52 research outputs found
Desmontar relatos patriarcales y crear relatos innovadores : dos tareas imprescindibles
págs. 137-152Capítulo incluido en el libro: Transversalidad de género en el audiovisual andaluz. Trinidad Núñez Domínguez, Teresa Vera Balanza y Rosa M.ª Díaz Jiménez (Eds.). Sevilla: Universidad Internacional de Andalucía, 2015. ISBN: 978-84-7993-280-0. Enlace: http://hdl.handle.net/10334/352
Effects of flooding on mental health: a case-control study
3rd International Congress on Neurobiology, Psychopharmacology & Treatment guidance (May 30th - June 2nd, 2013)Background: Post-disaster mental health problems may affect population in different ways.
Population exposure to a natural disaster has been associated with psychological distress, in
particular, in the development of Posttraumatic Stress Disorder (PTSD).
Most people experience distress after their exposure to an extreme event. For people with good psychosocial resilience and access to social support, mental health problems can be relatively less important since supporting relationships and inner capabilities may begin the adaptation processes. Mental disorders occur often, but less commonly than dis-tress, and in some cases they may require intensive and long term continuing interventions and treatment
Nutritional quality of the most consumed varieties of raw and cooked rice in Spain submitted to an in vitro digestion model
Rice is one of the most consumed staple foods around the world and its trade is highly globalized. Increased environmental pollution generates a large amount of waste that, in many cases, is discarded close to culture fields. Some species are able to bioaccumulate toxic substances, such as metals, that could be transferred to the food chain. The main goal of this study was to evaluate the content of metallic (Al, Cd, Pb, and Cr) and metalloid elements (As) in 14 of the most consumed varieties of rice in Spain and their effects on human health. The samples were cooked, and human digestion was simulated by using a standard in vitro digestion method. Metallic and metalloid element levels were analysed by Inductively Coupled Plasma Optical Emission Spectrometry (ICPOES), previous called microwave digestion. Both the human health risk index, Hazard Quotient, and Lifetime Cancer Risk did not show toxic values in any case. Rice with a higher non-digestible fraction showed a higher liberation of proteins and a lower glycemic index. There were no significant differences in the concentrations of metallic and metalloid elements in cooked rice or in the digestible fraction in all varieties analysed. However, Al concentrations were higher than other metals in all varieties studied due to its global distribution. No relationship has been observed between the digestibility of rice and the bioaccessibility of each metallic and metalloid element. All of the studied rice varieties are healthy food products and its daily consumption is safe. The regular monitoring of metals and As in rice consumed in Spain may contribute to improvements in the human health risk evaluation.Universidad de Sevilla VIPPIT-2021-I.
Biological Evaluation of New Thienopyridinium and Thienopyrimidinium Derivatives as Human Choline Kinase Inhibitors
This research was funded by Convocatoria 2019 Proyectos de I + D + i − RTI Tipo B
“Ministerio de Innovación y Ciencia” grant number PID2019-109294RB-I00 and “Convocatoria 2020
Proyectos I + D + i del Programa Operativo FEDER 2020”, grant number B-CTS-216-UGR20. E.P
thanks the European Regional Development Fund (ERDF) project BioDrug (No. 1.1.1.5/19/A/004)
and the Latvian Council of Science (grant No. lzp-2020/2-0013) for financial support.Due to its role in lipid biosynthesis, choline kinase α1 (CKα1) is an interesting target for the
development of new antitumor agents. In this work, we present a series of 41 compounds designed
based on the well-known and successful strategy of introducing thienopyridine and pyrimidine as
bioisosteres of other heterocycles in active antitumor compounds. Notwithstanding the fact that
some of these compounds do not show significant enzymatic inhibition, others, in contrast, feature
substantially improved enzymatic and antiproliferative inhibition values. This is also confirmed
by docking analysis, whereby compounds with longer linkers and thienopyrimidine cationic head
have been identified as the most compelling. Among the best compounds is Ff-35, which inhibits the
growth of different tumor cells at submicromolar concentrations. Moreover, Ff-35 is more potent in
inhibiting CKα1 than other previous biscationic derivatives. Treatment of A549, Hela, and MDA-MB-231 cells with Ff-35 results in their arrest at the G1 phase of the cell cycle. Furthermore, the compound
induces cellular apoptosis in a concentration-dependent manner. Altogether, these findings indicate
that Ff-35 is a promising new chemotherapeutic agent with encouraging preclinical potential.Ministerio de Innovación y Ciencia PID2019-109294RB-I00FEDER 2020 B-CTS-216-UGR20European Regional Development Fund (ERDF) 1.1.1.5/19/A/004Latvian Council of Science lzp-2020/2-00
New Compounds with Bioisosteric Replacement of Classic Choline Kinase Inhibitors Show Potent Antiplasmodial Activity
This research was funded by Convocatoria 2019 Proyectos de I + D + i - RTI Tipo B
“Ministerio de Ciencia e Innovación” grant number PID2019–109294RB-I00, University of Granada,
Cei-BioticProject grant number CEI2013-MP-1, the Instituto de Salud Carlos III Subdirección General
de Redes y Centros de Investigación Cooperativa-Red de Investigación Cooperativa en Enfermedades
Tropicales (RICET: RD16/0027/0014), the Plan Nacional (SAF PID2019-109623RB-I002016-79957-R)
and the Junta de Andalucía (BIO-199).Supplementary Materials: The following are available online at https://www.mdpi.com/article/10.3390/pharmaceutics13111842/s1, Figure S1. Pf CKIC50 Curves Inhibition of Pf CK. Figure S2. IC50Curves. Figure S3. Spectra.In the fight against Malaria, new strategies need to be developed to avoid resistance of
the parasite to pharmaceutics and other prevention barriers. Recently, a Host Directed Therapy
approach based on the suppression of the starting materials uptake from the host by the parasite
has provided excellent results. In this article, we propose the synthesis of bioisosteric compounds
that are capable of inhibiting Plasmodium falciparum Choline Kinase and therefore to reduce choline
uptake, which is essential for the development of the parasite. Of the 41 bioisosteric compounds
reported herein, none showed any influence of the linker on the antimalarial and enzyme inhibitory
activity, whereas an effect of the type of cationic heads used could be observed. SARs determined
that the thienopyrimidine substituted in 4 by a pyrrolidine is the best scaffold, independently of
the chosen linker. The decrease in lipophilicity seems to improve the antimalarial activity but to
cause an opposite effect on the inhibition of the enzyme. While potent compounds with similar good
inhibitory values have been related to the proposed mechanism of action, some of them still show
discrepancies and further studies are needed to determine their specific molecular target.Ministerio de Ciencia e Innovación PID2019–109294RB-I00University of Granada CEI2013-MP-1Plan Nacional (SAF PID2019-109623RB-I002016-79957-R)Junta de Andalucía (BIO-199)Instituto de Salud Carlos III (RICET: RD16/0027/0014
New compounds with bioisosteric replacement of classic choline kinase inhibitors show potent antiplasmodial activity.
In the fight against Malaria, new strategies need to be developed to avoid resistance of the parasite to pharmaceutics and other prevention barriers. Recently, a Host Directed Therapy approach based on the suppression of the starting materials uptake from the host by the parasite has provided excellent results. In this article, we propose the synthesis of bioisosteric compounds that are capable of inhibiting Plasmodium falciparum Choline Kinase and therefore to reduce choline uptake, which is essential for the development of the parasite. Of the 41 bioisosteric compounds reported herein, none showed any influence of the linker on the antimalarial and enzyme inhibitory activity, whereas an effect of the type of cationic heads used could be observed. SARs determined that the thienopyrimidine substituted in 4 by a pyrrolidine is the best scaffold, independently of the chosen linker. The decrease in lipophilicity seems to improve the antimalarial activity but to cause an opposite effect on the inhibition of the enzyme. While potent compounds with similar good inhibitory values have been related to the proposed mechanism of action, some of them still show discrepancies and further studies are needed to determine their specific molecular target.This research was funded by Convocatoria 2019 Proyectos de I + D + i - RTI Tipo B “Ministerio de Ciencia e Innovación” grant number PID2019–109294RB-I00, University of Granada, Cei-BioticProject grant number CEI2013-MP-1, the Instituto de Salud Carlos III Subdirección General de Redes y Centros de Investigación Cooperativa-Red de Investigación Cooperativa en Enfermedades Tropicales (RICET: RD16/0027/0014), the Plan Nacional (SAF PID2019-109623RB-I002016-79957-R) and the Junta de Andalucía (BIO-199)
New Compounds with Bioisosteric Replacement of Classic Choline Kinase Inhibitors Show Potent Antiplasmodial Activity
In the fight against Malaria, new strategies need to be developed to avoid resistance of the parasite to pharmaceutics and other prevention barriers. Recently, a Host Directed Therapy approach based on the suppression of the starting materials uptake from the host by the parasite has provided excellent results. In this article, we propose the synthesis of bioisosteric compounds that are capable of inhibiting Plasmodium falciparum Choline Kinase and therefore to reduce choline uptake, which is essential for the development of the parasite. Of the 41 bioisosteric compounds reported herein, none showed any influence of the linker on the antimalarial and enzyme inhibitory activity, whereas an effect of the type of cationic heads used could be observed. SARs determined that the thienopyrimidine substituted in 4 by a pyrrolidine is the best scaffold, independently of the chosen linker. The decrease in lipophilicity seems to improve the antimalarial activity but to cause an opposite effect on the inhibition of the enzyme. While potent compounds with similar good inhibitory values have been related to the proposed mechanism of action, some of them still show discrepancies and further studies are needed to determine their specific molecular target
Biological Evaluation of New Thienopyridinium and Thienopyrimidinium Derivatives as Human Choline Kinase Inhibitors
Due to its role in lipid biosynthesis, choline kinase α1 (CKα1) is an interesting target for the development of new antitumor agents. In this work, we present a series of 41 compounds designed based on the well-known and successful strategy of introducing thienopyridine and pyrimidine as bioisosteres of other heterocycles in active antitumor compounds. Notwithstanding the fact that some of these compounds do not show significant enzymatic inhibition, others, in contrast, feature substantially improved enzymatic and antiproliferative inhibition values. This is also confirmed by docking analysis, whereby compounds with longer linkers and thienopyrimidine cationic head have been identified as the most compelling. Among the best compounds is Ff-35, which inhibits the growth of different tumor cells at submicromolar concentrations. Moreover, Ff-35 is more potent in inhibiting CKα1 than other previous biscationic derivatives. Treatment of A549, Hela, and MDA-MB-231 cells with Ff-35 results in their arrest at the G1 phase of the cell cycle. Furthermore, the compound induces cellular apoptosis in a concentration-dependent manner. Altogether, these findings indicate that Ff-35 is a promising new chemotherapeutic agent with encouraging preclinical potential
Fingerprints as Predictors of Schizophrenia: A Deep Learning Study
Background and hypothesis: The existing developmental bond between fingerprint generation and growth of the central nervous system points to a potential use of fingerprints as risk markers in schizophrenia. However, the high complexity of fingerprints geometrical patterns may require flexible algorithms capable of characterizing such complexity. Study design: Based on an initial sample of scanned fingerprints from 612 patients with a diagnosis of non-affective psychosis and 844 healthy subjects, we have built deep learning classification algorithms based on convolutional neural networks. Previously, the general architecture of the network was chosen from exploratory fittings carried out with an independent fingerprint dataset from the National Institute of Standards and Technology. The network architecture was then applied for building classification algorithms (patients vs controls) based on single fingers and multi-input models. Unbiased estimates of classification accuracy were obtained by applying a 5-fold cross-validation scheme. Study results: The highest level of accuracy from networks based on single fingers was achieved by the right thumb network (weighted validation accuracy = 68%), while the highest accuracy from the multi-input models was attained by the model that simultaneously used images from the left thumb, index and middle fingers (weighted validation accuracy = 70%). Conclusion: Although fitted models were based on data from patients with a well established diagnosis, since fingerprints remain lifelong stable after birth, our results imply that fingerprints may be applied as early predictors of psychosis. Specially, if they are used in high prevalence subpopulations such as those of individuals at high risk for psychosis.This work was supported by several grants funded by the Instituto de Salud Carlos III and the Spanish Ministry of Science and Innovation (co-funded by the European Regional Development Fund/European Social Fund “Investing in your future”): Miguel Servet Research Contract (CPII13/00018 to RS, CPII16/00018 to EP-C, CP20/00072 to MF-V), PFIS Contract (FI19/0352 to MG-R). Research Mobility programme (MV18/00054 to EP-C), Research Projects (PI18/00877 and PI21/00525 to RS). It has also been supported by the Centro de Investigación Biomédica en Red de Salud Mental and the Generalitat de Catalunya: 2014SGR1573 and 2017SGR1365 to EP-C and SLT008/18/00206 to IF-R from the Departament de Salut. The authors have declared that there are no conflicts of interest in relation to the subject of this study.S
- …