gebhart/patrepeval huggingface dataset:
Novel Compounds with new Anti‐Ulcergenic Activity from <i>Convolvulus pilosellifolius</i> Using Bio‐Guided Fractionation. (2016)

Oral administration of the total alcohol extract of Convolvulus pilosellifolius Desr. (250 and 500 md/kg) showed potent anti-ulcerogenic activity in absolute ethanol-induced ulcer model in rats; it showed percent protection of control ulcer by 69.2 and 84.6%, respectively, while standard ranitidine (100 mg/kg) exhibited 46.2%. Bio-guided work leads to isolation of two novel compounds (1 and 2), which were identified through <sup>1</sup> H, <sup>13</sup> C NMR, HMPC, HMQC and DEPT as: methyl 2-(hydroxymethyl) octanoate, named as amanitate, and 16-amino-9,13-dimethyl-17-(prop-1-en-2-yl)-hexadecahydro-1H-cyclopenta[a] phenanthren-3-ol, named as asmatol. Both compounds (50 mg/kg) possessed anti-ulcerogenic activity with 95.4% and 55.84% protection, respectively. Two known compounds (3 and 4) were also isolated and identified through comparison with authentic samples and confirmed through different NMR techniques as kampeferol and quercetin. These compounds also showed anti-ulcerogenic activity with 78.38% and 5.38% protection, respectively. The cytoprotective mechanism explains the potent anti-ulcerogenic activity of the total alcohol extract and the isolated compounds. The extract was highly safe as the LD<sub>50</sub> was more than 5000 mg/kg. These results were well supported by the sub-chronic toxicity study, as the extract (500 mg/kg) administrated orally to rats for 35 consecutive days showed no alteration in the liver and kidney functions. Copyright © 2016 John Wiley & Sons, Ltd.
Intravesical liposome drug delivery and IC/BPS. (2015)

Intravesical therapy has previously shown to be effective in delaying or preventing recurrence of superficial bladder cancer. This local route of drug administration is now demonstrating promise in the treatment of interstitial cystitis/bladder pain syndrome (IC/BPS) with the benefit of minimal systemic side effects. Liposomes (LPs) are lipid vesicles composed of phospholipid bilayers surrounding an aqueous core. They can incorporate drug molecules, both hydrophobic and hydrophilic, and vastly improve cellular uptake of these drug molecules via endocytosis. Intravesical LPs have therapeutic effects on IC/BPS patients, mainly due to their ability to form a protective lipid film on the urothelial surface and repair the damaged urothelium. This review considers the current status of intravesical LPs and LP mediated drug delivery for the treatment of IC/BPS.
200Gb/s 10-channel miniature optical interconnect transmitter module for high-performance computing (HPC) (2010)

A major breakthrough to alleviating the interconnect bottleneck in intra cabinet system in HPC may happen by bringing optics directly to the processor package. In order to do so efficient and compact optical interconnect subassembly modules that utilize simple optical and electrical interfacing schemes are needed. In our current work the development of a novel 10-channel, miniature 7mm(W)x1.8mm(L)x3mm(H), optical interconnect transmitter subassembly module is described. The module consists of a high precision molded optical alignment unit with integrated microlens arrays, highspeed coplanar waveguide (CPW) electrical interfaces and a VCSEL (Vertical Cavity Surface Emitting Laser) array chip which is flip chip mounted. The module is designed to uniquely interface vertically with high-speed electrical I/O lines on a microprocessor style package or a motherboard to convert electrical signals to optical for transmission to other similar units using a standard (Multi-Terminal) MT style optical connector. We report on optical coupling efficiency, misalignment tolerance and high-speed electrical and optical measurements of the module. We have measured 40Gb/s electrical eye for the CPW interfaces on the module and 20Gb/s clear optical eyes for VCSEL assembled module from all the 10 channels to produce an aggregate transmitter bandwidth of 200Gb/s. We also measured 30Gb/s electrical and 20Gb/s optical eyes for the optical subassembly module that is bonded onto a microprocessor style package substrate.
Efficient Algorithms for Coded Multicasting in Heterogeneous Caching Networks (2019)

Coded multicasting has been shown to be a promising approach to significantly improve the performance of content delivery networks with multiple caches downstream of a common multicast link. However, the schemes that have been shown to achieve order-optimal performance require content items to be partitioned into several packets that grows exponentially with the number of caches, leading to codes of exponential complexity that jeopardize their promising performance benefits. In this paper, we address this crucial performance-complexity tradeoff in a heterogeneous caching network setting, where edge caches with possibly different storage capacity collect multiple content requests that may follow distinct demand distributions. We extend the asymptotic (in the number of packets per file) analysis of shared link caching networks to heterogeneous network settings, and present novel coded multicast schemes, based on local graph coloring, that exhibit polynomial-time complexity in all the system parameters, while preserving the asymptotically proven multiplicative caching gain even for finite file packetization. We further demonstrate that the packetization order (the number of packets each file is split into) can be traded-off with the number of requests collected by each cache, while preserving the same multiplicative caching gain. Simulation results confirm the superiority of the proposed schemes and illustrate the interesting request aggregation vs. packetization order tradeoff within several practical settings. Our results provide a compelling step towards the practical achievability of the promising multiplicative caching gain in next generation access networks.
Induction of CYP3A4 by 1 alpha,25-dihydroxyvitamin D3 is human cell line-specific and is unlikely to involve pregnane X receptor. (2001)

Under certain culture conditions, exposure of the human colon adenocarcinoma cell line Caco-2 to 1,25-(OH)(2)-D(3) induces expression of CYP3A4 to levels comparable to that in human small intestinal epithelium. To determine whether 1,25-(OH)(2)-D(3) could be used to restore CYP3A expression in other culture models, we examined several cell lines derived from malignancies of human tissues known to express CYP3A enzymes: Hep G2 (liver), LS180 (colon), HPAC (pancreas), Hs746T (stomach). Primary cultures of human hepatocytes from two donors were also examined. 1,25-(OH)(2)-D(3) increased CYP3A catalytic activity in LS180 (15-fold), HPAC (6-fold), and hepatocytes (2- to 3-fold); this was accompanied by induction of CYP3A4 mRNA and CYP3A immunoreactive protein. However, 1,25-(OH)(2)-D(3) had no effect on CYP3A expression in Hs746T or Hep G2. Known ligands for pregnane X receptor (PXR) (rifampin, dexamethasone, and dexamethasone t-butyl acetate) markedly induced CYP3A4 expression in human hepatocytes. In contrast, these ligands had little or no effect on CYP3A4 expression in Caco-2 cells, even at concentrations 1 to 2 orders of magnitude greater than effective concentrations of 1,25-(OH)(2)-D(3) or two other vitamin D receptor (VDR) ligands (25-OH-D(3) and 1-OH-D(3)). The retinoic acid receptor ligand all-trans-retinoic acid augmented the 1,25-(OH)(2)-D(3)-mediated induction of CYP3A4 catalytic activity up to 2-fold in Caco-2 cells, while having no demonstrable effect on levels of CYP3A4 mRNA or protein. The retinoid X receptor ligand 9-cis-retinoic acid appeared to slightly reduce CYP3A4 catalytic activity. We conclude that 1,25-(OH)(2)-D(3) can be used to increase CYP3A4 expression in some, but not all, human cell lines derived from tissues known to express CYP3A enzymes. The mechanisms involved in this induction are unlikely to involve PXR and may involve VDR.
A cloning and expression system to probe T-cell receptor specificity and assess functional avidity to neoantigens (2018)

Recent studies have highlighted the promise of targeting tumor neoantigens to generate potent antitumor immune responses and provide strong motivation for improving our understanding of antigen-T-cell receptor (TCR) interactions. Advances in single-cell sequencing technologies have opened the door for detailed investigation of the TCR repertoire, providing paired information from TCRα and TCRβ, which together determine specificity. However, a need remains for efficient methods to assess the specificity of discovered TCRs. We developed a streamlined approach for matching TCR sequences with cognate antigen through on-demand cloning and expression of TCRs and screening against candidate antigens. Here, we first demonstrate the system's capacity to identify viral-antigen-specific TCRs and compare the functional avidity of TCRs specific for a given antigen target. We then apply this system to identify neoantigen-specific TCR sequences from patients with melanoma treated with personalized neoantigen vaccines and characterize functional avidity of neoantigen-specific TCRs. Furthermore, we use a neoantigen-prediction pipeline to show that an insertion-deletion mutation in a putative chronic lymphocytic leukemia (CLL) driver gives rise to an immunogenic neoantigen mut-<i>MGA,</i> and use this approach to identify the mut-<i>MGA</i>-specific TCR sequence. This approach provides a means to identify and express TCRs, and then rapidly assess antigen specificity and functional avidity of a reconstructed TCR, which can be applied for monitoring antigen-specific T-cell responses, and potentially for guiding the design of effective T-cell-based immunotherapies.
Multicomponent Remote Sensing of Vehicle Exhaust by Dispersive Absorption Spectroscopy. 2. Direct On-Road Ammonia Measurements (2001)

Remote sensing was employed for the first time to measure NH3 levels in the exhaust of on-road light duty motor vehicles. The sensor also measured the concentration of CO2, CO, hydrocarbons, and NO, among other pollutants, in the emitted exhaust. Field measurements were conducted at a Los Angeles freeway on-ramp; vehicles traveled at cruise speeds between 20 and 25 m s(-1) (45-55 mi h(-1)). Mean fleet NH3 levels of 44.7 +/- 4.1 ppm were observed. These emissions exhibited a highly skewed distribution: 50.1% of the emitted NH3 was contributed by 10% of the sampled fleet. The pollutant distribution among high NH3 emitters is analyzed to identify the conditions that lead to three-way catalyst malfunction and, hence, NH3 formation. In contradiction with previous reports, we found that high NH3 emissions could not be attributed to vehicles running under rich air-fuel conditions. We estimate a mean fleet NH3 mass emission rate of 667 +/- 57 mg L(-1) (Er = 94 +/- 8 mg km(-1)). These findings could have significant implications on air quality in the South Coast Air Basin (SoCAB) of California, since they support the hypothesis that emissions from motor vehicles constitute a dominant regional source of NH3, between 20 and 27% of total daily emissions. As NH3 is the predominant atmospheric base, tropospheric levels play a key role in the buffering capacity of the atmosphere and, hence, the formation of fine aerosol. Our results could explain the ubiquitous distribution of ammonium fine particles observed during fall stagnation conditions in the SoCAB.
Time-resolved resonance fluorescence spectroscopy for study of chemical reactions in laser-induced breakdown spectroscopy (2017)

Laser-induced breakdown spectroscopy only provides limited information about chemical products in laser-induced plasmas. In this work, time-resolved resonance fluorescence spectroscopy was studied as a promising tool for the study of chemical reactions in laser-induced plasmas.
Selective and Bioavailable Inhibitors of Collagen Prolyl 4‐Hydroxylase (2015)

Collagen is the most abundant protein in animals. A variety of diseases are associated with the overproduction of collagen including cancer metastasis. The stability of collagen relies on post‐translational modifications that occur throughout the secretory pathway. One of the most important modifications is the hydroxylation of collagen strands by collagen prolyl 4‐hydroxylases (CP4Hs). Catalysis by CP4Hs converts proline residues to hydroxyproline residues, which are essential for the conformational stability of mature collagen strands. Importantly, CP4Hs are validated targets for the treatment of metastatic breast cancer, a significant unmet clinical need. Nonetheless, a therapy based upon this strategy has yet to emerge, primarily due to the difficulty in designing selective inhibitors for members of this enzyme family. Herein, we use a chemical approach based upon the classic 2,2′‐bipyridine (bipy) scaffold to probe the active site of human CP4H1 and understand the determinants of selectivity for this enzyme. Then, we redesign the bipy scaffold to enhance its pharmacological properties and generate potent biheteroaryl inhibitors that are selective for human CP4H1. Evaluations of these inhibitors in cell culture suggest that they are bioavailable and inhibit collagen synthesis at concentrations that do not disrupt iron homeostasis or cause general cytotoxicity. These results suggest the potential use of these inhibitors as leads for the development of antimetastatic therapeutics. This work was supported by grant R01 AR044276 (NIH).
Cationic Oligofluorene‐Substituted Polyhedral Oligomeric Silsesquioxane as Light‐Harvesting Unimolecular Nanoparticle for Fluorescence Amplification in Cellular Imaging (2009)

A new bottom-up strategy is used to construct water-soluble organic/inorganic fluorescent unimolecular nanoparticles based on polyhedral oligomeric silsesquioxane (POSS) and conjugated oligoelectrolyte. Their high quantum yield, good cytocompatibility, and unique whole-cell permeability could serve as a light-harvesting energy donor to amplify the intracellular dye fluorescence for high-quality biological imaging through fluorescence resonance energy transfer (see image).
Abstract 1209: Bone Morphogenic Protein-4 is Elevated in Chronic Kidney Disease Patients with Coronary Artery Disease (2006)

PUR0200 treatment caused bronchodilation in COPD patients that was similar in magnitude to that caused by tiotropium HH. This enabled a similar clinical effect on lung function to be achieved with PUR0200 using a lower metered dose of tiotropium compared with tiotropium HH.
Universal Optical Frequency Comb (2010)

We demonstrate that whispering gallery mode resonators can be utilized to generate optical frequency combs based on four wave mixing process at virtually any frequency that lies in the transparency window of the resonator host material. We show theoretically how the morphology of the resonator can be engineered to produce a family of spectrally equidistant modes with anomalous group velocity dispersion appropriate for the comb generation. We present experimental results for a frequency comb centered at 794 nm to support our theoretical findings.
Combined michelson and polarimetric fibre-optic interferometric sensor (1985)

A fibre-optic interferometric sensor utilising a highly birefringent fibre sensing element has been configured such that both Michelson and polarimetric outputs are simultaneously available. This device therefore offers the high resolution of a Michelson interferometer in conjunction with the increased dynamic range of a polarimetric device. The results of preliminary experiments in which the system was used as a temperature sensor are presented.
Size Performance of the Attractive Force for a Dental Magnetic Attachment. (1996)

A dental magnetic attachment is a denture retainer that makes it possible to design a denture without extracting any teeth. There is a strong need to miniaturize such attachments. We designed an advanced magnetic attachment that occupies over 40% less volume with an attractive force of 6.6 N using Nd-Fe-B magnet and the optimum dimension. The design allows the attachment to be used in all kinds of clinical cases. Furthermore, little influences on the attractive force is observed to be exerted by round corners and side grooves attached to yokes, which improve laboratory procedures for designing dentures.
New method for 3D reconstruction in digital tomosynthesis (2002)

Digital tomosynthesis mammography is an advanced x-ray application that can provide detailed 3D information about the imaged breast. We introduce a novel reconstruction method based on simple backprojection, which yields high contrast reconstructions with reduced artifacts at a relatively low computational complexity. The first step in the proposed reconstruction method is a simple backprojection with an order statistics-based operator (e.g., minimum) used for combining the backprojected images into a reconstructed slice. Accordingly, a given pixel value does generally not contribute to all slices. The percentage of slices where a given pixel value does not contribute, as well as the associated reconstructed values, are collected. Using a form of re-projection consistency constraint, one now updates the projection images, and repeats the order statistics backprojection reconstruction step, but now using the enhanced projection images calculated in the first step. In our digital mammography application, this new approach enhances the contrast of structures in the reconstruction, and allows in particular to recover the loss in signal level due to reduced tissue thickness near the skinline, while keeping artifacts to a minimum. We present results obtained with the algorithm for phantom images.
Ambient-Temperature Direct Synthesis of Poly(organophosphazenes) via the “Living” Cationic Polymerization of Organo-Substituted Phosphoranimines (1997)

A new, ambient-temperature method for the direct synthesis of organo-substituted polyphosphazenes is described. It involves the initiation of a series of organophosphoranimines R(R‘)XPNSiMe3 (3, R = Ph, R‘ = X = Cl; 5, R = R‘ = Ph, X = Cl; 7, R = Me, R‘ = Et, X = Cl; 9, R = R‘ = CF3CH2O, X = Br) with catalytic amounts of PCl5 in CH2Cl2 to yield (after treatment with NaOCH2CF3 in the case of 3) the corresponding polyphosphazene species (NPRR‘)n (4, R = Ph, R‘ = OCH2CF3; 6, R = R‘ = Ph; 8, R = Me, R‘ = Et; 10, R = R‘ = OCH2CF3) with narrow polydispersities. The molecular weights of the polyphosphazenes were controlled by altering the ratio of monomer to initiator. The polymer chains were found to be active after chain propagation since further addition of monomer resulted in the formation of higher molecular weight polymer. For monomers 7 and 9 optimum polymerization behavior was found to occur at 35 °C in the absence of solvent in the presence of catalytic quantities of PCl5. These reactions proceeded to 100% completion, while maintaining molecular weight control and narrow polydispersites. In the case of polymers 4, 8, and 10, which were synthesized with a 10:1 monomer to initiator ratio in CH2Cl2, the resultant polymers were analyzed by gel permeation chromatography (GPC) (4, Mn = 2.9 × 103, polydispersity (PDI = Mw/Mn) = 1.07); 8, Mn = 2.2 × 103, PDI = 1.31; 10, Mn = 7.8 × 103, PDI = 1.23). Poly(diphenylphosphazene), (NPPh2)n (6), was insoluble in common organic solvents and was characterized by magic angle spinning (MAS) solid state 31P NMR spectroscopy. The effects of side group steric bulk, electron-withdrawing or -donating properties, and leaving group types on the ambient-temperature cationic induced polymerizations are discussed.
Oral immunization of humans with Streptococcus sobrinus glucosyltransferase (1987)

The effect of oral administration of glucosyltransferase (GTF) from Streptococcus sobrinus 6715 on levels of immunoglobulin A (IgA) antibody to GTF in parotid saliva and on the number of indigenous Streptococcus mutans in the whole saliva was studied in young adult males. GTF combined with aluminum phosphate (AP) was administered in capsules to 14 subjects, while sodium phosphate buffer combined with AP was administered in the same way to 11 control subjects. Thirteen administrations were given during the first immunization regimen, and five administrations, approximately 3 months later, constituted the second immunization regimen. All subjects were given professional dental prophylaxis immediately prior to each immunization. Each subject served as his own control by using antibody and bacterial data collected prior to antigen administration for comparison. After the first immunization regimen, the GTF vaccine group exhibited a significantly higher distribution (P less than 0.05) of normalized parotid saliva IgA antibody elevations than observed in the placebo group. Between the first and second immunization regimens a significant increase (P less than 0.05) in parotid salivary anti-GTF activity also occurred in the GTF vaccine but not the placebo group. No significant differences between these two groups were observed on any occasion when serum IgG or IgA antibody to GTF was analyzed. Comparison of the group mean log ratios (post- to prevaccine administration) of S. mutans to total streptococci in whole saliva revealed that the GTF vaccine group values were always lower than those of the placebo group. These differences reached significance (P less than 0.01) on three of the last four sampling occasions (days 21, 35, and 42) following initiation of the first immunization regimen. The mean log ratios of the GTF vaccine group were also lower than those of the placebo group after the second immunization regimen but did not reach significance. These data indicate that oral administration of GTF from the mutans streptococci has the potential to elicit a salivary IgA antibody response when combined with an aluminum-based adjuvant and that this response can interfere with the reaccumulation of indigenous S. mutans following dental prophylaxis.
Tricyclic analogues of artemisinin: synthesis and antimalarial activity of (+)-4,5-secoartemisinin and (–)-5-nor-4,5-secoartemisinin (1990)

M. A. Avery, W. K. M. Chong and J. E. Bupp, J. Chem. Soc., Chem. Commun., 1990, 1487 DOI: 10.1039/C39900001487
Rank modulation for flash memories (2008)

We explore a novel data representation scheme for multi-level flash memory cells, in which a set of n cells stores information in the permutation induced by the different charge levels of the individual cells. The only allowed charge-placement mechanism is a ‘push-to-the-top’ operation which takes a single cell of the set and makes it the top-charged cell. The resulting scheme eliminates the need for discrete cell levels, as well as overshoot errors, when programming cells. We present unrestricted Gray codes spanning all possible n-cell states and using only ‘push-to-the-top’ operations, and also construct balanced Gray codes. We also investigate optimal rewriting schemes for translating arbitrary input alphabet into n-cell states which minimize the number of programming operations.
Thin-film rechargeable lithium batteries (1995)

Thin-film rechargeable lithium batteries using ceramic electrolyte and cathode materials have been fabricated by physical deposition techniques. The lithium phosphorous oxynitride electrolyte has exceptional electrochemical stability and a good lithium conductivity. The lithium insertion reaction of several different intercalation materials, amorphous V{sub 2}O{sub 5}, amorphous LiMn{sub 2}O{sub 4}, and crystalline LiMn{sub 2}O{sub 4} films, have been investigated using the completed cathode/electrolyte/lithium thin-film battery.
Amplitude encoded phase-only filters (1989)

The phase-only filter (POF) and binary phase-only filter (BPOF) have been shown to have high optical efficiency, good target discrimination, and virtually no sidelobes. We present a simple method of amplitude encoding the signal phase information. These new filters have most of the same advantages of a POF or BPOF so that amplitude modulating spatial light modulators or photographic film can be used.