gebhart/patrepeval huggingface dataset:
Synthesis and Glycosidase Inhibition Studies of 5‐Methyl‐Substituted Tetrahydroxyindolizidines and ‐pyrrolizidines Related to Natural Hyacinthacines B (2013)

Abstract The synthesis of three tetrahydroxyindolizidines and one tetrahydroxypyrrolizidine related to natural hyacinthacines B and their biological evaluation as glycosidase inhibitors is reported. The target molecules were obtained through highly stereoselective cycloadditions between sugriched allylic and homoallylic alcohols. This allowed the installation of a methyl group at C5 – a common feature of many natural hyacinthacines – with high control over the stereoselectivity. The new compounds inhibit amyloglucosidase from Aspergillus niger and β‐glucosidase from almonds. Compound 1 is a competitive inhibitor of amyloglucosidase and shows a fair selectivity towards this enzyme. The presence of C5‐Me substitution in indolizidines 2 and 3 slightly diminishes the inhibitory activity towards amyloglucosidase whereas it improves the inhibitory properties towards β‐glucosidase.
MONOPOLISTIC COMPETITION AND OPTIMUM PRODUCT DIVERSITY (1975)

Pettengill tests whether there is an excessive number of firms in a monopolistically competitive equilibrium by a device of considerable expository merit. He removes one firm, and redistributes the resources thus released equally over the remaining firms in the sector, to see if welfare can be improved. To do this correctly, we write n, for the equilibrium number of firms and xe for the output of each. With fixed cost a and constant average variable cost c, removing one firm releases (a + Cxe) of resources, and this enables the output of each of the remaining ( I) firms to be increased (a + c Xe )/(1fl 1)}. The quantity xo of the numeraire good is unaffected by this, and the utility function (equation (31) of our paper) is
Palytoxin both Induces and Inhibits the Release of Histamine from Rat Mast Cells (1982)

Palytoxin (PTX) is a potent releaser of histamine from rat mast cells. The concentration response curve is bell-shaped with its range between 0.05 ng/ml and 5 micrograms/ml and its maximum at 50 ng/ml. The release of histamine by PTX is specific because (a) heat-inactivated (50 degrees C) mast cells are insensitive to PTX, and (b) extracellular calcium is essential. Removal of extracellular potassium as well as the presence of borate shifts the curve to the left by factor of 10. At higher concentrations (5 micrograms/ml), PTX inhibits the release of histamine due to compound 48/80, MCD-peptide, Con-A, ionophore A-23187, and PTX itself.
New control method of piezoelectric transformer converter by PWM and PFM for wide range of input voltage (2002)

A new control method of a piezoelectric transformer (PT) converter by PWM and PFM is presented. The combination of an active-clamp circuit and a resonant circuit makes it possible to control the output voltage of the PT converter by PWM at a fixed switching frequency and PFM at a fixed duty ratio. The PT converter implemented on a printed circuit board was experimentally evaluated and a good controllability was successfully achieved.
Power systems and harmonic factors (2002)

Harmonic currents and distortions in power systems are a natural progression in society's use of electrical equipment. A proliferation of harmonics can cause problems-some severe. However, the benefits we receive from electrification far outweighs the downside to this problem. There is an increased awareness among equipment designers, manufacturers, and users for the need to reduce power system harmonics. However, much work still needs to be done. This paper describes how harmonics arise from nonlinear loads and their effects on the power system. The problems that arise from harmonic current flow are straightforward and simple. The two main problems are abnormal heating of components and disruption of operation. The paper also describe mitigation of harmonic effects which take on two strategies: one is to reduce the harmonic effect; the other is to reduce or control the harmonic content.
<i>Mycobacterium bovis</i>bacillus Calmette–Guérin (BCG) induces human CC- and CXC-chemokines<i>in vitro</i>and<i>in vivo</i> (2006)

Both CC- and CXC-chemokines are known to be potent leucocyte activators and chemoattractants and play important roles in inflammatory responses. However, chemokine response to bacillus Calmette-Guérin (BCG) infection remains incompletely defined. In this study, we investigated human CC- [macrophage-derived chemokine (MDC), monocyte chemoattractant protein (MCP)-1, macrophage inflammatory protein (MIP)-1alpha and eosinophil chemoattractant activity (eotaxin)] and CXC-interferon-inducible protein (IP)-10 chemokine production in response to BCG stimulation. BCG efficiently induced all chemokines tested in the urine of four bladder cancer patients undergoing intravesical BCG immunotherapy. The peak urinary chemokine responses occurred generally between the fourth and sixth weekly treatment, except eotaxin, which was less predictable. To evaluate the effect of BCG on induction of chemokines in vitro, urothelial cell lines and peripheral blood mononuclear cells (PBMCs) were used. Although BCG induced no or marginal chemokines from urothelial SV-HUC-1, RT4 and T24 cells, BCG-derived cytokines [interleukin (IL)-1beta, interferon (IFN)-gamma and tumour necrosis factor (TNF)-alpha] induced all chemokines tested except eotaxin from these cell lines. BCG also efficiently induced all chemokines tested except eotaxin from PBMCs of both BCG-naive and BCG-vaccinated subjects. MCP-1 and MIP-1alpha emerged at 4-5 h post-BCG exposure (early chemokines); IP-10 elevated at day 1 and peaked at day 2 (intermediate chemokine); and MDC elevated at day 1 and peaked at day 7 (late chemokine). This kinetic pattern was paralleled with that of BCG-induced cytokines [early: TNF-alpha; intermediate: IL-6 and IL-10; and late: IFN-gamma and granulocyte-macrophage colony-stimulating factor (GM-CSF)]. Taken together, these results indicate that BCG directly or indirectly induces human CC- and CXC-chemokine production, which may represent one of the mechanisms by which BCG exerts its anti-tumour activity.
Rad54 protein stimulates the postsynaptic phase of Rad51 protein-mediated DNA strand exchange (2001)

Rad54 and Rad51 are important proteins for the repair of double-stranded DNA breaks by homologous recombination in eukaryotes. As previously shown, Rad51 protein forms nucleoprotein filaments on single-stranded DNA, and Rad54 protein directly interacts with such filaments to enhance synapsis, the homologous pairing with a double-stranded DNA partner. Here we demonstrate that Saccharomyces cerevisiae Rad54 protein has an additional role in the postsynaptic phase of DNA strand exchange by stimulating heteroduplex DNA extension of established joint molecules in Rad51/Rpa-mediated DNA strand exchange. This function depended on the ATPase activity of Rad54 protein and on specific protein:protein interactions between the yeast Rad54 and Rad51 proteins.
Beneficial effects of high magnesium on alcohol-induced cardiac failure. (1993)

Although alcohol has long been known to induce cardiac depression and cardiomyopathy, it is not known whether drug therapy or pharmacologic manipulation can be used to prevent or reverse these toxicities. With this in mind, high levels (15 mM) of magnesium (Mg) were investigated for their potential antialcohol effects on perfused rat hearts. A high concentration of ethanol (135 mM) was used to induce rapid cardiac failure as assessed by hemodynamic and metabolic parameters. During ethanol perfusion in normal 1.2 mM [Mg2+]o physiologic salt solution, coronary flow decreased immediately, and all of the hemodynamic parameters studied (except for heart rate) were depressed significantly. After 10 min of 135 mM ethanol perfusion, only 60% of the hearts kept beating; at 15 min, only 42% of the hearts continued to beat. Myocardial metabolism under such conditions as assessed by examination of coronary effluent concentrations of lactic acid (LA), lactic acid dehydrogenase (LDH) and creatine phosphokinase (CPK) was rapidly and severely compromised. Although 15 mM MgSO4 alone did not alter coronary flow and systolic pressure under the conditions studied, it did decrease cardiac output, heart rate and total pressure developed. However, when 15 mM MgSO4 was given 10 min before ethanol, and continued during ethanol perfusion, the usual depression in all assessed cardiac hemodynamic parameters (except heart rate) caused by ethanol was not observed. During 15 min of high [Mg2+]o perfusion, coronary flow recovered from 19.1 +/- 6.8% (ethanol alone) to 68.1 +/- 9.9% of control values (p < 0.01); cardiac output recovered from 10.4 +/- 4.6% (ethanol alone) to 43.6 +/- 7.5% of control (p < 0.01); stroke volume went from 12.9 +/- 5.8% (ethanol alone) to 97.1 +/- 14.5% of control (p < 0.01); systolic pressure from 55.3 +/- 3.6% (ethanol alone) to 88.8 +/- 4.0% of control (p < 0.01), and total pressure developed from 23.9 +/- 7.8% (ethanol alone) to 35.0 +/- 4.5% of control (p < 0.05). Assessment of the metabolic biochemical parameters supported these changes in hemodynamic improvement. For example, LA, LDH and CPK all went from elevated values towards normal levels. There were similar hemodynamic and metabolic responses to high [Mg2+]o given during ethanol perfusion to that given before ethanol perfusion. The hemodynamic and metabolic beneficial effects between groups pretreated or treated with high [Mg2+]o exhibited no significant differences. These results suggest that high [Mg2+]o (15 mM) given either before or during ethanol-induced cardiotoxicity is effective in attenuating both functional and metabolic damage caused by high ethanol perfusion in the rat heart.
A New Phosphatidylinositol 4,5-Bisphosphate-binding Site Located in the C2 Domain of Protein Kinase Cα (2003)

In view of the interest shown in phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P(2)) as a second messenger, we studied the activation of protein kinase Calpha by this phosphoinositide. By using two double mutants from two different sites located in the C2 domain of protein kinase Calpha, we have determined and characterized the PtdIns(4,5)P(2)-binding site in the protein, which was found to be important for its activation. Thus, there are two distinct sites in the C2 domain: the first, the lysine-rich cluster located in the beta3- and beta4-sheets and which activates the enzyme through direct binding of PtdIns(4,5)P(2); and the second, the already well described site formed by the Ca(2+)-binding region, which also binds phosphatidylserine and a result of which the enzyme is activated. The results obtained in this work point to a sequential activation model, in which protein kinase Calpha needs Ca(2+) before the PtdIns(4,5)P(2)-dependent activation of the enzyme can occur.
TCR-Independent CD30 Signaling Selectively Induces IL-13 Production Via a TNF Receptor-Associated Factor/p38 Mitogen-Activated Protein Kinase-Dependent Mechanism (2002)

Initiation of T lymphocyte responses to most Ags requires concurrent stimulation through the TCR and costimulatory receptors such as CD28. Following initial activation, secondary receptors are up-regulated that can costimulate T cells in concert with TCR engagement. One such receptor is the TNFR family member CD30. In this study, we report that unlike CD28, ligation of CD30 on normal effector T cells induces IL-13 production in the absence of concurrent TCR engagement. TCR-independent CD30-mediated IL-13 release correlated with activation of c-Jun N-terminal kinase, p38 mitogen-activated protein kinase (MAPK), and NF-kappaB, and was completely inhibited by the expression of a TNFR-associated factor 2 (TRAF2) dominant-negative transgene (TRAF2.DN-Tg), but not by that of an I-kappaBalpha dominant-negative transgene. In parallel, expression of the TRAF2.DN-Tg selectively prevented the induction of c-Jun N-terminal kinase and p38 MAPK, but not that of NF-kappaB. Furthermore, IL-13 production was reduced in a dose-dependent manner by the p38 MAPK inhibitor SB203580. Together, these results suggest that TCR-independent CD30-mediated production of IL-13 is triggered by association of CD30 with TRAF family members and subsequent activation of p38 MAPK. Inasmuch as IL-13 can promote airway inflammation and cancer progression, production of IL-13 in a TCR-independent manner has important pathological implications in vivo.
Chromatin appearance in intermediate cells from patients with uterine cancer. (1981)

This paper presents the differences found by the computer analysis of digitized images of visually apparently normal intermediate cells from patients with normal cytology and patients with uterine cancer. There exist differences in the absolute amount of nuclear staining, the average density of staining, cell shape and size and also differences in spectral contrasts of the nuclear chromatin. Visual cytologic detection of these changes became more conspicuous when the photomicrographs were arranged in order of their discriminant function scores.
13C NMR spectra and biological activity of N-(1H-benzimidazol-2-yl)benzamides (2006)

Derivatives of 1H-benzimidazol-2-amine and halo-, nitro-, methoxy-, and hydroxy-substituted benzoic acids were synthesized, and their fungicide activity against pure Fusarium culmorum and Helminthosporium sativum cultures and pathogenic microflora of wheat and barley seeds in laboratory and field tests was studied. Some compounds were found to exhibit a strong fungicide activity.
LIFE HISTORY AND THE MALE MUTATION BIAS (2003)

If DNA replication is a major cause of mutation, then those life-history characters, which are expected to affect the number of male germline cell divisions, should also affect the male to female mutation bias (alpha(m)). We tested this hypothesis by comparing several clades of bird species, which show variation both in suitable life-history characters (generation time as measured by age at first breeding and sexual selection as measured by frequency of extrapair paternity) and in alpha(m), which was estimated by comparing Z-linked and W-linked substitution rates in gametologous introns. Alpha(m) differences between clades were found to positively covary with both generation time and sexual selection, as expected if DNA replication causes mutation. The effects of extrapair paternity frequency on alpha(m) suggests that increased levels of sexual selection cause higher mutation rates, which offers an interesting solution to the paradox of the loss of genetic variance associated with strong directional sexual selection. We also used relative rate tests to examine whether the observed differences in alpha(m) between clades were due to differences in W-linked or Z-linked substitution rates. In one case, a significant difference in alpha(m) between two clades was shown to be due to W-linked rates and not Z-linked rates, a result that suggests that mutation rates are not determined by replication alone.
A study of fast and metastable dissociations of adenine-thymine binary-base oligonucleotides by using positive-ion MALDI-TOF mass spectrometry (2002)

In the present study, fast and metastable dissociations of a number of adenine-thymine binary-base oligonucleotides under the conditions of UV matrix-assisted laser desorption/ionization mass spectrometry were investigated. 2-Aminobenzoic acid/ammonium fluoride (ABA/NH4F) matrix system was used. The spectra obtained under metastable and fast dissociation conditions exhibit distinctive dissociation products. From the post-source-decay analysis, all oligonucleotides underwent predominantly metastable dissociations at the 3' C-O linkages to form [a(n)-B]+ and w(n)+ complimentary ion series. Based on the present results, the so-called "[wn+80]+" ions were postulated to be the complimentary [Z(8-n)AH]+ ions rather than the expected phosphate rearrangement products. In addition, these oligonucleotides were found to generate fast dissociation products of b(n)+, d(N)+, w(N)+ and y(N)+ ions through backbone cleavages at 5' C-O, 5' O-P, 3' C-O and 3' P-O linkages, respectively. Product ion series formed under PSD conditions were not observed. The implications of this mutually exclusive occurrence of the two sets of fragment ions under fast and metastable conditions using ABA/NH4F matrix would be discussed. A model of ion activation under UV-MALDI conditions was also proposed.
Synthesis, molecular structure, and validation of metalloprobes for assessment of MDR1 P-glycoprotein-mediated functional transport (2010)

molecular imaging of the functional transport activity of MDR1 Pgp (ABCB1) with (67/68)Ga-metalloprobes could enable non-invasive monitoring of the blood-brain barrier, tumors, and tissues in vivo.
Conversion Formula for the Celestron Micro Guide Eyepiece Used to Determine Position Angles (2010)

The Celestron Micro Guide eyepiece is used to measure the position angle of double stars. Mathematical formulas are used to convert values from one circular scale to another. This enables observers to measure values on an easy to read scale and convert the readings to values on another scale where the numerals are often more difficult to read. The latter are used to obtain position angles. Observations were made in all four quadrants to test the formula.
Cytogenetics and cancer (2000)

Techniques based on fluorescence in situ hybridization (FISH) have bridged the gap between molecular genetics and conventional cytogenetics. Since its introduction in the late 1980s, advanced FISH-based methods have greatly enhanced the cytogenetic analysis of hematopoietic and solid tumors and are rapidly gaining ground in clinical cytogenetic diagnostics. As interest in FISH technologies has grown, it has inspired an era of new FISH-based technologies such as multiplex FISH, spectral karyotyping, and comparative genomic hybridization. In this review, the focus is on the impact of these technologies in the field of cancer genetics.
Morphological Behavior of Thermally Treated Polystyrene-<i>b</i>-polybutadiene-<i>b</i>-poly(ε-caprolactone) ABC Triblock Copolymers (2003)

The microphase morphology of a series of polystyrene-b-polybutadiene-b-poly(ε-caprolactone) ABC triblock copolymers (SBC) was studied by transmission electron microscopy (TEM) and synchrotron radiation small-angle X-ray scattering (SAXS) for selected samples. The studies were performed as a function of annealing time at high temperature (150 °C). Interestingly, even though crystallization took place under similar conditions (5 h at 40 °C), the annealing time at high temperature can influence the final morphology in such a way that within a copolymer (S51B09C40), a morphological transition from a lamellar−cylindrical (lc) to a cylindrical−ring (cr) morphology can occur. It was also observed that the copolymers reach varied levels of long-range order of the microdomains, depending on the composition. These results combined with the observation or not of well-defined spherulites in the bulk illustrate the strong “conflict” between microphase separation and crystallization, especially when the PCL content is relatively high. The morphological changes are directly related to the thermal behavior of the triblock copolymers, in particular, the melting temperature and Avrami parameter associated with the crystallization kinetics.
Multifunctional Rare-Earth Vanadate Nanoparticles: Luminescent Labels, Oxidant Sensors, and MRI Contrast Agents (2014)

Collecting information on multiple pathophysiological parameters is essential for understanding complex pathologies, especially given the large interindividual variability. We report here multifunctional nanoparticles which are luminescent probes, oxidant sensors, and contrast agents in magnetic resonance imaging (MRI). Eu(3+) ions in an yttrium vanadate matrix have been demonstrated to emit strong, nonblinking, and stable luminescence. Time- and space-resolved optical oxidant detection is feasible after reversible photoreduction of Eu(3+) to Eu(2+) and reoxidation by oxidants, such as H2O2, leading to a modulation of the luminescence emission. The incorporation of paramagnetic Gd(3+) confers in addition proton relaxation enhancing properties to the system. We synthesized and characterized nanoparticles of either 5 or 30 nm diameter with compositions of GdVO4 and Gd0.6Eu0.4VO4. These particles retain the luminescence and oxidant detection properties of YVO4:Eu. Moreover, the proton relaxivity of GdVO4 and Gd0.6Eu0.4VO4 nanoparticles of 5 nm diameter is higher than that of the commercial Gd(3+) chelate compound Dotarem at 20 MHz. Nuclear magnetic resonance dispersion spectroscopy showed a relaxivity increase above 10 MHz. Complexometric titration indicated that rare-earth leaching is negligible. The 5 nm nanoparticles injected in mice were observed with MRI to concentrate in the liver and the bladder after 30 min. Thus, these multifunctional rare-earth vanadate nanoparticles pave the way for simultaneous optical and magnetic resonance detection, in particular, for in vivo localization evolution and reactive oxygen species detection in a broad range of physiological and pathophysiological conditions.
Linear toeplitz space time block codes (2005)

In this paper we consider coherent flat fading wireless communication systems with multiple transmitter antennas and single receiver antenna (MISO). We propose a Toeplitz linear space time block code (STBC) that converts an original MISO flat fading channel into a Toeplitz virtual multiple inputs multiple outputs (MIMO) channel. We show that our proposed code has the following main features: (a) The symbol transmission rate is (T-M + 1)/T, where M is the number of transmitter antenna and T is the number of channel uses (T > M). (b) Linear receivers (zero-forcing and minimum mean square error) can extract full diversity. Moreover, when the channel coefficients are independent and the maximum likelihood (ML) detector is employed, our Toeplitz STBC minimizes the exact worst case average pair-wise error probability, (c) When channels are correlated, we design our Toeplitz STBC that minimizes the exact average worst case pair-wise error probability. By transforming this non-convex optimization problem into a convex one, the problem can be solved efficiently by employing an interior point method. In particular, when the design criterion in question is approximated by the Chernoff bound, we obtain a closed form solution, (d) Finally, for the independent MISO flat fading system, we prove that our proposed codes can approach the optimal diversity-vs-multiplexing tradeoff developed by Zheng and Tse with a linear zero-forcing receiver when the number of channel uses is large
The influence of diet upon liver function tests and serum lipids in healthy male volunteers resident in a Phase I unit (2003)

The rises in transaminases and triglycerides were caused by the carbohydrate content of the diet rather than its calorific value. Sucrose rather than starch was the carbohydrate which caused the rise in transaminases and triglycerides. The importance of controlling diet in Phase I studies is stressed.