77 research outputs found
Recent advances in the development of {CB}1R selective probes
No full textCannabinoid subtype 1 receptors (CB1Rs) are an important class of G protein-coupled receptors (GPCRs) belonging to the endocannabinoid system. CB1Rs play a crucial modulatory role in the functioning of other neurotransmitter systems and are involved in a wide range of physiological functions and dysfunctions; thus, they are considered one of the most important targets for drug development, as well as diagnostic purposes. Despite this, only a few molecules targeting this receptor are available on the pharmaceutical market, thus emphasizing the need to gain a deeper understanding of the complex activation pathways of CB1Rs and how they regulate diseases. As part of this review, we provide an overview of pharmacological and imaging tools useful for detecting CB1Rs. Herein, we summarize the derivations of cannabinoids and terpenoids with fluorescent compounds, radiotracers, or photochromic motifs. CB1Rs’ molecular probes may be used in vitro and, in some cases, in vivo for investigating and exploring the roles of CB1Rs together with the starting point for the development of CB1R-targeted drugs
"Negari tamen non potest Venetos Ius Civile Romanorum colere et venerari": Venetian Law and ius commune between the Seventeenth and Eighteenth Centuries
No full textIn the mid-Seventeenth century, Arthur Duck noted that the Venetians lived according to their own customs and laws, without adopting the Ius Civile Romanorum. The author, however, remarked that in modern Venice those same Roman laws were renowned and to some extent followed. The present contribution investigates this issue through an analysis of judicial practice in both criminal and civil matters. As we will see, the authority of ius commune in criminal matters was often evident and sometimes explicit, whereas in civil matters Roman laws were applied only insofar as they reflected natural justice and equity
FLAVANONES FROM AMYGDALUS LYCIOIDES SPACH: ISOLATION, CHARACTERIZATION AND BIOLOGICAL EVALUATION
No full textChiral Flavanones from Amygdalus lycioides Spach: Structural Elucidation and Identification of TNFalpha Inhibitors by Bioactivity-guided Fractionation
No full textl-Lactate metabolism in HEP G2 cell mitochondria due to the l-lactate dehydrogenase determines the occurrence of the lactate/pyruvate shuttle and the appearance of oxaloacetate, malate and citrate outside mitochondria
No full textAs part of an ongoing study of l-lactate metabolism both in normal and in cancer cells, we investigated whether and how l-lactate metabolism occurs in mitochondria of human hepatocellular carcinoma (Hep G2) cells. We found that Hep G2 cell mitochondria (Hep G2-M) possess an l-lactate dehydrogenase (ml-LDH) restricted to the inner mitochondrial compartments as shown by immunological analysis, confocal microscopy and by assaying ml-LDH activity in solubilized mitochondria. Cytosolic and mitochondrial l-LDHs were found to differ from one another in their saturation kinetics. Having shown that l-lactate itself can enter Hep G2 cells, we found that Hep G2-M swell in ammonium l-lactate, but not in ammonium pyruvate solutions, in a manner inhibited by mersalyl, this showing the occurrence of a carrier-mediated l-lactate transport in these mitochondria. Occurrence of the l-lactate/pyruvate shuttle and the appearance outside mitochondria of oxaloacetate, malate and citrate arising from l-lactate uptake and metabolism together with the low oxygen consumption and membrane potential generation are in favor of an anaplerotic role for l-LAC in Hep G2-M
Adherence to Antibiotic Prescription of Dental Patients: The Other Side of the Antimicrobial Resistance
No full textSince non-adherence to antibiotic therapy can cause several problems, including antimicrobial resistance (AMR) and treatment failures, the present study evaluated adherence to oral antibiotic therapy and AMR awareness among consecutively enrolled dental patients. Data concerning age, gender, socioeconomic status, education level, cohabitation, and general health were retrieved from medical records. AMR awareness was investigated through direct questions and adherence to antibiotic treatment was assessed through a modified Italian version of the Morisky medical scale-8 items. Participants' characteristics were analyzed in relation to treatment adherence and AMR, using a Χ2 independence test (significance level of α <0.1). Dental patients generally showed a low (51.82%) adherence to oral antibiotic therapy, and medium and high adherence was reported only by 29.37% and 18.81% of participants. Treatment adherence was similar in relation to participants' gender and age but significantly lower in subjects with only secondary school graduation and higher in participants with higher education levels. Non-cohabitants were significantly more adherent than cohabitants. AMR awareness was declared by 42.15% of males and 38.70% of females: 56.52% of dental patients aware of AMR were 18-38 years old, 35.20% were 39-59 years old, and 26.95% were aged between 60 and 80. Further studies are needed to develop adequate strategies, expanding dental patients' knowledge of AMR, thus optimizing the benefits and reducing the risks of antibiotic administration in dental patients
Synthesis and biological evaluation of epothilone A dimeric compounds
No full textThe preparation and biological evaluation of a novel series of dimeric epothilone A derivatives (1-6) are described. Two types of diacyl spacers were introduced to establish the various dimeric epothilone A constructs. The effect of these compounds on tubulin polymerization and their cytotoxicity against four different cancer cell lines are reported. Several of the newly synthesized compounds inhibit endothelial cell differentiation and endothelial cell migration that are key steps of the angiogenic process
Deploying an Instance Segmentation Algorithm to Implement Social Distancing for Prosthetic Vision
No full textThe COVID-19 pandemic outbreak is causing a dramatic worsening in the already complicated living conditions of blind and visually impaired individuals. Social distancing is the most effective strategy to limit virus spread, but is extremely difficult for blind people to actuate. Here we propose a deep-learning algorithm to recognize and locate in space people and other categories of objects from RGB-D images. The algorithm, based on Mask R-CNN, performs semantic segmentation on RGB images and uses depth maps to extract information about the relative distance of the instances. It was evaluated using Salient Person dataset and RGB-D Scenes Dataset v.2, and proved effective in segmenting and locating instances. This preliminary work could be a valuable starting point for developing a technology to assist the visually impaired in implementing social distancing.TN
Cane d’un filosofo, cane d’un eretico. Appunti sulla fortuna cristiana del cane “sillogistico"
No full textThe author studies some aspects of the Christian fortune of Chrysippus' "syllogistical dog", from Late antiquity to the byzantine ag
The so-called improper delegated legislation at national and local levels
No full textFil: Passarella, Julián Emmanuel. Universidad Nacional del Litoral. Facultad de Ciencias Jurídicas y Sociales; Argentina.En la República Argentina, tanto el Poder Ejecutivo nacional como los ejecutivos provinciales y municipales tienen a su cargo la aplicación, integración y puesta en práctica de las leyes y ordenanzas. Esta atribución es ejercida a través del dictado de normas reglamentarias de distinta jerarquía, intensidad y amplitud, que el autor clasifica en reglamentos de ejecución, reglamentos autorizados o de integración —a partir de una delegación legislativa impropia— y reglamentos delegados. La tesis consiste en delimitar los contornos y demostrar la existencia de la llamada "delegación legislativa impropia", tanto en el ámbito nacional como en los regímenes provinciales y municipales. Dicho objetivo es abordado a partir del estudio del régimen federal argentino, de las constituciones de la Nación y de las provincias, de la doctrina y, principalmente, de la jurisprudencia de la Corte Suprema de Justicia de la Nación y de los tribunales de la mayoría de las provincias de nuestro país.In the Argentine Republic, the National Executive Branch as well as the Provincial and Municipal Executive Branches are in charge of the application, integration and enforcement of laws and ordinances. Such powers are exercised through the issuance of regulations of different levels, intensity and scope, which the author classifies as Implementing Regulations, Authorized or Integrative Regulations (which stem from an improper delegated legislation) and Delegated Regulations. This dissertation consists in delimiting their scope and proving the existence of the so-called “Improper Delegated Legislation” at a national level as well as at the provincial and municipal levels. This objective has been approached from the study of the Argentine Federal Regime, the National and Provincial Constitutions, the legal Doctrine and, mainly, the Case Law of the Argentine Supreme Court of Justice and the Courts of the majority of the Argentine provinces
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