Search results for "Tropa"
showing 10 items of 170 documents
Discovery and SAR Evolution of Pyrazole Azabicyclo[3.2.1]octane Sulfonamides as a Novel Class of Non-Covalent N-Acylethanolamine-Hydrolyzing Acid Ami…
2021
Inhibition of intracellular N-acylethanolamine-hydrolyzing acid amidase (NAAA) activity is a promising approach to manage the inflammatory response under disabling conditions. In fact, NAAA inhibition preserves endogenous palmitoylethanolamide (PEA) from degradation, thus increasing and prolonging its anti-inflammatory and analgesic efficacy at the inflamed site. In the present work, we report the identification of a potent, systemically available, novel class of NAAA inhibitors, featuring a pyrazole azabicyclo[3.2.1]octane structural core. After an initial screening campaign, a careful structure–activity relationship study led to the discovery of endo-ethoxymethyl-pyrazinyloxy-8-azabicyclo…
Activation of propane 2-nitronate to a genotoxicant in V79-derived cell lines engineered for the expression of rat hepatic sulfotransferases
1999
2-Nitropropane (2-NP) is a genotoxic hepatocarcinogen in rats. The genotoxicity of the compound has been attributed to a sulfotransferase-mediated formation of DNA-reactive species from the anionic form of 2-NP, propane 2-nitronate (P2N). Several observations have suggested that sulfotransferases (SULTs) 1A1 and/or 1C1 may be important in the activation of P2N to a genotoxicant in rat liver, but a definite proof is lacking. In order to identify the sulfotransferase(s) of rat liver that are capable of activating P2N, we have investigated the genotoxicity of P2N in various V79-derived cell lines engineered for expression of individual forms of rat hepatic sulfotransferases. Genotoxicity was a…
Dietary lycopene decreases the initiation of liver preneoplastic foci by diethylnitrosamine in the rat
1997
To test whether carotenoids can modulate the initiation of liver preneoplasia by diethylnitrosamine (DEN) or by 2-nitropropane (2-NP) in a sequential protocol of hepatocarcinogenesis, male weanling rats were fed for three or four weeks (respectively) diets containing beta-carotene, canthaxanthin, astaxanthin, or lycopene (300 mg/kg diet) or an excess of vitamin A (15,000 retinol equivalents/kg diet) or were treated intraperitoneally with 3-methylcholanthrene. During this period, all rats were injected intraperitoneally with the initiator carcinogen, either 2-NP (6 times at 100 mg/kg body wt) or DEN (once at 100 mg/kg body wt). Three weeks after the termination of carotenoid or vitamin A fee…
Using the Hemophilia Joint Health Score for assessment of children: Reliability of the Spanish version
2018
Introduction: Numerous measuring instruments for the evaluation of hemophilic arthropathy have been developed. One of the most used systems is the Hemophilia Joint Health Score (HJHS) given its sensitivity to clinical changes appearing in the joints because of recurrent hemarthrosis. Objective: Assessing the interrater reliability, using the Spanish version of the HJHS (version 2.1) in children with hemophilia. Design: Reliability study to assess the interrater reliability of the Spanish version of HJHS. Methods: A sample of 36 children aged 7–13 years diagnosed with hemophilia A or B was used. Two physiotherapists performed physical assessments with the Spanish version of the HJHS. Descrip…
Microbiota Variation Across Life Stages of European Field-Caught Anopheles atroparvus and During Laboratory Colonization: New Insights for Malaria Re…
2021
The potential use of bacteria for developing novel vector control approaches has awakened new interests in the study of the microbiota associated with vector species. To set a baseline for future malaria research, a high-throughput sequencing of the bacterial 16S ribosomal gene V3-V4 region was used to profile the microbiota associated with late-instar larvae, newly emerged females, and wild-caught females of a sylvan Anopheles atroparvus population from a former malaria transmission area of Spain. Field-acquired microbiota was then assessed in non-blood-fed laboratory-reared females from the second, sixth, and 10th generations. Diversity analyses revealed that bacterial communities varied …
Bioaccumulation of selenium-by fruit origin lactic acid bacteria in tropical fermented fruit juices
2021
Abstract Adequate fruit consumption helps to prevent several chronic age-related diseases. Selenium (Se) is an elemental micronutrient with antioxidant capacity. In general, fruits and Se ingest by humans are below the recommended daily intake value. Fresh fruits are highly susceptible to deterioration during storage. Fermentation can improve the storage period, sensory profile, and bioactive compound content of foods; moreover, some lactic acid bacteria can accumulate organic Se intracellularly. In this work, microbial growth and Se accumulation by Levilactobacillus brevis CRL2051 and Fructobacillus tropaeoli CRL2034 in tropical fruit juices were evaluated. The strains could grow 1–2 log c…
SNEWS 2.0 : a next-generation supernova early warning system for multi-messenger astronomy
2021
The next core-collapse supernova in the Milky Way or its satellites will represent a once-in-a-generation opportunity to obtain detailed information about the explosion of a star and provide significant scientific insight for a variety of fields because of the extreme conditions found within. Supernovae in our galaxy are not only rare on a human timescale but also happen at unscheduled times, so it is crucial to be ready and use all available instruments to capture all possible information from the event. The first indication of a potential stellar explosion will be the arrival of a bright burst of neutrinos. Its observation by multiple detectors worldwide can provide an early warning for t…
MONOTROPA HYPOPHEGEA WALLR., A NEW RECORD FOR THE SICILIAN FLORA
2014
During field investigations in the Mountains around Palermo, an unusual population of Monotropa sp. was found. After revision of the taxonomic literature and herbarium specimens, it was referred to Monotropa hypophegea Wallr. This species is closely related to M. hypopytis L., and in the past was considered only a variety (Pignatti 1982) or a subspecies (Křisa 1972) ) of it. More recently this entity has been considered an independent taxon deserving the rank of species (Conti et al. 2005). The most important morphological differences between the two taxa are the number of flowers in the raceme and the hairiness of sepals, petals and capsule. The individuals of the observed population have …
SEARCHES FOR POINT-LIKE AND EXTENDED NEUTRINO SOURCES CLOSE TO THE GALACTIC CENTER USING THE ANTARES NEUTRINO TELESCOPE
2014
A search for cosmic neutrino sources using six years of data collected by the ANTARES neutrino telescope has been performed. Clusters of muon neutrinos over the expected atmospheric background have been looked for. No clear signal has been found. The most signal-like accumulation of events is located at equatorial coordinates R.A. = -46º.8 and decl. = -64º.9 and corresponds to a 2.2 sigma background fluctuation. In addition, upper limits on the flux normalization of an E-2 muon neutrino energy spectrum have been set for 50 pre-selected astrophysical objects. Finally, motivated by an accumulation of seven events relatively close to the Galactic Center in the recently reported neutrino sample…
Designing robust immediate release tablet formulations avoiding food effects for BCS class 3 drugs
2019
Abstract Food induced viscosity in the gastrointestinal tract is reported to reduce the bioavailability of tablets containing BCS class 3 drugs, mainly by retarding their disintegration and dissolution of the active pharmaceutical ingredient. The role of formulation factors in minimizing this negative food effect is largely unknown. Combinations of disintegrants were studied together with soluble and insoluble fillers and trospium chloride as model drug substance. Different batches of tablets were compressed at 10 kN and 30 kN, by incorporating different combinations of croscarmellose sodium (CSS), cross-linked (CPD) and sodium starch glycolate (SSG) at low level i.e, 2% + 2% and high level…