gebhart/patrepeval huggingface dataset:
Potentiation of Antitumor Activity of Vincristine by the Biscoclaurine Alkaloid Cepharanthine (1987)

A membrane stabilizer, the biscoclaurine alkaloid cepharanthine markedly enhanced the cytotoxicity of vincristine (VCR) and adriamycin in cultured L1210 cells at a noncytotoxic dose. When 0.1-0.5 micrograms cepharanthine/ml was added along with VCR to L1210 cells in vitro, the cytotoxicity of VCR was potentiated 1.5-fold to 7-fold, whereas such potentiation was not found in mitomycin C, bleomycin, and 5-fluorouracil. The potentiating action of cepharanthine was stronger when the cells were preincubated with cepharanthine prior to the treatment of cells with VCR and cepharanthine, suggesting that a long-term contact with cells is required for the enhancement. Cepharanthine was found to induce the increase of the cellular level of VCR in L1210 cultured cells. It was suggested that the accumulation of VCR is due to the inhibition of a VCR efflux function of the cells. The administration of cepharanthine at the dose of 5 mg/kg/day for 10 days with VCR significantly enhanced the antitumor activity of VCR in L1210 leukemia and P388 leukemia (P less than .025). However, the combined effect of cepharanthine and VCR in this regimen was marginal synergism. When the same dose of cepharanthine was administered in split administration, three times daily for 10 days, the therapeutic effect of VCR was further enhanced compared to its effect under the former regimen. Furthermore, cepharanthine was found to partially overcome the resistance of VCR in P388/VCR.
Efficacy and Safety of a New Vaginal Contraceptive Antimicrobial Formulation Containing High Molecular Weight Poly(Sodium 4-Styrenesulfonate)1 (2002)

Host cell infection by sexually transmitted disease (STD)-causing microbes and fertilization by spermatozoa may have some mechanisms in common. If so, certain noncytotoxic agents could inhibit the functional activity of both organisms. High molecular mass poly(sodium 4-styrenesulfonate) (T-PSS) may be one of these compounds. T-PSS alone (1 mg/ml) or in a gel (2% or 5% T-PSS) completely prevented conception in the rabbit. Contraception was not due to sperm cytotoxicity or to an effect on sperm migration. However, T-PSS inhibited sperm hyaluronidase (IC(50) = 5.3 microg/ml) and acrosin (IC(50) = 0.3 microg/ml) and caused the loss of acrosomes from spermatozoa (85% maximal loss by 0.5 microg/ml). T-PSS (5% in gel) also reduced sperm penetration into bovine cervical mucus (73% inhibition by 1 mg gel/ml). T-PSS (5% in gel) inhibited human immunodeficiency virus (HIV; IC(50)= 16 microg gel/ml) and herpes simplex viruses (HSV-1 and HSV-2; IC(50) = 1.3 and 1.0 microg gel/ml, respectively). The drug showed high efficacy against a number of clinical isolates and laboratory strains. T-PSS (5% in gel) also inhibited Neisseria gonorrhea (IC(50) < 1.0 gel/ml) and Chlamydia trachomatis (IC(50) = 1.2 microg gel/ml) but had no effect on lactobacilli. These results imply that T-PSS is an effective functional inhibitor of both spermatozoa and certain STD-causing microbes. The noncytotoxic nature should make T-PSS safe for vaginal use. T-PSS was nonmutagenic in vitro and possessed an acute oral toxicity of >5 g/kg (rat). Gel with 10% T-PSS did not irritate the skin or penile mucosa (rabbit) and caused no dermal sensitization (guinea pig). Vaginal administration of the 5% T-PSS gel to the rabbit for 14 consecutive days caused no systemic toxicity and only mild (acceptable) vaginal irritation. T-PSS in gel form is worthy of clinical evaluation as a vaginal contraceptive HIV/STD preventative.
Identification and Properties of Very High Affinity Brain Membrane-binding Sites for a Neurotoxic Phospholipase from the Taipan Venom (1989)

Four new monochain phospholipases were purified from the Oxyuranus scutellatus (taipan) venom. Three of them were highly toxic when injected into mice brain. One of these neurotoxic phospholipases, OS2, was iodinated and used in binding experiments to demonstrate the presence of two families of specific binding sites in rat brain synaptic membranes. The affinities were exceptionally high, Kd1 = 1.5 +/- 0.5 pM and Kd2 = 45 +/- 10 pM, and the maximal binding capacities were Bmax 1 = 1 +/- 0.4 and Bmax 2 = 3 +/- 0.5 pmol/mg of protein. Both binding sites were sensitive to proteolysis and demonstrated to be located on proteins of Mr 85,000-88,000 and 36,000-51,000 by cross-linking and photoaffinity labeling techniques. The binding of 125I-OS2 to synaptic membranes was dependent on Ca2+ ions and enhanced by Zn2+ ions which inhibit phospholipase activity. Competition experiments have shown that, except for beta-bungarotoxin, a number of known toxic snake or bee phospholipases have very high affinities for the newly identified binding sites. A good correlation (r = 0.80) was observed between toxicity and affinity but not between phospholipase activity and affinity.
Touchdown and Pull-In Voltage Behavior of a MEMS Device with Varying Dielectric Properties (2005)

The pull-in voltage instability associated with a simple MEMS device, consisting of a thin dielectric elastic membrane supported above a rigid conducting ground plate, is analyzed. The upper surface of the membrane is coated with a thin conducting film. In a certain asymptotic limit representing a thin device, the mathematical model consists of a nonlinear partial differential equation for the deflection of the thin dielectric membrane. When a voltage V is applied to the conducting film, the dielectric membrane deflects towards the bottom plate. For a slab, a circular cylindrical, and a square domain, numerical results are given for the saddle-node bifurcation value $V_{*}$, also referred to as the pull-in voltage, for which there is no steady-state membrane deflection for $V > V_{*}$. For $V > V_{*}$ it is shown numerically that the membrane dynamics are such that the thin dielectric membrane touches the lower plate in finite time. Results are given for both spatially uniform and nonuniform dielectric permittivity profiles in the thin dielectric membrane. By allowing for a spatially nonuniform permittivity profile, it is shown that the pull-in voltage instability can be delayed until larger values of V and that greater pull-in distances can be achieved. Analytical bounds are given for the pull-in voltage $V_{*}$ for two classes of spatially variable permittivity profiles. In particular, a rigorous analytical bound $V_1$, which depends on the class of permittivity profile, is derived that guarantees for the range $V > V_{1} > V_{*}$ that there is no steady-state solution for the membrane deflection and that finite-time touchdown occurs. Numerical results for touchdown behavior, both for $V > V_1$ and for $V_{*} < V < V_1$, together with an asymptotic construction of the touchdown profile, are given for both a spatially uniform and a spatially nonuniform permittivity profile.
Human CD34+ cell EST database: single-pass sequencing of 402 clones from a directional cDNA library. (1996)

A directional cDNA library was constructed from human CD34+ cells, and single-pass DNA sequence analysis was used to sequence 402 randomly picked cDNA clones. Sequence homology searches against the GenBank/EMBL databases revealed that 144 clones (35.8%) represented new genes, whereas 39 clones (9.7%) matched the partial sequences of cDNA clones (expressed sequence tags [ESTs]) from cDNA libraries from other tissues or cells. One hundred three (25.6%) of the clones were highly homologous or identical to genes of known function. 18.6% of the clones were ribosomal and 6 % were mitochondrial sequences. Seventeen (4.2%) of the clones were coding for Alu or L1 repetitive sequences. Our results suggest that random single-pass sequencing of cDNA clones provides a rapid way to obtain a profile of genes expressed in CD34+ cells and to identify new and potentially interesting genes.
The anthelmintic effects of flubendazole on Brugia pahangi (1979)

The anthelmintic effects of flubendazole (methyl [5-(4-fluorobenzoyl)-1-H-benzimidazol-2-yl] carbamate) (Janssen Pharmaceutica) were evaluated in jirds (Meriones unguiculatus) and cats (Felis cattus) infected with Brugia pahangi. Flubendazole was macrofilaricidal at 5 x 2.5 mg/kg and 1 x 25 mg/kg in jirds and 1 x 100 mg/kg in cats when administered by subcutaneous injection. It also killed developing larvae in jirds. It was not microfilaricidal.
Overexpression of BiP has Inhibitory Effects on the Accumulation of Seed Storage Proteins in Endosperm Cells of Rice (2009)

Seed storage proteins are specifically and highly synthesized during seed maturation and are deposited into protein bodies (PBs) via the endoplasmic reticulum (ER) lumen. The accumulation process is mediated by ER chaperones such as luminal binding protein (BiP) and protein disulfide isomerase (PDI). To examine the role of ER chaperones and the relationship between ER chaperones and levels of accumulation of seed storage proteins, we generated transgenic rice plants in which the rice BiP and PDI genes were overexpressed in an endosperm-specific manner under the control of the rice seed storage protein glutelin promoter. The seed phenotype of the PDI-overexpressing transformant was almost identical to that of the wild type, whereas overexpression of BiP resulted in transgenic rice seed that displayed an opaque phenotype with floury and shrunken features. In the BiP-overexpressing line, the levels of accumulation of seed storage proteins and starch contents were significantly lower compared with the wild type. Interestingly, overproduction of BiP in the endosperm of the transformant not only altered the morphological structure of ER-derived PB-I, but also generated unusual new PB-like structures composed of a high electron density matrix containing glutelin and BiP and a low electron density matrix containing prolamins. Notably, polysomes were attached around the aberrant PB-like structures, indicating that this aberrant structure is an ER-derived PB-I derivative. These results suggested that the PB-like structure may be formed in the ER lumen, resulting in inhibition of translation, folding and transport of seed proteins.
Nuevo desarrollo del derecho internacional — Prohibición o restricción de utilizar ciertas armas clásicas (1981)

La « Conferencia de las Naciones Unidas sobre Prohibiciones o Restricciones del Empleo de Ciertas Armas Convencionales que Puedan Considerarse Excesivamente Novicas o de Efectos Indiscriminados » terminó, el 10 de octubre de 1980, con la aprobación, por consenso, de los instrumentos siguientes: — Convención sobre Prohibiciones o Restricciones del Empleo de Ciertas Armas Convencionales, — Protocolo sobre Fragmentos no Localizables (Protocolo I), — Protocolo sobre Prohibiciones o Restricciones del Empleo de Minas, Armas Trampa y otros Artefactos (Protocolo II), — Protocolo sobre Prohibiciones o Restricciones del Empleo de Armas Incendiarias (Protocolo III). Además, ya en su primer período de sesiones, la Conferencia aprobó una Resolución sobre los sistemas de armas de pequeño calibre.
Rock physics model for seismic velocity & fluid substitution in sub‐resolution interbedded sand–shale sequences (2018)

ABSTRACT The measured geophysical response of sand – shale sequences is an average over multiple layers when the tool resolution (seismic or well log) is coarser than the scale of sand – shale mixing. Shale can be found within sand – shale sequences as laminations, dispersed in sand pores, as well as load bearing clasts. We present a rock physics framework to model seismic/sonic properties of sub‐resolution interbedded shaly sands using the so‐called solid and mineral substitution models. This modelling approach stays consistent with the conceptual model of the Thomas–Stieber approach for estimating volumetric properties of shaly sands; thus, this work connects established well log data‐based petrophysical workflows with quantitative interpretation of seismic data for modelling hydrocarbon signature in sand – shale sequences. We present applications of the new model to infer thickness of sand – shale lamination (i.e., net to gross) and other volumetric properties using seismic data. Another application of the new approach is fluid substitution in sub‐resolution interbedded sand–shale sequences that operate directly at the measurement scale without the need to downscale; such a procedure has many practical advantages over the approach of “first‐downscale‐and‐then‐upscale” as it is not very sensitive to errors in estimated sand fraction and end member sand/shale properties and remains stable at small sand/shale fractions.
Engineering microbial cell factories for the production of plant natural products: from design principles to industrial-scale production (2017)

Plant natural products (PNPs) are widely used as pharmaceuticals, nutraceuticals, seasonings, pigments, etc., with a huge commercial value on the global market. However, most of these PNPs are still being extracted from plants. A resource-conserving and environment-friendly synthesis route for PNPs that utilizes microbial cell factories has attracted increasing attention since the 1940s. However, at the present only a handful of PNPs are being produced by microbial cell factories at an industrial scale, and there are still many challenges in their large-scale application. One of the challenges is that most biosynthetic pathways of PNPs are still unknown, which largely limits the number of candidate PNPs for heterologous microbial production. Another challenge is that the metabolic fluxes toward the target products in microbial hosts are often hindered by poor precursor supply, low catalytic activity of enzymes and obstructed product transport. Consequently, despite intensive studies on the metabolic engineering of microbial hosts, the fermentation costs of most heterologously produced PNPs are still too high for industrial-scale production. In this paper, we review several aspects of PNP production in microbial cell factories, including important design principles and recent progress in pathway mining and metabolic engineering. In addition, implemented cases of industrial-scale production of PNPs in microbial cell factories are also highlighted.
Long duration strapdown stellar-inertial navigation using satellite tracking (2003)

A strapdown stellar-inertial navigation system (INS) is currently being developed which can be used to correct for the gyro drift in an INS throughout a long-duration mission. The star sensor provides updates of the inertial angle error derived from stellar observations. However, since the star sensor updates are unable to correct for INS drifts due to accelerometer errors, the stellar inertial navigation solution accuracy degrades with time. A study has been performed on the number of visible satellites that can be tracked by the stellar-inertial system. The authors discuss the results of this study and include simulation results showing the performance improvement possible using both star and satellite observations to bound the system error growth. The results have shown that the combination of measurements can maintain the system error growth to within 700 ft over a long-duration mission.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
1-(1-Indanyl)- and 1-(1-Tetralyl)imidazole-5-carboxylate Esters, a Novel Type of Antifungal Agents (1967)

1-(1-Indanyl)imidazole-5-carboxylates (I) and 1-(1-tetralyl)imidazole-5-carboxylates (II) are synthesized and evaluated for antifungal activity. The N-(1-indanyl)- or N-(1-tetralyl)-N-formylglycine ester, OCHNRCH2CO2R1 (III, R = 1-indanyl, R1 = Me) (IV, R = 1-tetralyl, R1 = Et), undergoes Claisen formylation to the enolate, the enolate treated with HCl-HNCS, and the resulting N-(1-indanyl)- or N-(1-tetralyl)-2-mercaptoimidazole (V and VI, resp.) desulfurized and converted to the desired III via the acid and acid chloride. I and II exhibit excellent fungistatic activity against several organisms, including Microsporum canis, Trichophyton mentagrophytes, and T. rubrum. The optimum effect is achieved when R = Et or Pr, lengthening of the chain results in diminished activity, the introduction of bulky groups causes greatly diminished inhibition, and carboxylic acids are totally inactive.
Demonstration of an early and a late phase of ischemic preconditioning in mice (1998)

It is unknown whether ischemic preconditioning (PC; either early or late) occurs in the mouse. The goal of this study was to answer this question and to develop a reliable and physiologically relevant murine model of both early and late ischemic PC. A total of 201 mice were used. In nonpreconditioned open-chest animals subjected to 30 min of coronary occlusion followed by 24 h of reperfusion, infarct size (tetrazolium staining) averaged 52% of the region at risk. When the 30-min occlusion was performed 10 min after a PC protocol consisting of six cycles of 4-min occlusion and 4-min reperfusion, infarct size was reduced by 75%, indicating an early PC effect. When the 30-min occlusion was performed 24 h after the same PC protocol, infarct size was reduced by 48%, indicating a late PC effect. In mice in which the 30-min occlusion was followed by 4 h of reperfusion, infarct size was similar to that observed after 24 h of reperfusion, indicating that a 4-h reperfusion interval is sufficient to detect the final extent of cell death in this model. Fundamental physiological variables (body temperature, arterial oxygenation, acid-base balance, heart rate, and arterial pressure) were measured and found to be within normal limits. Taken together, these results demonstrate that, in the mouse, a robust infarct-sparing effect occurs during both the early and the late phases of ischemic PC, although the early phase is more powerful. This murine model is physiologically relevant, provides reliable measurements, and should be useful for elucidating the cellular mechanisms of ischemic PC in genetically engineered animals.
<title>Real Time Digital Correction Of Acquisition Errors Applied To Solid State Scanners</title> (1977)

Capturing an image using a solid state scanner requires focusing the subject image on to the scanner array with some type of lens. Various kinds of degradations occur including Cos4 law, illumination non-uniformity, dust on the optical surfaces and flaws in the imaging array. The combined effects of all sources of image acquisition errors can result in serious cosmetic defects in the resulting image. Dramatic improvements in image quality can be achieved by multiplying the intensity value of each image pel by a correction factor: () Pout = Pin Pmax CFi Pout = corrected pel value Pin = pel value as captured Pmax = maximum possible pel intensity value CFi = correction factor for the ith position on the scan line The correction factors (CFi) are determined by capturing an image of a "standard white material" and calculating the average white value for each position on the scan line. The correction calculation requires multiply and divide operations which are too complicated to be performed at real time (21 million pels/second) in computer software. Therefore a 2-stage tabular lookup procedure has been implemented in bipolar RAM and PROM hardware. An additional feature of the approach is the possibility of performing any arbitrary intensity transformation by the substitution of a different PROM table.
Telechelic Poly(ethylene glycol)−POSS Amphiphiles at the Air/Water Interface (2007)

Combining two non-surface-active building blocks, oligomeric poly(ethylene glycol) (PEG) and a completely hydrophobic polyhedral oligomeric silsesquioxane (POSS) cage, creates amphiphilic telechelic polymers (POSS−PEG−POSS), which exhibit surface activity at the air/water (A/W) interface. POSS moieties serve as the hydrophobic groups for hydrophilic PEG chains of different number-average molar mass (1, 2, 3.4, 8, and 10 kg mol-1). For short PEG chains (1, 2, and 3.4 kg mol-1), insoluble monolayers form, whereas POSS end groups were not sufficiently hydrophobic to keep higher molar mass hydrophilic PEG blocks (8 and 10 kg mol-1) at the A/W interface. Thermodynamic analyses of the 1, 2, and 3.4 kg mol-1 POSS−PEG−POSS via surface pressure−area per monomer isotherms indicate that the POSS end groups reside at the A/W interface and that the PEG chains are squeezed into the subphase with increasing surface pressure. This conclusion is supported by X-ray reflectivity studies on Y-type Langmuir−Blodgett multilayer films which reveal a double-layer structure with a double-layer spacing of about 3.52 nm. These findings provide a strategy for producing new surface active species from non-surface-active precursors.
A constraint-length based modified Viterbi algorithm with adaptive effort (1999)

A modified Viterbi (1971) algorithm for convolutional codes is described that provides for signal-to-noise ratio (SNR) adaptive computational effort. The algorithm has three levels of prioritized effort. Movement from one level to the next is controlled by parameters that can be selected according to desired output bit error rate performance. For 3-bit soft decision detected signals, a coding gain within 0.06 dB of Viterbi at a 3-dB SNR is achieved for the same constraint-length code with modest parameter values and computational effort. At values of SNR above 6 dB, the algorithm decodes with very low computational effort. Effort levels are controlled by spanning the decoding trellis in steps that are one constraint-length long.
A Eubacterial Gene Conferring Spectinomycin Resistance on <i>Chlamydomonas reinhardtii</i>: Integration Into the Nuclear Genome and Gene Expression (1997)

We have constructed a dominant selectable marker for nuclear transformation of C. reinhardtii, composed of the coding sequence of the eubacterial aadA gene (conferring spectinomycin resistance) fused to the 5' and 3' untranslated regions of the endogenous RbcS2 gene. Spectinomycin-resistant transformants isolated by direct selection (1) contain the chimeric gene(s) stably integrated into the nuclear genome, (2) show cosegregation of the resistance phenotype with the introduced DNA, and (3) synthesize the expected mRNA and protein. Small linearized plasmids appeared to be inserted into the nuclear genome preferentially through their ends, with relatively few large deletions and/or rearrangements. Multiple copy transformants often integrated concatemers of transforming DNA. Our detailed analysis of the complex integration patterns of plasmid DNA in C. reinhardtii nuclear transformants should be useful for improving the technique of insertional mutagenesis. We also found that the spectinomycin-resistance phenotype was unstable in about half of the transformants. When maintained under nonselective conditions, neither the aadA mRNA nor the AadA protein were detected in these subclones. Moreover, since the integrated transforming DNA was not altered or lost expression of the RbcS2::aadA::RbcS2 gene(s) appears to be repressed. Measurements of transcriptional activity, mRNA accumulation, and mRNA stability suggest that expression of this chimeric gene(s) may also be affected by rapid RNA degradation, presumably due to defects in mRNA processing and, or nuclear export. Thus, both gene silencing and transcript instability, rather than biased codon usage, may explain the difficulties encountered in the expression of foreign genes in the nuclear genome of Chlamydomonas.