gebhart/patrepeval huggingface dataset:
Spin–orbital coupling effects on the photophysical properties and photocytotoxicity of merocyanine dyes (1997)

A series of merocyanine dyes possessing different heteroatoms in the terminal aromatic and barbiturate units has been synthesized. The nature of the heteroatom does not affect the all-trans alignment of the central polyenic bridge, as demonstrated by 1 H NMR spectroscopy. There are pronounced changes, however, in the photophysical properties of the individual molecules due to structural, electronic and spin–orbital coupling effects induced by the heteroatoms. In particular, it has been possible to vary the quantum yield for formation of the lowest-energy triplet excited state by more than two orders of magnitude. Quantum yields and lifetimes for fluourescence and photoisomerization are also affected by the choice of heteroatom. Despite the major changes in triplet yield that take place upon insertion of heteroatoms displaying strong spin–orbital coupling effects (e.g., Se) the efficacy for light-induced cytotoxicity towards cancer cells shows but a modest dependence on the structure of the dye. There is a reasonably good correlation between triplet yield and the rate of light-induced cell killing as might be expected for a mechanism based on intermediate generation of singlet molecular oxygen. However, equally good correlations exist between cell-killing performance and both relative lipophilicity and the rate at which the dye penetrates into intact biological cells.
STUDIES ON TSUSHIMYCIN. II (1969)

The constituent fatty acids of the antibiotic tsushimycin were examined by gas-liquid chromatography, mass spectrometry, nuclear magnetic resonance and infrared spectroscopy. Also, periodate-permanganate oxidation unequivocally indicated the position of double bonds. The structures of two major constituent fatty acids were determined as cis-3-isotetradecenoic acid and cis- 3-anteisopentadecenoic acid. As a result of parallel experiments, the main constituent fatty acid of the antibiotic amphomycin was also elucidated as cis-3-anteisotridecenoic acid.
Efficient Run-time Monitoring Using Shadow Processing. (1995)

General purpose multiprocessors are becoming increasingly common. We propose using pairs of processors, one running an ordinary application program and the other monitoring the application&amp;apos;s execution. We call the processor doing the monitoring a &amp;quot;shadow processor, &amp;quot; as it &amp;quot;shadows&amp;quot; the main processor&amp;apos;s execution. We have developed a prototype shadow processing system which supports full-size programs written in C. Our system instruments an executable user program in C to obtain a &amp;quot;main process&amp;quot; and a &amp;quot;shadow process.&amp;quot; The main process performs computations from the original program, occasionally communicating a few key values to the shadow process. The shadow process follows the main process, checking pointer and array accesses and detecting memory leaks. The overhead to the main process is very low --- almost always less than 10%. Further, since the shadow process avoids repeating some of the computations from the input program, it runs much faster than a single process pe...
Exopolysaccharide Biosynthesis in Lactococcus lactis NIZO B40: Functional Analysis of the Glycosyltransferase Genes Involved in Synthesis of the Polysaccharide Backbone (1999)

ABSTRACT We used homologous and heterologous expression of the glycosyltransferase genes of the Lactococcus lactis NIZO B40 eps gene cluster to determine the activity and substrate specificities of the encoded enzymes and established the order of assembly of the trisaccharide backbone of the exopolysaccharide repeating unit. EpsD links glucose-1-phosphate from UDP-glucose to a lipid carrier, EpsE and EpsF link glucose from UDP-glucose to lipid-linked glucose, and EpsG links galactose from UDP-galactose to lipid-linked cellobiose. Furthermore, EpsJ appeared to be involved in EPS biosynthesis as a galactosyl phosphotransferase or an enzyme which releases the backbone oligosaccharide from the lipid carrier.
Advancements in tissue engineered bone substitutes (1999)

The limitations of autogenous and allogenic bone grafts have driven the search for synthetic alternatives. Using a tissue engineering approach, researchers have developed a series of scaffolds for bone repair applications. In the past year, implants with a variety of structures and compositions have been fabricated. Several of these structures have incorporated bone morphogenetic proteins to provide osteoinductive capabilities. This article describes new bone grafting methods highlighting recent advances in the design and evaluation of several synthetic bone graft substitutes. The trends toward the use of porous biphasic calcium phosphates as bone graft materials and the combination of poly(α-hydroxy acid) scaffolds with recombinant bone morphogenetic proteins are discussed. A new form of synthetic bone graft that can be customized is also described.Curr Opin Orthop 1999, 10:445–451© 1999 Lippincott Williams & Wilkins, Inc.
The insulin-like growth factor (IGF)-dependent IGF binding protein-4 protease secreted by human fibroblasts is pregnancy-associated plasma protein-A (1999)

Proteolytic cleavage of the six known insulin-like growth factor binding proteins (IGFBPs) is a powerful means of rapid structure and function modification of these important growth-regulatory proteins. Intact IGFBP-4 is a potent inhibitor of IGF action in vitro, and cleavage of IGFBP-4 has been shown to abolish its ability to inhibit IGF stimulatory effects in a variety of systems, suggesting that IGFBP-4 proteolysis acts as a positive regulator of IGF bioavailability. Here we report the isolation of an IGF-dependent IGFBP-4-specific protease from human fibroblast-conditioned media and its identification by mass spectrometry microsequencing as pregnancy-associated plasma protein-A (PAPP-A), a protein of unknown function found in high concentrations in the maternal circulation during pregnancy. Antibodies raised against PAPP-A both inhibited and immunodepleted IGFBP-4 protease activity in human fibroblast-conditioned media. Moreover, PAPP-A purified from pregnancy sera had IGF-dependent IGFBP-4 protease activity. PAPP-A mRNA was expressed by the human fibroblasts and osteoblasts, and PAPP-A protein was secreted into the culture medium. In conclusion, we have identified an IGF-dependent IGFBP protease and at the same time assigned a function to PAPP-A. This represents an unanticipated union of two areas of research that were not linked in any way before this report.
CaT1 Contributes to the Stores-operated Calcium Current in Jurkat T-lymphocytes (2002)

T-lymphocyte activation requires sustained Ca(2+) signaling dependent upon capacitative Ca(2+) entry (CCE). The protein(s) that forms the stores-operated Ca(2+) channel (SOCC) responsible for CCE has long been sought but has not been definitively identified. Members of the TRPV family (transient receptor potential superfamily-vanilloid receptor subfamily) of channel genes have been proposed to encode SOCCs responsible for CCE in non-excitable cells. Here we present evidence that a member of the TRPV group, CaT1, is involved in generating I(CRAC), the CCE current that is necessary for T-cell activation. CaT1 is expressed in Jurkat T-lymphocytes. When overexpressed in Jurkat cells, CaT1 produces a Ca(2+) entry current that mimics the endogenous I(CRAC) in its dependence on external Ca(2+), inactivation by elevated concentration of internal Ca(2+), and pharmacological block by capsaicin. Overexpressed CaT1 is partially regulated by the release of internal Ca(2+) stores via thapsigargin or receptor-mediated generation of inositol 1,4,5-trisphosphate. A pore-region mutant of CaT1, TRIA-CaT1, fails to carry Ca(2+) currents and associates with co-expressed wild type CaT1 to functionally suppress permeation of Ca(2+) ions. Expression of the TRIA-CaT1 mutant in Jurkat cells results in suppression of the endogenous I(CRAC). Taken together these results indicate that CaT1 is the channel protein that contributes to T-lymphocyte SOCCs either alone or as a subunit in a heterogeneous channel complex.
Repeated administration of bone marrow-derived mesenchymal stem cells improved the protective effects on a remnant kidney model (2010)

Mesenchymal stem cell (MSC) has been implied to have the therapeutic potential on chronic kidney disease (CKD). However, the underlying mechanism is still unclear and administration frequency of MSCs could be an issue in a chronic disease model. We evaluated the effect of repeated administration of MSCs on a remnant kidney model. MSCs from 5-week male Sprague-Dawley rats were infused by tail vein into 7-week female 5/6 nephrectomized rats after tagging with a fluorescent probe, chloromethyl-1,1-dioctadecyl-3,3,3',3'-tetramethyl- indocarbocyanine perchlorate (CM-Dil). Effect of weekly administration of MSCs was compared with the effect of once injection of MSCs and mesangial cells (MCs) at 1 and 5 weeks, respectively. Engraftment of MSCs into the kidney was evaluated by the presence of CM-Dil fluorescence or SRY gene expression. Weekly MSCs administration showed significant improvement in systolic blood pressure (SBP), urinary protein excretion amount, and serum creatinine level at 5 weeks, whereas once MSCs or MCs administration did not. Although once MSCs administration attenuated glomerulosclerosis and infiltration of ED-1 positive cells at 5 weeks as compared with MCs, weekly MSC administration led to a more significant improvement. Renal SRY gene expression and presence of CM-Dil-tagged cells could be confirmed at 1 week after injection of MSCs or weekly injected group, but not at 5 weeks after once injection. MSCs attenuated cortical expression of interleukin (IL)-6 and elevated the expression of IL-10, but these effects were only sustained in the weekly group. Thus, repeated administration of MSCs improves the protective effect on remnant kidney injury, but primarily via the paracrine effect rather than differentiation.
一个可怕的理性主义者——K.阿佩尔 (1983)

法兰克福学派的哲学家K.O.阿佩尔反对当前存在的贬低规范的、合乎逻辑的或伦理学的思想倾向,试图建立一个新学科:从盎格鲁撒克逊人的分析思想中得到启发的“先验的实用主义力。K.O.阿佩尔1922年生于杜塞尔多夫,曾任美因兹大学、基尔大学和萨尔布吕肯大学教授,后来在法兰克福大学任教。他在1973年出版了《哲学的变革》(上、下卷)一书,该书1976年以袖珍本再版,这部作品不仅想要起一种总结的作用,而且也期望建立一个新的学科——“先验的实用主义”。K.O.阿佩尔所走的道路代表了德国当代的哲学运动,德国当代哲学果断地对盎格鲁撒克逊人的分析思想产生了兴趣,以便拯救和实现摆脱了羁绊的理性主义灵感。
Charge Detection Mass Spectrometry Measurements of Exosomes and other Extracellular Particles Enriched from Bovine Milk (2020)

The masses of particles in a bovine milk extracellular vesicle (EV) preparation enriched for exosomes were directly determined for the first time by charge detection mass spectrometry (CDMS). In CDMS, both the mass-to-charge ratio (<i>m</i>/<i>z</i>) and <i>z</i> are determined simultaneously for individual particles, enabling mass determinations for particles that are far beyond the mass limit (∼1.0 MDa) of conventional mass spectrometry (MS). Particle masses and charges span a wide range from <i>m</i> ∼ 2 to ∼90 MDa and <i>z</i> ∼ 50 to ∼1300 e (elementary charges) and are highly dependent upon the conditions used to extract and isolate the EVs. EV particles span a continuum of masses, reflecting the highly heterogeneous nature of these samples. However, evidence for unique populations of particles is obtained from correlation of the charges and masses. An analysis that uses a two-dimensional Gaussian model, provides evidence for six families of particles, four of which having masses in the range expected for exosomes. Complementary proteomics measurements and electron microscopy (EM) imaging are used to further characterize the EVs and confirm that these samples have been enriched in exosomes. The ability to characterize such extremely heterogeneous mixtures of large particles with rapid, sensitive, and high-resolution MS techniques is critical to ongoing analytical efforts to separate and purify exosomes and exosome subpopulations. Direct measurement of each particle's mass and charge is a new means of characterizing the physical and chemical properties of exosomes and other EVs.
Role of Estrogens in Adipocyte Development and Function (2004)

Estrogen has historically been viewed as a major regulator of adipose tissue in adult females, but recent work has indicated that estrogen's role in adipose biology may be broader than initially appreciated and has also provided important insights into the mechanism of estrogen effects on adipose tissue. Estrogen has direct effects on adipocytes to inhibit lipogenesis and may also have direct effects on other cellular constituents of adipose tissue, as well as metabolic effects on other target organs that can regulate adipose tissue. Estrogen has central effects on food consumption and energy expenditure that contribute to its overall inhibitory effects on adipose deposition. Estrogen also plays an important role in regulating adipose deposition in males and recently has been shown to be an important factor in the determination of adipocyte number, indicating that it regulates key developmental events in adipogenesis. Although critical questions still remain in our understanding of the overall role of estrogen in adipose tissue, it is clear that estrogen plays a more important role in adipose tissue than originally realized and that it is a major regulator of adipose tissue in both sexes during development and adulthood.
Inhibitory Effects ofScutellaria BarbataD. Don. andEuonymus Alatus Sieb. on Aromatase Activity of Human Leiomyomal Cells (2004)

It is now well documented that a large proportion of breast tumors express their own aromatase. This intratumoral aromatase produces estrogen in situ and therefore may contribute significantly to the amount of estrogen to which the cell is exposed. Thus it is not only important that aromatase inhibitors potently inhibit the peripheral production of estrogen and eliminate the external supply of estrogen to the tumor cell, but that they in addition potently inhibit intratumoral aromatase and prevent the tumor cell from making its own estrogen within the cell. To study the inhibition of intracellular aromatase, we have examined the aromatase-inhibiting potency of the Scutellaria barbata D. Don. (SB) and Euonymus alatus Sieb. (EA) in myometrial and leiomyomal cells which contain aromatase. We have also used human placental tissues. Although SB and EA are approximately equipotent in a cell-free aromatase system (human placental microsomes), EA is consistently 10-30 times more potent than SB in inhibiting intracellular aromatase in myometrial and leiomyomal cells. To provide insights into the effect of SB and EA on aromatase activity in leiomyomal cells, we examined the cell lines, which is induced to differentiate toward the more transformed cell phenotype by 12-tetradecanoylphorbal-13-acetate (TPA) as a protein kinase C activator and transforming growth factor-beta1 (TGF-beta1). Enzyme activity was inhibited in a time-and dose-dependent fashion by SB and EA and by either 1-50 nM TPA or 0.01-0.5 ng/ml TGF-beta1, with maximal responses after 2-3 h exposure.
10 Φ grid-connection PV power inverter with partial active power filter (2003)

This paper presents a single-phase three-wire (1/spl phi/ 3W) grid-connection photovoltaic (PV) power inverter with a of partial active power filter (PAPF) feature, which can not only deal with PV power but filter current harmonics and improve power factor. Once the processed power exceeds the switch ratings, the inverter can reduce its output reactive power and harmonic power, while still supplying the maximum real power generated by the PV arrays. In the derivation of control laws, a limit circle is defined to confine the output power of the inverter. To determine the power that the inverter can process, the instantaneous reactive power of a 1/spl phi/ 3W system is defined and used to calculate reactive power, which can avoid complex detections of phase angle and magnitude of the fundamental component of a nonlinear load current. Simulation results and experimental measurements have verified the proposed algorithm and the feasibility of the inverter.
The Nerve of Glaucoma! (1994)

Contemporary concepts of open angle glaucoma suggest that the current emphasis on reduction of elevated intraocular pressure could be augmented by other therapeutic approaches. In this article, we describe significant recent developments in the molecular and cellular biology and neuropharmacology of nerve damage that are likely, in coming years, to suggest new therapeutic approaches to the management of glaucoma. These developments may lead to the achievement of pharmacologic protection of the optic nerve from damage or possibly promotion of reversal of damage. We review selected studies of excitotoxins and N-methyl-D-aspartate receptor antagonists, Ca(2+)-induced damage and calcium channel blockers, the intracellular messenger nitric oxide and its perturbation, free-radical damage and scavengers, nerve regeneration, and growth factors. Several basic research questions are posed, answers to which may transform our concepts of glaucoma therapy.
Smart Particles as Foam and Liquid Marble Stabilizers (2008)

Small particles adsorbed to gas-liquid interfaces are widely observed and utilized in many products and various industrial sections, such as flotation, washing, food, water treatment, treatment of radioactive wastes, and distillation in the petroleum industry. After a dormant period of nearly half a century, there is a revival of interests in studying their behaviour. Colloidal particles with a suitable wettability can strongly adsorb to gas-liquid interfaces, and can work as effective stabilizers for foams and liquid marbles (dry liquids). This article presents an overview of current research activities that center on foams and liquid marbles stabilized with well-defined colloidal particles. It is organized into three parts: i) brief discussions of small particles adsorbed to gas-liquid interfaces and their characterizations; ii) demonstrations of aqueous foams stabilized with inorganic or organic particles; and iii) demonstrations of liquid marbles (dry liquids) stabilized with colloidal particles.
Hypothalamic regulation of sleep and arousal (2003)

The hypnogenic function of the rostral hypothalamic region, particularly the preoptic area (POA) was established previously on the basis of lesion, neuronal unit recording, and neurochemical and thermal stimulation studies. Recent studies have mapped the locations of putative sleep-promoting neurons in the POA using c-Fos immunostaining techniques and confirmed these findings with electrophysiological methods. Segregated groups of sleep-active neurons have been localized in the ventrolateral POA (vlPOA) and median preoptic nucleus (MnPN). MnPN and vlPOA sleep-active neurons express the inhibitory transmitter, GABA. In vlPOA neurons, GABA is co-localized with a second inhibitory transmitter, galanin. Descending projections from these sites terminate in putative arousal-promoting cell groups, including histaminergic, serotonergic, orexinergic, noradrenergic, and cholinergic neurons. These findings suggest the hypothesis that non-REM sleep occurs as a consequence of GABAergic and galaninergic inhibition of arousal-promoting neurons resulting from activation of vlPOA and MnPN sleep-promoting neurons. In support of this hypothesis, it was shown that putative sleep-promoting and arousal-promoting neurons exhibit reciprocal changes in discharge across the sleep-wake cycle and that GABA release in wake-promoting sites increases during nonREM sleep. In addition, some POA sleep-active neurons are warm-sensitive. Local POA warming inhibits discharge of multiple arousal-promoting neuronal groups. POA warming, unit recording, and lesion studies also show that POA regulates the amount of delta EEG activity within nonREM sleep, and index of the depth of sleep. Finally, there is evidence that arousal systems inhibit vlPOA and MnPN neurons and the POA hypnogenic mechanism. Mutually-inhibitory interactions between sleep-promoting and arousal-promoting systems are hypothesized to form a functional sleep-wake switch.
Adaptive comb filtering for harmonic signal enhancement (1986)

A new algorithm is presented for adaptive comb filtering and parametric spectral estimation of harmonic signals with additive white noise. The algorithm is composed of two cascaded parts. The first estimates the fundamental frequency and enhances the harmonic component in the input, and the second estimates the harmonic amplitudes and phases. Performance analysis provides new results for the asymptotic Cramer-Rao bound (CRB) on the parameters of harmonic signals with additive white noise. Results of simulations indicate that the variances of the estimates are of the same order of magnitude as the CRB for sufficiently large data sets, and illustrate the performance in enhancing noisy artificial periodic signals.
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors (2016)

A new subseries of substituted piperidines as p53-HDM2 inhibitors exemplified by 21 has been developed from the initial lead 1. Research focused on optimization of a crucial HDM2 Trp23-ligand interaction led to the identification of 2-(trifluoromethyl)thiophene as the preferred moiety. Further investigation of the Leu26 pocket resulted in potent, novel substituted piperidine inhibitors of the HDM2-p53 interaction that demonstrated tumor regression in several human cancer xenograft models in mice. The structure of HDM2 in complex with inhibitors 3, 10, and 21 is described.
Glucagon-Like Peptide I Reduces Postprandial Glycemic Excursions in IDDM (1995)

Effects of human glucagon-like peptide I (GLP-I)(7-36)amide were examined in volunteers having insulin-dependent diabetes mellitus (IDDM) with residual C-peptide (CP) secretion (n = 8, 7 men and 1 woman; age, 31 +/- 1.4 years; body mass index, 24.7 +/- 0.7 kg/m2; duration of diabetes, 3.2 +/- 0.8 years; insulin dose, 0.41 +/- 0.05 U.kg-1.day-1; meal-stimulated CP, 1.0 +/- 0.2 nmol/l [means +/- SE]). After a mixed meal (Sustacal, 30 kJ/kg body wt), intravenous injection of GLP-I, 1.2 pmol.kg-1.min-1 through 120 min, virtually abolished increments of plasma glucose, CP, pancreatic polypeptide (PP), and glucagon concentrations, with no significant effect on plasma gastrin levels during the infusions. At reduced dosage (0.75 pmol.kg-1.min-1), GLP-I had lesser effects on plasma glucose and CP levels. On cessation of intravenous GLP-I infusions after the meals, plasma glucose, CP, PP, and glucagon concentrations rebounded toward control levels by 180 min, and the response of plasma gastrin was prolonged. These rebound responses are consistent with intestinal delivery of food retained in the stomach on escape from inhibition of gastric emptying by GLP-I. Infusion of 1.2 pmol.kg-1.min-1 GLP-I with 20 g glucose (10% dextrose in water) injected intravenously over 60 min enhanced plasma responses of immunoreactive CP; the mean incremental areas under concentration curves (0-60 min) increased sixfold, but the glycemic excursion was not affected. Thus, in CP-positive IDDM, pharmacological doses of GLP-I reduce glycemic excursions after meals by a mechanism(s) not dependent on stimulation of insulin secretion, presumably involving delayed gastric emptying.(ABSTRACT TRUNCATED AT 250 WORDS)