Investigation on Quantitative Structure-Activity Relationships of 1,3,4 Oxadiazole Derivatives as Potential Telomerase Inhibitors

The published manuscript is available at EurekaSelect via http://www.eurekaselect.com/164022/article, DOI : 10.2174/1570163815666180724113208. © 2018 Bentham ScienceA series of 1,3,4-oxadiazole derivatives with significant broad-spectrum anticancer activity against different cell lines, and demonstrated telomerase inhibition, was subjected to Quantitative Structure-Activity Relationships (QSAR) analysis. Validated models with high correlation coefficients were developed. The Multiple Linear Regression (MLR) models, by Ordinary Least Squares (OLS), showed good robustness and predictive capability, according to the Multi-Criteria Decision Making (MCDM = 0.8352), a technique that simultaneously enhances the performances of a certain number of criteria. The descriptors selected for the models, such as electrotopological state (E-state) descriptors, and extended topochemical atom (ETA) descriptors, showed the relevant chemical information contributing to the activity of these compounds. The results obtained in this study make sure about the identification of potential hits as prospective telomerase inhibitors.Peer reviewedFinal Accepted Versio

Predicting Skin Permeability by means of Computational Approaches : Reliability and Caveats in Pharmaceutical Studies

© 2019 American Chemical Society.The skin is the main barrier between the internal body environment and the external one. The characteristics of this barrier and its properties are able to modify and affect drug delivery and chemical toxicity parameters. Therefore, it is not surprising that permeability of many different compounds has been measured through several in vitro and in vivo techniques. Moreover, many different in silico approaches have been used to identify the correlation between the structure of the permeants and their permeability, to reproduce the skin behavior, and to predict the ability of specific chemicals to permeate this barrier. A significant number of issues, like interlaboratory variability, experimental conditions, data set building rationales, and skin site of origin and hydration, still prevent us from obtaining a definitive predictive skin permeability model. This review wants to show the main advances and the principal approaches in computational methods used to predict this property, to enlighten the main issues that have arisen, and to address the challenges to develop in future research.Peer reviewedFinal Accepted Versio

Massive thymic hyperplasia in a 15-month-old boy: Case report and literature review

Key Clinical Message A surgical approach is the choice in young infants with MTH, who are furthest from the time of physiological involution of the thymus, and when the thymus achieves the largest relative size, a surgical approach is the choice. Steroid therapy has been shown to be ineffective (4, 9, 16, 18-20). No surgical complications have been reported, and the outcome is excellent. Recurrence has been seen in only one case

Inflammatory myofibroblastic lung tumor: its birth, its bleeding growth, its difficult diagnosis and its surgical end in a child

The diagnosis of inflammatory myofibroblastic tumor is based on radiology and histology. The treatment is surgical, and the prognosis is good. For this reason, although this lung disease is rare, when a child show up at hospital with an unknown hemoptysis, this medical condition should not be underestimated

Long COVID-19 in Children: From the Pathogenesis to the Biologically Plausible Roots of the Syndrome

Long Coronavirus disease-19 (COVID-19) refers to the persistence of symptoms related to the infection with severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2). This condition is described as persistent and can manifest in various combinations of signs and symptoms, such as fatigue, headache, dyspnea, depression, cognitive impairment, and altered perception of smells and tastes. Long COVID-19 may be due to long-term damage to different organs-such as lung, brain, kidney, and heart-caused by persisting viral-induced inflammation, immune dysregulation, autoimmunity, diffuse endothelial damage, and micro thrombosis. In this review, we discuss the potential and biologically plausible role of some vitamins, essential elements, and functional foods based on the hypothesis that an individual's dietary status may play an important adjunctive role in protective immunity against COVID-19 and possibly against its long-term consequences

Health-Related Quality of Life in Patients with CVID Under Different Schedules of Immunoglobulin Administration: Prospective Multicenter Study

We assessed the health-related quality of life (HRQoL) in CVID adults receiving different schedules of immunoglobulin replacement therapy (IgRT) by intravenous (IVIG), subcutaneous (SCIG), and facilitated (fSCIG) preparations. For these patients, IgRT schedule was chosen after a period focused on identifying the most suitable individual option

Hemp Stem Epidermis and Cuticle: From Waste to Starter in Bio-Based Material Development

Nowadays, hemp farmers are facing an urgent problem related to plant stem disposal after seed harvesting. In this work, the commonly discarded epidermis and cuticle of hemp stems were valorized, turning them towards a sustainable recycling and reuse, contributing to the circular economy concept. Cellulose deprived of amorphous regions was obtained by a green process consisting of an ethanolic ultrasound-assisted maceration followed by mild bleaching/hydrolysis. The obtained hemp cellulose was esterified with citric acid resulting in a 1.2-fold higher crystallinity index and 34 ∘C lower Tg value compared to the non-functionalized hemp cellulose. Green innovative biocomposite films were developed by embedding the modified cellulose into PLA by means of an extrusion process. The structural and morphological characterization of the obtained biocomposites highlighted the functionalization and further embedment of cellulose into the PLA matrix. Attenuated Total Reflectance–Fourier Transform Infrared spectroscopy (ATR-FTIR) results suggested physical and chemical interactions between PLA and the organic filler in the biofilms, observing a homogeneous composition by Field Emission-Scanning Electron Microscopy (FESEM). Moreover, some increase in thermal stability was found for biocomposites added with 5%wt of the hemp cellulose filler. The obtained results highlighted the feasible recovery of cellulose from hemp stem parts of disposal concern, adding value to this agro-waste, and its potential application for the development of novel biocomposite films to be used in different applications

The cloning of the virus envelope glycoprotein F of canine distemper virus expressed in Pichia pastoris

Canine distemper virus (CDV) is a pathogen which affects members of the Canidae family, causing an acute, often fatal, systemic disease. CDV is an RNA virus of the family Paramyxoviridae that contains two envelope glycoproteins: F and HA. In this study, we focused on the envelope glycoprotein F as the main target for neutralizing antibodies produced after infection or vaccination. The complete coding region of the protein (60 kDa) was expressed in the methylotrophic yeast Pichia pastoris, obtained in a recombinant form and secreted to the culture medium. Later, to analyze its immunogenicity, the protein was combined with an oily adjuvant and used to inoculate mice. The results provide evidence supporting a potential application of this recombinant protein as a subunit vaccine.Fil: Tizzano, Marco Antonio. Universidad Nacional de La Plata. Facultad de Ciencias Veterinarias; ArgentinaFil: Sguazza, Guillermo Hernán. Universidad Nacional de La Plata. Facultad de Ciencias Veterinarias; ArgentinaFil: Picotto, Leandro Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina. Universidad Nacional de La Plata. Facultad de Ciencias Veterinarias; ArgentinaFil: Echeverria, Maria Gabriela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina. Universidad Nacional de La Plata. Facultad de Ciencias Veterinarias; ArgentinaFil: Pecoraro, Marcelo Ricardo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de La Plata. Facultad de Ciencias Veterinarias; Argentin

Non-vitamin K antagonist oral anticoagulants and antiphospholipid syndrome

The current treatment of thrombotic APS patients includes long-term anticoagulation with oral vitamin K antagonists (VKAs), with warfarin being the one most commonly used. However, the use of VKAs can be challenging, especially in patients with APS. VKAs monitoring in patients with aPL is complicated by the heterogeneous responsiveness to LAs of reagents used in the International Normalized Ratio test, potentially resulting in instability of anticoagulation. For decades, VKAs were the only available oral anticoagulants. However, non-VKA oral anticoagulants, including a direct thrombin inhibitor (dabigatran etexilate) and direct anti-Xa inhibitors (rivaroxaban, apixaban and edoxaban), are currently available. The use of these agents may represent a major step forward since, unlike VKAs, they have few reported drug interactions and they do not interact with food or alcohol intake, thereby resulting in more stable anticoagulant intensity. Most importantly, monitoring their anticoagulant intensity is not routinely required due to their predictable anticoagulant effects. In this review, we discuss the clinical and laboratory aspects of non-VKA oral anticoagulants, focusing on the available evidence regarding their use in patients with APS