gebhart/patrepeval huggingface dataset:
Comparison of Species Differences of P-Glycoproteins in Beagle Dog, Rhesus Monkey, and Human Using ATPase Activity Assays (2005)

P-glycoprotein (P-gp) is a transmembrane efflux transporter which possesses many important functions in drug absorption, disposition, metabolism, and toxicity. The ultimate goal of investigating drug interactions between P-gp and drug molecules in early drug discovery is to understand the contribution of P-gp to the pharmacokinetic and pharmacodynamic properties of drug candidates and to project drug-drug interaction (DDI) potentials in humans. Understanding species differences in P-gp activities further helps the prediction of P-gp-mediated drug disposition and DDI in humans from preclinical pharmacokinetics data. The objective of the present study is to investigate the species difference in P-gp activities, via P-gp ATPase assays, using rhesus monkey Mdr1, beagle dog Mdr1, and human MDR1 expressed insect cell membranes. Twenty-one compounds with diverse chemical structures and different P-gp binding sites were chosen for the ATPase assays. P-gp ATPase binding affinities (alphaKa) and fold increases in P-gp ATPase activities (beta) of P-gp substrates were determined. Consistent with the gene and amino acid similarity, the binding affinities of test compounds to rhesus monkey P-gp were much closer to those of human P-gp than beagle dog P-gp. This is the first study which investigates the ligand affinities of P-gp from three different species. The result of this study provides an example of how to use membrane P-gp ATPase assays to evaluate interspecies P-gp differences.
Palladium-Catalyzed Ullmann Cross-Coupling of β-Iodoenones and β-Iodoacrylates with o-Halonitroarenes or o-Iodobenzonitriles and Reductive Cyclization of the Resulting Products To Give Diverse Heterocyclic Systems (2018)

The palladium-catalyzed Ullmann cross-coupling of β-iodoenones and β-iodoacrylates such as 5 (X = I) with o-halonitroarenes and o-iodobenzonitriles including 2 affords products such as compound 7. These can be engaged in a range of reductive cyclization reactions leading to heterocyclic frameworks such as 3,4-benzomorphan derivative 43.
Investigation of ultrasound phase shifts caused by the skull bone using low-frequency reflection data (2002)

A potential noninvasive means for obtaining the value of phase shifts caused by the skull is examined. Knowledge of these shifts could be used to restore the focus from an ultrasound array after transcranial propagation. A pulsed signal is emitted from a single element of a therapeutic ultrasound transducer. After reflecting off the skull, the steady-state amplitude of the response is recorded. The data are examined over the bandwidth of the transducer, between 0.6 MHz and 1.7 MHz, producing amplitude data as a function of frequency. This measurement methodology is similar to that previously used by Hakim, et. al. [1997 Proc. IEEE Ultrason. Symp. p1153]. After deconvolution of the transducer's frequency response, a periodic appearance of local maxima and minima is observed in the data as a function of frequency. We hypothesize the amplitude is primarily determined by the superposition of reflections between the interfaces at the inner and outer surfaces of the skull and between the interior interfaces of trabecular and cortical bone. A homogeneous layer model is used to predict the forward-propagated phase using the reflection data. Good correlation is found between the numeric calculation and phases measured after propagation through a three-layer plastic phantom. The method is next tested on three excised human skulls using CT images of the skulls to provide the thickness of the bone layers. The procedure could eventually be applied toward phasing multi-element arrays. Such an application could have implications in both therapeutic and diagnostic brain procedures.
Growth Characteristics and Nitrification Rate of Nitrifying Bacteria Entrapped in Pellets. (2000)

To estimate a biological succession of nitrifying bacteria entrapped in PEG gel, growth rate, death rate and nitrifying rate of nitrifying bacteria were investigated under a various phase condition. The immobilized nitrifying bacteria were acclimated for 2 weeks with supply of inorganic synthetic wastewater containing NH4-N of 20mg/l. Specific growth rate of nitrifying bacteria was 0.73 d-1 and nitrifying bacteria increased to 109 MPN/ml-pellet under acclimation term. After acclimation wastewater with NH4-N 20-100mg/l was continuously treated at a loading rate of 0.16-0.80kg-N/m3/d. The NH4-N concentration of the effluent could be reduced to 2mg/l or less and removal ratio was 90%. Number of nitrifying bacteria was oscillated between 107-109MPN/ml-pellet under steady state loading condition. Nitrification rate was increasing with increase in number of nitrifying bacteria. Nitrifying bacteria was decreasing during no loading condition. The specific death rate was 0.14-0.15d-1 and half life time was 4-5d.
Investigating the Role of VDR and Megalin in Semi-Selectivity of Side-Chain Modified 19-nor Analogs of Vitamin D (2019)

1,25-dihydroxyvitamin D<sub>3</sub> (1,25D3) is implicated in many cellular functions, including cell proliferation and differentiation, thus exerting potential antitumor effects. A major limitation for therapeutic use of 1,25D3 are potent calcemic activities. Therefore, synthetic analogs of 1,25D3 for use in anticancer therapy should retain cell differentiating potential, with calcemic activity being reduced. To obtain this goal, the analogs should effectively activate transcription of genes responsible for cell differentiation, leaving the genes responsible for calcium homeostasis less active. In order to better understand this phenomenon, we selected a series of structurally related 19-<i>nor</i> analogs of 1,25D (PRI-5100, PRI-5101, PRI-5105, and PRI-5106) and tested their activities in blood cells and in cells connected to calcium homeostasis. Affinities of analogs to recombinant vitamin D receptor (VDR) protein were not correlated to their pro-differentiating activities. Moreover, the pattern of transcriptional activities of the analogs was different in cell lines originating from various vitamin D-responsive tissues. We thus hypothesized that receptors which participate in transport of the analogs to the cells might contribute to the observed differences. In order to study this hypothesis, we produced renal cells with knock-out of the megalin gene. Our results indicate that megalin has a minor effect on semi-selective activities of vitamin D analogs.
Use of a Plackett−Burman Design with Multivariate Calibration for the Analysis of Polycyclic Aromatic Hydrocarbons in Micellar Media by Synchronous Fluorescence (2001)

This work describes the use of a multilevel Plackett-Burman design (PB) for the creation of a calibration set for partial least square regression (PLS). The PB calibration set was compared to a collinear analogue by testing these two PLS models for the analysis of six polycyclic aromatic hydrocarbons (PAHs). These compounds were analyzed in micellar media by synchronous fluorescence after determination of the experimental conditions (choice of surfactant, analytical conditions such as deltalambda, step, and scan range). The external validation shows that the collinear set is inappropriate to quantify PAH in real samples, but the PB calibration set affords optimal results.
Selection and Characterization of PCB-Binding DNA Aptamers (2011)

Polychlorinated biphenyls (PCBs) are persistent organic pollutants (POPs) that resist natural degradation and bioaccumulate in nature. Combined with their toxicity, this leads them to cause cancer and other health hazards. Thus, there is a vital need for rapid and sensitive methods to detect PCB residues in food and in the environment. In this study, PCB-binding DNA aptamers were developed using PCB72 and PCB106 as targets for aptamer selection. Aptamers are synthetic DNA recognition elements which form unique conformations that enable them to bind specifically to their targets. Using in vitro selection techniques and fluorometry, an aptamer that binds with nanomolar affinity to both the PCBs has been developed. It displayed high selectivity to the original target congeners and limited affinity toward other PCB congeners (105, 118, 153, and 169), suggesting general specificity for the basic PCB skeleton with varying affinities for different congeners. This aptamer provides a basis for constructing an affordable, sensitive, and high-throughput assay for the detection of PCBs in food and environmental samples and offers a promising alternative to existing methods of PCB quantitation. This study therefore advances aptamer technology by targeting one of the highly sought-after POPs, for the first time ever recorded.
10 Gb/s, 120 km normal fiber transmission experiment using a 1.56 µm Multiple Quantum Well InP/InGaAsP Mach-Zehnder modulator (1993)

Mach-Zehnder (MZ) intensity modulators are well suited to transmission applications in multigigabit, long distance optical fiber systems because of the ability to control the frequency chirp in these devices [1]. To date, system results have only been reported for LiNb03 MZ modulators. Although DI-V semiconductor MZ modulators have been fabricated by other groups [2,3], we report here the first system experiment performed with such a device. The III-V semiconductor device is compact (.25 mm X1.5 mm), has low drive power requirements and is potentially integrable with a laser [4]. 10 Gb/s NRZ transmission is demonstrated over 120 km of normal fiber with a push-pull drive of only 2 V peak-peak/side and a dispersion penalty of 4.8 dB. No dispersion penalty is obtained for fiber lengths up to 80 km.
Supplementary Figure S4 from Mixed Response to Cancer Immunotherapy is Driven by Intratumor Heterogeneity and Differential Interlesion Immune Infiltration (2023)

&lt;p&gt;Additional in vitro data using the MC-38 clones.&lt;/p&gt;
LiCl‐vermittelte Synthese funktionalisierter benzylischer Indium(III)‐halogenide und hoch chemoselektive Palladium‐katalysierte Kreuzkupplung mit einem protischen Cosolvens (2009)

Abstract Empfindliche Funktionen wie COR, CHO oder CH 2 OH können in benzylischen Indiumreagentien vorhanden sein, die über direkte Indiuminsertion mithilfe von LiCl hergestellt wurden. Diese Reagentien lassen sich in Gegenwart eines protischen Cosolvens in Pd‐katalysierten Kreuzkupplungen nach Aktivierung mit i PrMgCl⋅LiCl umsetzen (siehe Schema). Die Umsetzung mit Elektrophilen mit NH‐ oder OH‐Gruppen ergibt bemerkenswerte Chemoselektivitäten. magnified image
Frostbite: Pathogenesis and Treatment (2000)

Frostbite, once almost exclusively a military problem, is becoming more prevalent among the general population and should now be considered to be within the scope of the civilian physician's practice. Studies into the epidemiology of civilian frostbite have identified several risk factors that may aid the clinician in the diagnosis and management of cold injuries. Research into the pathophysiology has revealed marked similarities in inflammatory processes to those seen in thermal burns and ischemia/reperfusion injury. Evidence of the role of thromboxanes and prostaglandins has resulted in more active approaches to the medical treatment of frostbite wounds. Although the surgical management of frostbite involves delayed debridement 1 to 3 months after demarcation, recent improvements in radiologic assessment of tissue viability have led to the possibility of earlier surgical intervention. In addition, several adjunctive therapies, including vasodilators, thrombolysis, hyperbaric oxygen, and sympathectomy, are discussed.
THz generation in plasmas using multiple color laser pulses (2009)

Experiments have demonstrated the generation of THz radiation when an intense, short laser pulse is mixed with its frequency-doubled counterpart in a gas. A number of mechanisms have been proposed to account for the observed THz radiation. Our analysis indicates that under the proper conditions the nonlinear coupling of the two short pulse lasers, one at frequency omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> and the other at 2omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> , in plasma can lead to the generation of THz radiation. The nonlinear coupling of the fundamental E <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sub> (omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> ) and the frequency-doubled E <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> (2omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> ) laser pulses is shown to lead to a third order susceptibility which has a time dependence characteristic of the laser pulse durations. Since the laser pulse duration is typically in the pico-second or sub-picosecond regime the resulting radiation is in the THz or multi-THz regime. The appropriate third order susceptibility is chi <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">(3)</sup> (omega= 0; omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> ,omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> ,2omega <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">0</sub> ) and is proportional to(E <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sub> ) <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> E <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> . To obtain the third order susceptibility we solve the plasma fluid equations correct to third order in the laser fields, including both the relativistic and ponderomotive force terms. The relativistic and ponderomotive contributions to the susceptibility exactly cancel in the absence of electron collisions. Therefore, in this THz generation mechanism collisional effects play a critical role. In addition, THz generation depends on the relative polarizations of the lasers. We discuss the experimental observations and compare the results with our theoretical and numerical predictions.
On the equivalence of the Berlekamp-Massey and the Euclidean algorithms for decoding (2000)

The Berlekamp-Massey (1968, 1969) algorithm (BMA) and the Euclidean algorithm (EA) for decoding have been considered as two different algorithms for solving the same problem, namely, the one given by the key equation. We argue that they are essentially identical by showing how one can be adapted to perform the same arithmetic as the other. As a tool we use Feng and Tzeng's (1991) fundamental iterative algorithm that when adapted to the syndrome matrix is regarded as equivalent to the BMA.
Punjab right to services act 2011: An analytical study of role of saanjh kendras (2019)

Public Administration means to provide the services to the people without any prejudice. With the coming of the Right to Services Act, it has become obligatory on the part of public agencies not only to provide the services to the people but also to ensure that provision of the services is time bound. Under the name of Saanjh, the Government of Punjab launched a community policing project to bridge the gap between the Police and the People. The main aim these Kendras were to resolve the disputes between the Police and Public and also to provide basic police services through a single window system. These Saanjh Kendras became fully operational since 2011. The present paper is an attempt to analyse the role of Saanjh Kendras in the State of Punjab.
Supersymmetric analysis of stochastic micro-bending in optical waveguides (2021)

Micro-bending attenuation in an optical waveguide can be modeled by a Fokker-Planck equation. It is shown that a supersymmetric transformation applied to the Fokker-Planck equation is equivalent to a change in the refractive index profile, resulting in a larger or smaller attenuation. For a broad class of monomial index profiles, it is always possible to obtain an index profile with a larger micro-bending attenuation using a supersymmetric transformation. However, obtaining a smaller attenuation is not always possible and is restricted to a subset of index profiles.
Immunological activity of lipopolysaccharide of Helicobacter pylori on human peripheral mononuclear blood cells in comparison to lipopolysaccharides of other intestinal bacteria (1993)

Lipopolysaccharide of Helicobacter pylori was tested for its mitogenicity and for its ability to stimulate cytokine release in human peripheral blood mononuclear cells (PBMC) of healthy and H. pylori-infected blood donors. Mitogenicity in PBMC induced by H. pylori LPS was similar to that induced by Campylobacter jejuni lipopolysaccharide, but lower than that induced by Escherichia coli lipopolysaccharide in the H. pylori negative blood donor group. Furthermore, H. pylori LPS was able to induce tumour necrosis factor (TNF) interleukin 1 (IL-1) and interleukin 6 (IL-6) secretion of PBMC. Compared with the ability of C. jejuni and E. coli lipopolysaccharides to stimulate cytokine release, H. pylori lipopolysaccharide induced a significantly lower TNF and IL-1 secretion of PBMC than the other tested bacterial lipopolysaccharides. Similar amounts of IL-6 release were obtained by stimulation of PBMC with H. pylori and C. jejuni lipopolysaccharides, whereas a higher IL-6 release was measured by stimulation with E. coli lipopolysaccharide. The results of this study suggest that H. pylori lipopolysaccharide has a lower immunological activity than lipopolysaccharides of other intestinal bacteria. This is probably due to its unusual acylation and phosphorylation pattern of lipid A.
Convenient Synthesis of Furo[3,2-b]quinolin-4(1H)-ones (2020)

In this work, we report the simple synthesis of furo[3,2-b]quinolin-4(1H)-ones from readily available 4-ethynyl-[1,3]dioxolo[4,5-c]quinolone as the key starting material. After Sonogashira (hetero)arylation, formation of the furoquinoline scaffold was accomplished using methanesulfonic acid and metal-free conditions. Although the cyclization was affected by the substitution of reaction intermediates, the method allowed the preparation of derivatives varying at the C3-position.
Combination of a silane coupling agent and resin primer reinforces bonding effectiveness to a CAD/CAM indirect resin composite block (2021)

The effects of silanization and resin primer application on CAD/CAM indirect resin composite block bonding were investigated. KATANA AVENCIA P blocks (Kuraray Noritake Dental) were treated with a silane coupling agent and/or a resin primer. The contact angles (CAs) of resin primer were observed before and after silanization. Panavia V5 (Kuraray Noritake Dental) was built after each treatment. Bond strengths were measured, and the interface was analyzed by energy dispersive X-ray spectroscopy (EDS). The CA showed that silane treatment improved the wettability of the resin primer to the resin block. The combination treatment of the silane and resin primer showed significantly higher bond strength than no treatment, only in the silanization or resin primer group (p<0.001 each). EDS analysis showed that the resin primer penetrated both cement and block sides. The combination of the silane and resin primer improved bonding effectiveness between the resin block and resin cement.
A case control study of age related macular degeneration and use of statins (2005)

In the short and medium term statin use is not associated with a decreased risk of AMD. Whether subgroups of patients with specific forms of AMD (particularly choroidal neovascularisation) benefit from statin therapy remains a possibility.
Mechanisms of Polymyxin B Endotoxin Removal from Extracorporeal Blood Flow: Hydrodynamics of Sorption (2010)

The removal of blood endotoxins with the Toraymyxin extracorporeal sorption device exploits the capability of immobilized polymyxin B (PMB) to bind endotoxins stably with a high specificity. Although adsorption is a molecular-scale mechanism, it involves hydrodynamic phenomena in the whole range from the macroscopic down to the supramolecular scales. In this paper we summarize our experience with a computational, multiscale investigation of this device's hydrodynamic functionality. 3D computational fluid dynamics models were developed for the upper-scale studies. The flow behavior in the sorbent material was either modeled as a homogeneous Darcy's flow (macroscale study), or described as the flow through realistic geometrical models of its knitted fibers (mesoscale study). In the microscale study, simplified 2D models were used to track the motion of modeled endotoxin particles subjected to the competition of flow drag and molecular attraction by the fiber-grafted PMB. The results at each scale level supplied worst-case input data for the subsequent study. The macroscale results supplied the peak velocity of the flow field that develops in the sorbent. This was used in the mesoscale analysis, yielding a realistic range for the shear stresses in the fluid next to the fiber surface. With wall shear stresses in this range, endotoxin particle tracking was studied both in the vicinity of a single immobilized PMB molecule, and in the presence of a layer of PMB molecules evenly distributed at the fiber surface. Results showed that the capability to seize endotoxin molecules extends at least at a distance of 10-20 nm from the surface, which is one order of magnitude greater than the stable intermolecular bond characteristic distance. We conclude that a multiscale approach has the power to provide a comprehensive understanding, shedding light both upon the physics involved at each scale level and the mutual interactions of phenomena occurring at different scales.
Pilocarpine hydrochloride liposomes: characterization in vitro and preliminary evaluation in vivo in rabbit eye (1984)

Liposomes containing either pilocarpine hydrochloride or pilocarpine free base were prepared by the sonication method. This manufacturing process yielded after removal of non-encapsulated solute, small multilamellar vesicles (MLV) as was confirmed by electron microscopy examinations. For an identical liposomal composition, the encapsulation capacity and the drug content of the liposomes were drastically higher for pilocarpine hydrochloride than for pilocarpine free base. Investigation of the preparative parameters revealed that increasing the initial amount of drug decreased the drug content and the encapsulation efficiency of the liposomes formed. Since fixed amounts of lipids were used, the volume sequestration rate decrease was attributed to a moderate viscosity increase of the dispersion medium. Increase of phospholipid concentration at a constant ratio of cholesterol and dicetylphosphate to phosphatidylcholine reduced the aqueous volume entrapped per mg of lipid and subsequently the pilocarpine content in the liposomes. Negatively charged liposomes gave larger rates of pilocarpine hydrochloride and aqueous volume encapsulation than neutral liposomes but, on the contrary, positively charged liposomes gave the lowest rates of pilocarpine hydrochloride and aqueous volume encapsulation. Thus, for drug carrying the same net charge as the phospholipids an increase in the surface charge density of the liposome was not only ineffective, but actually resulted in a lower drug encapsulation due to electrostatic repulsion. Preliminary in vivo results on rabbit eyes suggested that the liposomal vehicle was probably unable to improve sufficiently the corneal penetration of pilocarpine to reach satisfactory therapeutic levels when administered at lower concentrations than commonly used.