Search results for "substrat"
showing 10 items of 1042 documents
Quantitative analysis of the effect of controlled-release formulation on nonlinear gastrointestinal absorption of P-glycoprotein substrate talinolol …
2020
Abstract Oral absorption of talinolol, a substrate of P-glycoprotein (P-gp), from a sustained-release (SR) formulation was reportedly decreased compared to that from an immediate-release (IR) formulation. The aim of this study was to predict and understand the effect of controlled-release formulation on the oral absorption of P-gp substrates by developing a physiologically based pharmacokinetic (PBPK) absorption model incorporating multiple kinetic parameters obtained from in vitro studies, using talinolol as a model substrate. Simulation analysis using the developed PBPK absorption model indicated that the clinically observed marked decrease in the plasma concentration of talinolol adminis…
Fabrication and characterization of vacuum deposited fluorescein thin films
2011
Simple vacuum evaporation technique for deposition of dyes on various solid surfaces has been developed. The method is compatible with conventional solvent-free nanofabrication processing enabling fabrication of nanoscale optoelectronic devices. Thin films of fluorescein were deposited on glass, fluorine-tin-oxide (FTO) coated glass with and without atomically layer deposited (ALD) nanocrystalline 20 nm thick anatase TiO2 coating. Surface topology, absorption and emission spectra of the films depends on their thickness and the material of supporting substrate. On a smooth glass surface the dye initially formes islands before merging into a uniform layer after 5 to 10 monolayers. On FTO cove…
A quantum mechanics/molecular mechanics study of the acylation reaction of TEM1 β-lactamase and penicillanate
2000
The acylation step in β-lactamase catalyzed hydrolysis of β-lactams has been explored by means of a quantum mechanics/molecular mechanics approach (AM1/CHARMM). The TEM1 enzyme, a class A β-lactamase, and the penicillanate constitute the system employed in our study. The entire molecular system is divided into a quantum and a classical region: the quantum part is composed by the substrate, the serine Ser70 and the essential moieties of key active site residues, Lys73, Ser130 and Glu166, as well as a water molecule present in the active site region, while the classical part is formed by the remaining residues and structural waters of the enzyme. In particular, the sequence of steps proposed …
Numerical simulations demonstrate that the double tapering of the spatualae of lizards and insects maximize both detachment resistance and stability
2011
Many biological attachment devices of insects, spiders and geckos consist of arrays of hairs (setae), which are terminated by contact elements of different shapes. However, the most frequently observed shape is a thin plate-like spatula. In spite of a rather wide range of sizes, most spatulae of different animals are not uniform, but rather possess a gradient in thickness and width. Here we show that the spatulae of insects and geckos become gradually thinner and wider approaching the end. This geometrical effect is explained in the present paper, by using a numerical approach for the modelling of the van der Waals adhesion and friction between the contact elements and the substrate. The ap…
Human liver cytosolic epoxide hydrolases.
1988
Human liver epoxide hydrolases were characterized by several criteria and a cytosolic cis-stilbene oxide hydrolase (cEHcso) was purified to apparent homogeneity. Styrene oxide and five phenylmethyloxiranes were tested as substrates for human liver epoxide hydrolases. With microsomes activity was highest with trans-2-methylstyrene oxide, followed by styrene 7, 8-oxide, cis-2-With methylstyrene oxide, cis-1,2-dimethylstyrene oxide, trans-1, 2-dimethylstyrene oxide and 2, 2-dimethylstyrene oxide. With cytosol the same order was obtained for the first three substrates, whereas activity with 2, 2-dimethylstyrene oxide was higher than with cis-1,2-dimethylstyrene oxide and no hydrolysis occurred …
AISF update on the diagnosis and management of adult-onset lysosomal storage diseases with hepatic involvement.
2020
Lysosomal storage diseases (LSDs) are a heterogeneous group of inherited disorders caused by loss-of-function mutations in genes encoding for lysosomal enzymes/proteins. The consequence is a progressive accumulation of substrates in these intracellular organelles, resulting in cellular and tissue damage. The overall incidence is about 1/8000 live births, but is likely underestimated. LSDs are chronic progressive multi-systemic disorders, generally presenting with visceromegaly, and involvement of the central nervous system, eyes, the skeleton, and the respiratory and cardiovascular systems. The age at onset and phenotypic expression are highly variable, according to the specific enzymatic d…
Neural substrates of the interaction of emotional stimulus processing and motor inhibitory control: an emotional linguistic go/no-go fMRI study.
2007
Neural substrates of behavioral inhibitory control have been probed in a variety of animal model, physiologic, behavioral, and imaging studies, many emphasizing the role of prefrontal circuits. Likewise, the neurocircuitry of emotion has been investigated from a variety of perspectives. Recently, neural mechanisms mediating the interaction of emotion and behavioral regulation have become the focus of intense study. To further define neurocircuitry specifically underlying the interaction between emotional processing and response inhibition, we developed an emotional linguistic go/no-go fMRI paradigm with a factorial block design which joins explicit inhibitory task demand (i.e., go or no-go)…
Effects of gender on resting leg blood flow: implications for measurement of regional substrate oxidation.
1998
Jensen, Michael D., Tu T. Nguyen, A. Hernández Mijares, C. Michael Johnson, and Michael J. Murray. Effects of gender on resting leg blood flow: implications for measurement of regional substrate oxidation. J. Appl. Physiol. 84(1): 141–145, 1998.—These studies were designed to examine whether the respiratory quotient (RQ) of leg tissue (primarily skeletal muscle) would increase to a greater degree in women than in men during meal ingestion. We found that mean leg and systemic RQ values were similar in men under both basal and fed conditions, whereas the agreement was poor in women. In women, leg RQ values tended to be greater than the systemic RQ, whereas splanchnic RQ values tended to be l…
Neural dynamics of learning sound-action associations.
2008
A motor component is pre-requisite to any communicative act as one must inherently move to communicate. To learn to make a communicative act, the brain must be able to dynamically associate arbitrary percepts to the neural substrate underlying the pre-requisite motor activity. We aimed to investigate whether brain regions involved in complex gestures (ventral pre-motor cortex, Brodmann Area 44) were involved in mediating association between novel abstract auditory stimuli and novel gestural movements. In a functional resonance imaging (fMRI) study we asked participants to learn associations between previously unrelated novel sounds and meaningless gestures inside the scanner. We use functio…
Resting metabolic rate and postabsorptive substrate oxidation in morbidly obese subjects before and after massive weight loss
1996
OBJECTIVE: To investigate the changes of resting metabolic rate (RMR) and postabsorptive oxidation of carbohydrates (CHO), lipids (LIP) and proteins (PT) in morbidly obese subjects after long-term stable massive weight reduction. DESIGN: Longitudinal, intervention study of a bilio-pancreatic by-pass. SUBJECTS: Ten (Four men, six women) obese subjects (BMI: 53.7 ± 2.1 kg/m2, men, nine women) control subjects (BMI: 21.4 ± 1.0 kg/m2). MEASUREMENTS: RMR and substrates oxidation (indirect calorimetry), body composition (bioelectrical impedance), plasma concentrations of glucose, FFA, insulin and thyroid hormones before (T0, prior to surgery), during (T1: 1-3 months, and T2: 9-16 months following…