Synthesis, structural characterization and biological evaluation of 40-C-methyl- and phenyl-dioxolane pyrimidine and purine nucleosides

Silvia Franchini,Umberto M. Battisti,Claudia Sorbi,Annalisa Tait,Andrea Cornia,정낙신,이상국,송자영,Roberta Loddo,Silvia Madeddu,Giuseppina Sanna,Livio Brasili 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.5

Nucleoside analogues play an important role inantiviral, antibacterial and antineoplastic chemotherapy. Herein we report the synthesis, structural characterizationand biological activity of some 40-C-methyl- and -phenyldioxolane-based nucleosides. In particular, a and banomers of all natural nucleosides were obtained andcharacterized by NMR, HR-MS and X-ray crystallography. The compounds were tested for antimicrobial activityagainst some representative human pathogenic fungi, bacteriaand viruses. Antitumor activity was evaluated in alarge variety of human cancer cell-lines. Although most ofthe compounds showed non-significant activity, 23aweakly inhibited HIV-1 multiplication. Moreover, 22a and32a demonstrated a residual antineoplastic activity, interestinglylinked to the unnatural a configuration. Theseresults may provide structural insights for the design ofactive antiviral and antitumor agents.

The Role of Serine/Threonine Kinases in Signal Transduction : The Multi - gene Family of Protein Kinase C

Silvia Stable 한국유전학회 1990 Genes & Genomics Vol.12 No.4

Protein kinase C (PKC), originally identified as a novel cytoplasmic protein kinase, then recognized as the major phorbol ester receptor in mammalian cells is now defined as a family of at least seven related polypeptides encoded by separate genes and expressed in a tissue-specific manner (reviewed in: Stabel, 1990). This protein kinase has gained a central role in the analysis of signal transduction through numerous experiments providing evidence for activation of protein kinase C by the second messenger diacylglycerols produced mainly from the membrane lipids phosphatidylinositol and phosphatidylcholine. With the elucidation of the structural organization of the PKC molecule it became clear that the entity "PKC" comprises more than one polypeptide (Parker et al., 1986). The complexity of this enzyme family suggests that the individual members may serve distinct roles in signal transduction pathways. As an approach to analyse the characteristics of the PKC subtypes we have used the baculovirus - insect cell expression system to produce and isolate large amounts of the polypeptides encoded by the different genes (Patel and Stabel, 1989). The mammalian enzymes expressed in the insect cells are produced as phosphoproteins which show authentic protein kinase C properties and are amenable to biochemical characterization (Stabel et al., submitted). We have also used this expression system to express another serine/threonine kinase involved in signal transduction, the protooncogene product c-Raf, in order to analyse its activation and substrate requirements. Site-directed mutagenesis has proved a useful tool to dissect functional domains of polypeptides. The construction of a kinasenegative mutant of PKC type γ has allowed us to investigate the role of the kinase domain in post-translational modification of the PKC polypeptide and its role in defined events involving PKC. One such extensively studied event is the "downregulation" of PKC after prolonged phorbol ester treatment of mammalian cells, mainly fibroblasts, epithelial cells and hematopoietic cells, which mostly contain the α and/or β types of PKC (Kischel et al., 1990). We have introduced the PKC γ type which is exclusively expressed in nervous tissue into fibroblasts and shown that it is activated and downregulated by phorbol esters in vivo. The downregulation of the PKC-γ polypeptide by proteolytic degradation also proceeds if the molecule carries an inactivated kinase domain. This suggests that downregulation of PKC-γ is not a consequence of constitutive signalling through the kinase domain but rather due to an increased proteolytic susceptibility of the polypeptide after contact with phorbol esters (Freisewinkel et al., submitted). The kinase-deficient mutant is hypophosphorylated suggesting that a substantial proportion of the post-translational modification on PKC-γ is due to inter- or intramolecular autophosphorylation.

Arsenic Uptake and Partitioning in Grafted Tomato Plants

Silvia Rita Stazi,Carla Cassaniti,Rosita Marabottini,Francesco Giuffrida,Cherubino Leonardi 한국원예학회 2016 Horticulture, Environment, and Biotechnology Vol.57 No.3

Arsenic is a toxic and cancerogenic metalloid that poses a threat to food crop consumption. Previous studies have shown that grafting vegetables onto certain rootstocks may restrict the uptake of some toxic metals, such as cadmium, lead, and so on, but no such study has investigated the uptake of arsenic. The aim of this work was to determine the following: i) if grafting can influence and reduce arsenic translocation in the root and/or aerial organs; ii) how tomato plants irrigated with arsenic-enriched nutrient solution (100 μg·L-1) accumulate this metalloid; and iii) if arsenic poses a potential risk to fruit quality. We found that differences in plant growth and the qualitative traits of fruits were mainly related to the adopted rootstock rather than to the addition of arsenic. Grafting influenced metalloid accumulation in roots and its translocation from roots to shoots and fruits. Tomato plants accumulated arsenic in their roots, and only a small portion was translocated to shoots and fruits, making the risk for human consumption negligible. Therefore, the uptake of this toxic element and its translocation are influenced by the rootstock utilized.

Quality of Life in Patients Treated with Percutaneous Laser Ablation for Non-Functioning Benign Thyroid Nodules: A Prospective Single-Center Study

Silvia Oddo,Edineia Felix,Michele Mussap,Massimo Giusti 대한영상의학회 2018 Korean Journal of Radiology Vol.19 No.1

Objective: While many studies have reported that laser ablation (LA) for benign non-fuctioning thyroid nodules is efficacious in reducing nodular volume and neck symptoms, none have described changes in quality of life (QoL). The purpose of this study was to report post-LA changes in QoL in our cohort of patients. Materials and Methods: Fourteen patients with benign thyroid nodules were involved in a prospective, single-center study and underwent a single session of LA. We evaluated the following: changes in nodule volume, thyroid function, and autoimmunity; adverse events during and after LA; changes in neck discomfort by means of a visual analogic scale (VAS) at one week and 1, 3, 6, and 12 months; and changes in QoL through the 13-scale Thyroid-specific Patient Reported Outcome (ThyPRO) questionnaire at 1, 3, 6, and 12 months. ThyPRO is a validated questionnaire for thyroid diseases, which consists of 13 scales with multiple-choice answers. They investigate several aspects of life that may be impaired by goiter-related compression symptoms, by esthetic alterations and by hypo- or hyperthyroidism. Results: Nodule volume decrease was -37 ± 23%, -55 ± 22%, -53 ± 25%, -58 ± 25% (p < 0.01 vs. baseline) at the first, third, sixth, and twelfth month, respectively. No hypothyroidism or positivization of autoimmunity was observed. There were no major complications during or after LA. After LA, VAS scores improved significantly from 1 week onwards in 100% of patients, while a significant improvement was seen in the goiter symptoms score after one month, and in the general score and mean values of ThyPRO after six months. Scores on the other ThyPRO scales did not change significantly. Conclusion: Laser ablation is safe and effective in reducing nodule volume and neck symptoms; this is confirmed by improvements in the goiter scale, general score, and mean values of ThyPRO and in the VAS score.

Experimental and numerical assessment of EBF structures with shear links

Silvia Caprili,Nicola Mussini,Walter Salvatore 국제구조공학회 2018 Steel and Composite Structures, An International J Vol.28 No.2

Eccentrically braced frames (EBF) represent an optimal structural solution for seismic prone areas, being able to provide high dissipative capacity and good elastic stiffness, to withstand strong seismic events without significant loss of bearing capacity and to avoid damage to non-structural elements in case of low and moderate earthquakes. The accurate knowledge of the cyclic behaviour of the dissipative links, characterizing the whole performance of EBFs, is required to optimize the structural properties and to refine the design techniques adopted for multi-storey buildings' analysis. Reliable numerical models for the links, at the same time requiring a limited computational effort, are then needed. The present work shows the results of a wide experimental test campaign executed on real-scale one storey/one bay frames with horizontal and vertical links, together with the elaboration of a simple semi-analytical model for the quick representation of the cyclic behaviour of shear links.

A case study of gear wheel material and heat treatment effect on gearbox strength calculation

Silvia Maláková,Anna Guzanová,Dagmar Draganovská,Gabriel Fedorko,Vieroslav Molnár 대한기계학회 2019 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.33 No.12

The paper is focused on the influence of gearing material and thermal or chemical-thermal processing of wheels on the results of the strength calculation carried out in accordance to the standard, in particular on the safety factor. This effect is examined on a gearbox that was part of the steel coil production line in the integrated steel plant. Due to changes in production, the load on the gears increased. Thus, the result of this work is the selection of new materials for the two-speed gearbox and their heat treatment to meet the safety conditions of the gearing mechanism without changing the geometrical parameters of the gearbox.

Local Innovation for Public Transfers and Management Policy in the Case of Canada

Silvia Amato 한국경제연구학회 2018 Korea and the World Economy Vol.19 No.3

For the critical knowledge area of the nuclear industry and nuclear waste management what has come into evidence is the attachment to territorial and identity norms. Most studies have referred to environmental politics and environmental justice but, at the same time, it needs to be addressed the territorial national dimension. In connection with public and private partnerships (PPPs) in Canada, the sectoral development has been experienced in terms of public performances and territorial practices. For the management of nuclear power plants through the PPPs, political relationships have been shaped according to different levels of productive interactions, which have been related to environmental affectation policies. The comparative increase of regional productions and trans-sectoral economic interests has determined social adaptive patterns indicating the interrelated environmental justice issues, which have been expressed on the basis of common knowledge platforms and social open confrontations.

Global , Universal Human Rights in a Cross - Cultural Perspective

(Silvia Augeneder) 세계헌법학회 한국학회 2001 世界憲法硏究 Vol.6 No.-

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Intraumbilical versus intramuscular oxytocin in the management of the third stage of labor

Silvia Waleska Bu,César Alas-Pineda,David Aguilar-Andino,Dalton Argean Norwood,Kristhel Gaitán-Zambrano,Mario Pinto-Romero 대한산부인과학회 2023 Obstetrics & Gynecology Science Vol.66 No.2

ObjectiveTo compare the effect of intraumbilical vein oxytocin injection with standard management in reducing blood loss during the third and fourth stages of labor. Acute complications threaten the mother’s life during the third and fourth stages of labor. The most common complication is postpartum hemorrhage, which remains a leading cause of maternal mortality, particularly in developing countries. MethodsA randomized controlled trial was conducted in the Gynecology and Obstetrics Department of Leonardo Mart?nez Valenzuela Hospital from January to June 2021. A probabilistic sample was used: 332 pregnant patients were enrolled in the study and randomized into the case (166 patients) and control (166 patients) groups. The volume of blood lost was compared between the groups. ResultsThe median estimated blood loss was 120 mL (interquartile range [IQR], 80-218.75 mL). There was a statistically significant difference between the groups, showing less estimated blood loss in the international unit group with a median of 80 mL (IQR, 60-100 mL) (P<0.001), and 200 mL (IQR, 143.75-300 mL) in the intramuscular (IM) group, highlighting that 66.8% of the IM group had an estimated blood loss >251 mL. ConclusionAny reduction in bleeding during labor is clinically relevant because it improves patient prognosis. The use of intraumbilical oxytocin injection with active management of the third stage of labor significantly reduced postpartum blood loss and the duration of the third stage compared with the IM group.

The Relationship of Steroid Hormones, Genes Related to Testosterone Metabolism and Behavior in Boys With Autism in Slovakia

Silvia Lakatošová,Katarína Janšáková,Jaroslava Babková,Gabriela Repiská,Ivan Belica,Mária Vidošovičová,Daniela Ostatníková 대한신경정신의학회 2022 PSYCHIATRY INVESTIGATION Vol.19 No.2

Objective Purpose of the study was to identify the relationship among actual plasmatic levels of steroid hormones and behavioral manifestations in boys with autism and to assess the genetic contribution to these manifestations.Methods 172 boys with autism under 10 years of age and 135 neurotypical boys attended the study. ADI-R and ADOS-2 were used to evaluate the core symptom severities. Problem behavior was assessed using BPI-01 questionnaire. Levels of testosterone, estradiol, dehydroepiandrosterone, dehydroepiandrosterone-sulfate and sex hormone binding globulin (SHBG) were measured in plasma of autistic boys. Three SNPs (in ESR1, SHBG, SRD5A2 genes) and one STR in AR gene (number of CAG repeats in first exon) were assessed. Hormonal levels and number of CAG repeats in AR gene were used for correlation analysis with behavioral measures. Genotype and allelic frequencies were compared among autistic and neurotypical boys.Results We found negative relationship among SHBG levels and restricted, repetitive behaviors (measured by ADOS-2) and positive relationship among actual testosterone levels and frequency of stereotyped behavior (measured by BPI-01).Conclusion Actual levels of SHBG and testosterone are related to severities of restricted and repetitive behaviors in boys with autism. Mechanisms of action of these hormones in brain require further investigation.