injury recovery.
Signal transduction and transcriptional and posttranscriptional control of iron-regulated genes in bacteria (1997)

Iron is an essential element for nearly all living cells. Thus, the ability of bacteria to utilize iron is a crucial survival mechanism independent of the ecological niche in which the microorganism lives, because iron is scarce both in potential biological hosts, where it is bound by high-affinity iron-binding proteins, and in the environment, where it is present as part of insoluble complex hydroxides. Therefore, pathogens attempting to establish an infection and environmental microorganisms must all be able to utilize the otherwise unavailable iron. One of the strategies to perform this task is the possession of siderophore-mediated iron uptake systems that are capable of scavenging the hoarded iron. This metal is, however, a double-edged sword for the cell because it can catalyze the production of deadly free hydroxyl radicals, which are harmful to the cells. It is therefore imperative for the cell to control the concentration of iron at levels that permit key metabolic steps to occur without becoming a messenger of cell death. Early work identified a repressor, Fur, which as a complex with iron repressed the expression of most iron uptake systems as well as other iron-regulated genes when the iron concentration reached a certain level. However, later work demonstrated that this regulation by Fur was not the only answer under low-iron conditions, there was a need for activation of iron uptake genes as well as siderophore biosynthetic genes. Furthermore, it was also realized that in some instances the actual ferric iron-siderophore complex induced the transcription of the cognate receptor and transport genes. It became evident that control of the expression of iron-regulated genes was more complex than originally envisioned. In this review, I analyze the processes of signal transduction, transcriptional control, and posttranscriptional control of iron-regulated genes as reported for the ferric dicitrate system in Escherichia coli; the pyochelin, pyoverdin, and enterobactin systems in Pseudomonas species; the irgB system in Vibrio cholerae; and the plasmid-mediated anguibactin system in Vibrio anguillarum. I hope that by using these diverse paradigms, I will be able to convey a unifying picture of these mechanism and their importance in the maintenance and prosperity of bacteria within their ecological niches.
Pyruvate Dehydrogenase Complex from Higher Plant Mitochondria and Proplastids: Kinetics (1977)

A steady-state kinetic analysis has been performed on the pyruvate dehydrogenase complex from pea (Pisum sativum L.) mitochondria and castor bean (Ricinus communis L.) proplastids. Substrate interaction kinetics for all substrates gave parallel lines consistent with a multisite ping-pong mechanism. Product inhibition studies showed uncompetitive inhibition between acetyl-CoA and pyruvate and competitive inhibition between NADH and NAD(+), both of which are also consistent with this mechanism. In the mitochondrial complex, acetyl-CoA showed noncompetitive inhibition versus CoA which suggests that the intermediate complex is kinetically important in the lipoamide transacetylase component of this complex. In contrast, the proplastid complex showed competitive inhibition in this interaction. NADH is a noncompetitive inhibitor versus CoA in both complexes indicating that these complexes, like the mammalian complex, may have protein-protein interactions between the second and third enzymes of the complex. Since NADH also shows noncompetitive inhibition versus pyruvate, this interaction may extend to all components of the complex. Acetyl-CoA shows noncompetitive inhibition versus NAD(+) which may also be a result of interaction between the second and third enzymes of the complex. The limiting Michaelis constants for substrates and the inhibitor constants for both complexes were determined.
Thermomechanical properties of blends of pectin and poly(vinyl alcohol) (1996)

Blends of citrus pectin and several types of poly(vinyl alcohol) were investigated to determine the effects of compositional variables and polymer type on film properties. Some films were also plasticized with glycerol. Films were cast from water onto Lexan™ plates, dried, and removed. Thermomechanical properties were obtained using a dynamic mechanical analyzer, and thermodynamic transitions were also obtained using a differential scanning calorimeter. Increasing the amount of poly(vinyl alcohol) in the blends reduced the storage and loss modulus of the films above the glass transition temperature (Tg). The Tg values observed decreased as the amount of PVOH in the blend increased. Addition of glycerol depressed the PVOH Tg and merged it into the Tg of the pectin/glycerol blend. Changes in the molecular weight and degree of ester hydrolysis of poly(vinyl alcohol) exerted a rather small effect on the blends. © 1996 John Wiley & Sons, Inc. 1 Reference to a brand or firm name does not constitute an endorsement by the U.S. Department of Agriculture over others of a similar nature.
Hexosamine-Induced Fibronectin Protein Synthesis in Mesangial Cells Is Associated With Increases in cAMP Responsive Element Binding (CREB) Phosphorylation and Nuclear CREB (2001)

Hyperglycemia-induced alterations in mesangial (MES) cell function and extracellular matrix protein accumulation are seen in diabetic glomerulopathy. Recent studies have demonstrated that some of the effects of high glucose (HG) on cellular metabolism are mediated by the hexosamine biosynthesis pathway (HBP), in which fructose-6-phosphate is converted to glucosamine 6-phosphate by the rate-liming enzyme glutamine:fructose-6-phosphate amidotransferase (GFA). In this study, we investigated the role of HBP on HG-stimulated fibronectin protein synthesis, a matrix component, in SV-40-transformed rat kidney MES cells. Treatment of MES cells with 25 mmol/l glucose (HG) for 48 h increases cellular fibronectin levels by two- to threefold on Western blots when compared with low glucose (5 mmol/l). Glucosamine (GlcN; 1.5 mmol/l), which enters the hexosamine pathway distal to GFA action, also increases fibronectin synthesis. Azaserine (AZA; 0.5 micromol/l), an inhibitor of GFA, blocks the HG- but not the GlcN-induced fibronectin synthesis. Fibronectin contains cAMP responsive element (CRE) consensus sequences in its promoter and the phosphorylation of CRE-binding protein (CREB) may regulate its expression. On Western blots, HG and GlcN stimulate two- to threefold the phosphorylation of CREB at Ser 133, whereas CREB protein content was unaltered by either HG or GlcN. In addition, nuclear CREB activity was increased by HG and GlcN on gel-shift assays using (32)P-CRE oligonucleotides. AZA impeded the HG-enhanced CREB phosphorylation and CRE binding but had no effect on GlcN-mediated CREB phosphorylation and CRE binding. Pharmacologic inhibition of protein kinase C (PKC) and protein kinase A (PKA), which are involved in hexosamine-mediated matrix production, blocked the CREB phosphorylation and fibronectin synthesis seen in HG and GlcN conditions. We conclude that the effects of HG on fibronectin synthesis in the mesangium are mediated by the HBP possibly via hexosamine regulation of CREB and PKC/PKA signaling pathways. These results support the hypothesis that the HBP is a sensor and regulator of the actions of glucose in the kidney.
α5β1 Integrin Activates an NF-κB-Dependent Program of Gene Expression Important for Angiogenesis and Inflammation (2002)

GeneCalling, a genome-wide method of mRNA profiling, reveals that endothelial cells adhering to fibronectin through the alpha 5 beta 1 integrin, but not to laminin through the alpha 2 beta 1 integrin, undergo a complex program of gene expression. Several of the genes identified are regulated by the NF-kappa B transcription factor, and many are implicated in the regulation of inflammation and angiogenesis. Adhesion of endothelial cells to fibronectin activates NF-kappa B through a signaling pathway requiring Ras, phosphatidylinositol 3-kinase, and Rho family proteins, whereas adhesion to laminin has a limited effect. Retroviral transfer of the superrepressor of NF-kappa B, I kappa B-2A, blocks basic fibroblast growth factor-induced angiogenesis in vivo. These results suggest that engagement of the alpha 5 beta 1 integrin promotes an NF-kappa B-dependent program of gene expression that coordinately regulates angiogenesis and inflammation.
The interleukin-1 and interleukin-1 converting enzyme families in the cardiovascular system. (1998)

The multifunctional cytokine interleukin-1 (IL-1) is a key mediator in the cytokine network. The IL-1 family consists of two zymogen isoforms of IL-1 (IL-1alpha and IL-1beta), the IL-1 receptor antagonists, two receptors and receptor-associated proteins. Identification of the enzyme responsible for cleavage and activation of the IL-1beta precursor, the IL-1beta converting enzyme (ICE; caspase 1), unexpectedly linked the IL-1 family to the apoptosis machinery, since ICE is the founding molecule of the caspase family, which is important for regulation of apoptosis. Although it has been suggested that cytokines are involved in pathogenesis of cardiovascular diseases only few informations exist regarding the endogenous production and function of IL-1 and the associated enzyme(s) of the caspase family in the cardiovascular system. Here, we summarize informations regarding the IL-1 and the caspase family in the cardiovascular system.
Similarity estimation techniques from rounding algorithms (2002)

(MATH) A locality sensitive hashing scheme is a distribution on a family $\F$ of hash functions operating on a collection of objects, such that for two objects x,y, PrheF[h(x) = h(y)] = sim(x,y), where sim(x,y) e [0,1] is some similarity function defined on the collection of objects. Such a scheme leads to a compact representation of objects so that similarity of objects can be estimated from their compact sketches, and also leads to efficient algorithms for approximate nearest neighbor search and clustering. Min-wise independent permutations provide an elegant construction of such a locality sensitive hashing scheme for a collection of subsets with the set similarity measure sim(A,B) = \frac{|A ∩ B|}{|A ∪ B|}.(MATH) We show that rounding algorithms for LPs and SDPs used in the context of approximation algorithms can be viewed as locality sensitive hashing schemes for several interesting collections of objects. Based on this insight, we construct new locality sensitive hashing schemes for:A collection of vectors with the distance between → \over u and → \over v measured by O(→ \over u, → \over v)/π, where O(→ \over u, → \over v) is the angle between → \over u) and → \over v). This yields a sketching scheme for estimating the cosine similarity measure between two vectors, as well as a simple alternative to minwise independent permutations for estimating set similarity.A collection of distributions on n points in a metric space, with distance between distributions measured by the Earth Mover Distance (EMD), (a popular distance measure in graphics and vision). Our hash functions map distributions to points in the metric space such that, for distributions P and Q, EMD(P,Q) ≤ Ehe\F [d(h(P),h(Q))] ≤ O(log n log log n). EMD(P, Q).
Stereoselective disposition of ibuprofen enantiomers in human cerebrospinal fluid. (1995)

Since both (R)- and (S)-enantiomers of ibuprofen may act on the central nervous system, we investigated their plasma and cerebrospinal fluid (CSF) concentrations in 46 patients with nerve-root compression pain requiring a lumbar puncture. Each patient received an oral dose of 800 mg rac-ibuprofen. A single blood and CSF sample was drawn concomitantly from each patient at intervals between 30 min and 8 h after dosing. Both isomers peaked later in the CSF (3 h) than in the plasma (1.5 h). Their CSF concentrations became higher than their concurrent free plasma concentrations after 90 min. The estimated elimination half-lives of (R)- and (S)-ibuprofen were 1.7 h and 2.5 h in plasma and 3.9 h and 7.9 h in CSF, respectively. The AUCCSF/AUCplasma ratios (0, 8 h) were 0.009 and 0.015 for the (R)- and (S)-forms, respectively.
Finishing the finished human chromosome 22 sequence (2008)

Thus, we have made significant progress to completing the sequence of the euchromatic regions of human chromosome 22 using a combination of detailed approaches. Our experience suggests that substantial work remains to close the outstanding gaps in the human genome sequence.