Evaluation of a new educational resource-dynamic slides- for the teaching of Organic Chemistry in the Pharmacy Degree

Se ha llevado a cabo la implantación de un nuevo recurso didáctico en la enseñanza de la Química Orgánica de la Licenciatura de Farmacia, con los objetivos de adaptar la docencia tradicional al Espacio Europeo de Educación Superior (EEES) y de facilitar la comprensión y el aprendizaje de la asignatura. El citado recurso didáctico está basado en la utilización de presentaciones dinámicas en PowerPoint. Con él se intenta paliar algunos de los problemas más comunes que se suelen presentar en la enseñanza de la Química Orgánica, como es la dificultad experimentada por el alumnado para la asimilación de los conceptos complejos implicados en la materia. La metodología empleada hace uso de dos recursos: Hand-outs (guías), parcialmente completos, de las diapositivas del tema a impartir y diapositivas dinámicas. Se ha efectuado una evaluación preliminar del método mediante un cuestionario de opinión que han contestado los alumnos. Del análisis de esta encuesta hemos extraído conclusiones positivas, que indican una buena aceptación por parte del alumnado hacia la nueva metodología docente.A new educational resource has been introduced for the teaching of Organic Chemistry to second-year students in the Pharmacy Degree. Its aim is the adaptation of the traditional education to the European Space for Higher Education and to facilitate the learning and understanding of Organic Chemistry. This resource involves the use of dynamic PowerPoint presentations in an attempt to overcome some of the most common problems in the teaching of Organic Chemistry. One of them is the difficulty of making complex concepts understandable to the students. The used methodology makes use of two different resources for the teaching of each lesson: Partially completed hand-outs, made out from the slides of the lesson to teach, and dynamic slides. A preliminary evaluation of the method has been performed by means of an opinion poll completed by the students. A series of positive conclusions has been drawn from the analysis of the answers to this survey, indicating a good acceptance of the new educational methodology between the students

Selective Anticancer Therapy Based on a HA-CD44 Interaction Inhibitor Loaded on Polymeric Nanoparticles

This research was funded by the Consejeria de Economia, Conocimiento, Empresas y Universidad of the Junta de Andalucia (grant number Excellence Research Project P18-RT-1679) and the Research Results Transfer Office (OTRI) of the University of Granada (grant number PR/17/006 project). This work was partially supported by grants from the Spanish Ministry of Economy and Competitiveness (MINECO), grant number PID2019.110987RB.I00; the Health Institute Carlos III (ISCIII), grant number DTS18/00121 the Junta de Andalucia-FEDER, Ministry of Economy, Knowledge, Companies, and University (FEDER 2018: ref. B-FQM-475-UGR18, PAIDI2020: ref. PT18-TP-4160); and the Andalusian Regional Government, grant number PAIDI-TC-PVT-PSETC-2.0. C.D. thanks HECBioSim, the UK High End Computing Consortium for Biomolecular Simulation (hecbiosim.ac.uk), which is supported by the EPSRC (EP/L000253/1) for awarding computing time in Jade, a UK Tier-2 resource. B.R.-R. gratefully acknowledges funding from the European Union's Horizon 2020 Research and Innovation Program under Marie Sklodowska-Curie Grant Agreement no. 754446 and UGR Research and Knowledge Transfer Fund-Athenea3i. J.M.E.-R. thanks the Spanish Ministry of Education for PhD funding (scholarship FPU 16/02061). V.C.-C. thanks the Andalusian Regional Government for her postdoctoral fellowship (POSTDOC_21_00118).Hyaluronic acid (HA), through its interactions with the cluster of differentiation 44 (CD44), acts as a potent modulator of the tumor microenvironment, creating a wide range of extracellular stimuli for tumor growth, angiogenesis, invasion, and metastasis. An innovative antitumor treatment strategy based on the development of a nanodevice for selective release of an inhibitor of the HACD44 interaction is presented. Computational analysis was performed to evaluate the interaction of the designed tetrahydroisoquinoline-ketone derivative (JE22) with CD44 binding site. Cell viability, efficiency, and selectivity of drug release under acidic conditions together with CD44 binding capacity, effect on cell migration, and apoptotic activity were successfully evaluated. Remarkably, the conjugation of this CD44 inhibitor to the nanodevice generated a reduction of the dosis required to achieve a significant therapeutic effect.Junta de Andalucia P18-RT-1679Research Results Transfer Office (OTRI) of the University of Granada PR/17/006Spanish Government PID2019.110987RB.I00Health Institute Carlos III (ISCIII) DTS18/00121Junta de Andalucia-FEDER, Ministry of Economy, Knowledge, Companies, and University (FEDER) B-FQM-475-UGR18 PT18-TP-4160Andalusian Regional Government POSTDOC_21_00118UK Research & Innovation (UKRI)Engineering & Physical Sciences Research Council (EPSRC) EP/L000253/1European Union's Horizon 2020 Research and Innovation Program under Marie Sklodowska-Curie Grant 754446UGR Research and Knowledge Transfer Fund-Athenea3iSpanish Government FPU 16/0206

The use of a web application – SciFinder to complement the Organic Chemistry teaching to the student of the Degree in Pharmacy

La necesidad de motivación del alumno, además de la adaptación de la actual enseñanza a los créditos ECTS, han sido los motores que nos han llevado a proponer el uso de una aplicación web denominada SciFinder en la enseñanza de la Química Orgánica. Se trata de una herramienta imprescindible en la investigación avanzada que se utiliza en cualquier laboratorio de síntesis química. La Universidad de Granada dispone de una suscripción que permite 6 usos simultáneos a la que el alumno puede acceder a través de un acceso directo a SciFinder on Web en el sólo es necesario registrarse como usuario. Permitir al alumno transportarse a un laboratorio virtual es una de las múltiples posibilidades que ofrece esta aplicación web ayudándoles a complementar los conocimientos científicos básicos que se han explicado en clase. Durante el desarrollo de los distintos temas que componen la asignatura se plantearán reacciones concretas que el alumno deberá ampliar con la información que esta aplicación les proporciona: reactivos empleados en dichas reacciones condiciones de reacción (estequiometría, tiempo, temperatura…) bibliografía actual. Al final del curso académico se evaluará esta nueva experiencia mediante encuestas de opinión del alumnado para determinar dos aspectos fundamentales de la misma, el aumento de interés por la asignatura durante el desarrollo del trabajo y la dificultad en la realización del mismo.The need to motivate the students, besides adapting the teaching to the ECTS credits, have been the driving force that leads us to propose the use of a web application called Sci Finder in the education of Organic Chemistry. It is an essential tool used in any advanced research laboratory of synthetic chemistry. The University of Granada provides a subscription with 6 simultaneous accesses. The students may accede directly to the SciFinder on Web being only necessary the registration as users. One of the many possibilities that offers this web application allows to the student be transported to a virtual laboratory and complement the basic scientific knowledge explained in class. During the development of the different topics, specific reactions will be presented to the student and they may increase the information by using this application: reagents of the reactions reaction conditions (stoichiometry, time, temperature…) up-to-date bibliography At the end of the academic year this new experience will be evaluate through opinion poll to the student in order to determinate two essential aspect, the interest increase for the subject during the development of this work and the difficulty in carrying out it

N-Aryltetrahydroisoquinoline derivatives as HA-CD44 interaction inhibitors: design, synthesis, computational studies, and antitumor effect

Supplementary data to this article can be found online at https://doi.org/10.1016/j.ejmech.2023.115570.Funding This research was funded by the Consejería de Universidad, Inves- tigaci´on e Innovaci´on of the Junta de Andalucía and FEDER, Una manera de hacer Europa (P18-RT-1679, PT18-TP-4160, B-FQM-475- UGR18 and PAIDI-TC-PVT-PSETC-2.0.), the Research Results Transfer Office (OTRI) of the University of Granada (PR/17/006), the Spanish Ministry of Economy and Competitiveness (PID2019.110987RB.I00 and PID2021.128109OB.I00) and the Health Institute Carlos III (DTS18/ 00121). C.D. thanks HECBioSim, the UK High End Computing Con- sortium for Biomolecular Simulation (hecbiosim.ac.uk), which is sup- ported by the EPSRC (EP/L000253/1) for awarding computing time in Jade, a UK Tier-2 resource. B.R.-R. gratefully acknowledges funding from the European Union’s Horizon 2020 Research and Innovation Program under Marie Sklodowska-Curie Grant Agreement no. 754446 and UGR Research and Knowledge Transfer Fund—Athenea3i. J.M.E.-R. thanks the Spanish Ministry of Education for a studentship (FPU 16/ 02061). A.M.-M. gratefully acknowledges funding from the HPC- Europa3 Transnational Access programme supported by the European Commission H2020 Research & Innovation GA # 730897 (application number HPC17ARM6V). Funding for open access charge: Universidad de Granada / CBUA.Hyaluronic acid (HA) plays a crucial role in tumor growth and invasion through its interaction with cluster of differentiation 44 (CD44), a non-kinase transmembrane glycoprotein, among other hyaladherins. CD44 expression is elevated in many solid tumors, and its interaction with HA is associated with cancer and angiogenesis. Despite efforts to inhibit HA-CD44 interaction, there has been limited progress in the development of small molecule inhibitors. As a contribution to this endeavour, we designed and synthesized a series of N-aryltetrahydroisoquinoline derivatives based on existing crystallographic data available for CD44 and HA. Hit 2e was identified within these structures for its antiproliferative effect against two CD44+ cancer cell lines, and two new analogs (5 and 6) were then synthesized and evaluated as CD44-HA inhibitors by applying computational and cell-based CD44 binding studies. Compound 2-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-5-ol (5) has an EC50 value of 0.59 μM against MDA-MB-231 cells and is effective to disrupt the integrity of cancer spheroids and reduce the viability of MDA-MB-231 cells in a dose-dependent manner. These results suggest lead 5 as a promising candidate for further investigation in cancer treatment.Consejería de Universidad, Investigación e Innovación of the Junta de Andalucía and FEDER, Una manera de hacer Europa (P18-RT-1679, PT18-TP-4160, B-FQM-475- UGR18 and PAIDI-TC-PVT-PSETC-2.0.)Research Results Transfer Office (OTRI) of the University of Granada (PR/17/006),panish Ministry of Economy and Competitiveness (PID2019.110987RB.I00 and PID2021.128109OB.I0)Health Institute Carlos III (DTS18/ 00121)EPSRC (EP/L000253/1)European Union’s Horizon 2020 Research and Innovation Program under Marie Sklodowska-Curie Grant Agreement no. 754446HPC-Europa3 Transnational Access programme supported by the European Commission H2020 Research & Innovation GA # 730897Funding for open access charge: Universidad de Granada / CBUA

1-(Benzenesulfonyl)-1,5-dihydro-4,1-benzoxazepine as a new scaffold for the design of antitumor compounds

Aim: Bozepinib is a potent and selective anticancer compound which chemical structure is made up of a benzofused seven-membered ring and a purine moiety. We previously demonstrated that the purine fragment does not exert antiproliferative effect per se. Methodology: A series of 1-(benzenesulfonyl)-4,1-benzoxazepine derivatives were synthesized in order to study the influence of the benzofused seven-membered ring in the biological activity of bozepinib by means of antiproliferative, cell cycle and apoptosis studies. Results & conclusion: Our results show that the methyleneoxy enamine sulfonyl function is essential in the antitumor activity of the structures and thus, it is a scaffold suitable for further modification with a view to obtain more potent antitumor compounds

Overexpression of budding yeast protein phosphatase Ppz1 impairs translation

The Ser/Thr protein phosphatase Ppz1 from Saccharomyces cerevisiae is the best characterized member of a family of enzymes only found in fungi. Ppz1 is regulated in vivo by two inhibitory subunits, Hal3 and Vhs3, which are moonlighting proteins also involved in the decarboxylation of the 4-phosphopantothenoylcysteine (PPC) intermediate required for coenzyme A biosynthesis. It has been reported that, when overexpressed, Ppz1 is the most toxic protein in yeast. However, the reasons for such toxicity have not been elucidated. Here we show that the detrimental effect of excessive Ppz1 expression is due to an increase in its phosphatase activity and not to a plausible down-titration of the PPC decarboxylase components. We have identified several genes encoding ribosomal proteins and ribosome assembly factors as mild high-copy suppressors of the toxic Ppz1 effect. Ppz1 binds to ribosomes engaged in translation and copurifies with diverse ribosomal proteins and translation factors. Ppz1 overexpression results in Gcn2-dependent increased phosphorylation of eIF2α at Ser-51. Consistently, deletion of GCN2 partially suppresses the growth defect of a Ppz1 overexpressing strain. We propose that the deleterious effects of Ppz1 overexpression are in part due to alteration in normal protein synthesis.Ministerio de Economia, Industria y Competitividad BFU2017-82574-P, BFU2016-75352-

From binge eating to binge drinking: A new and robust paradigm for assessing binge ethanol self-administration in male rats

Animal models of alcohol (ethanol) self-administration are crucial to dissect the neurobiological mechanisms underlying alcohol dependence, yet only a few of these induce pharmacologically relevant levels of alcohol consumption and rarely the alcohol self-administration co-occurs with other addictive behaviours. The present study aims to validate a novel model of voluntary ethanol consumption in male Wistar rats, in which ethanol access follows a binge eating experience. Over 10 sessions, Wistar rats were exposed to binge or control eating (i.e., the ingestion of 11.66 and 0.97 kcal/3 min, respectively, derived from a highly palatable food), immediately followed by two-bottle choice intake tests (2%, 6%, 10% or 14% w/w ethanol vs. water). Rats exposed to binge eating drank significantly more 6% or 10% (w/w) ethanol than control peers, reaching up to 6.3 gEtOH/kg. Rats stimulated with 2%, 6%, 10% or 14% ethanol after binge eating, but not those given those ethanol concentrations after control eating, exhibited significant within-group increases in ethanol drinking. This ethanol consumption was not altered by quinine adulteration (up to 0.1 g/L), and it was blocked by naltrexone (10 mg/kg), administered immediately before binge eating. Blood ethanol levels significantly correlated with ethanol consumption; and the more ethanol consumed, the greater the distance travelled in an open field test conducted after the two-bottle choice test. Altogether, this self-administration model seems a valid and robust alternative with remarkable potential for research on different stages of the alcohol addiction and, particularly, to assess interactions between alcohol consumption and others addictive-like behaviours.Junta de Andalucía, Grant/Award Numbers: CTS109, B-CTS-422-UGR18Ministerio de Universidades, Spain, Grant/Award Number: FPU18/05012Ministry of Science and Innovation, Grant/Award Number: MICIUPID2020- 114269GB-I00Spanish Ministry of Health (Government Delegation for the National Plan on Drugs), Grant/Award Number: PNSD 2020-04

Adaptation to climate variability among the coffee farmers of the watersheds of the rivers Porce and Chinchiná, Colombia

ABSTRACT: This article seeks to explain the practices used by small farmers to cope with climate variability and extreme weather events in the basins of the Chinchiná and Porce rivers located on the central Andes in Colombia. The information wasglacie collected through interviews, observations on farms and workshops with farmers. Additionally historical averages on temperature, precipitation and sunshine were compared with those values recorded in 2010 during the transition between El Niño an La Niña events. During the first quarter of 2010 the average temperature in Chinchiná increased by 1.4 C° and the solar brightness by 14%, while the precipitation experienced a 46% reduction. In contrast, during the second half of the year there was a decrease of 0.8 C° in temperature, a 31% reduction in solar brightness and an increase in precipitation of 62%. The coffee production in the years 2011 and 2012 was the lowest in the country in the last 35 years despite the cultivated area increased.RESUMEN: Este artículo pretende dar cuenta de las prácticas usadas por algunos caficultores de dos cuencas andinas colombianas para enfrentar la variabilidad climática. La información fue recogida a través de entrevistas, observaciones en las fincas y talleres. Los resultados indican que el manejo de la sombra en los cafetales, la renovación con variedades resistentes a la roya, la asociación de cultivos, las coberturas vegetales, la siembra escalonada y la reforestación son estrategias utilizadas para minimizar los efectos de la variabilidad climática. Sin embargo, en una de las cuencas estas estrategias son más frecuentes que en la otra, donde la producción ha cambiado hacia un sistema más tecnificado. Los caficultores utilizan además otras alternativas como el agroturismo, la integración de la mano de obra familiar, la asociatividad comunitaria y gremial, el jornaleo y estrategias de comercialización como los mercados justos y las certificaciones que ayudan a mejorar los precios de venta para resistir los momentos de crisis

Aplicación de la imagen infrarroja para la detección en línea de producción de defectos en flejes de focos para cocinas vitrocerámicas

La termografía activa es una conocida técnica de ensayo no destructivo que se aplica en multitud de campos. En esta comunicación se presenta una aplicación de la misma a la detección de defectos en el línea de producción de focos para cocinas vitrocerámicas. El fleje del foco se excita con un pulso eléctrico y su respuesta térmica en forma de secuencia de imágenes es capturada y procesada en un tiempo inferior a 250 ms