Person: Villacampa Sanz, Mercedes
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First Name
Mercedes
Last Name
Villacampa Sanz
Affiliation
Universidad Complutense de Madrid
Faculty / Institute
Farmacia
Department
Química en Ciencias Farmacéuticas
Area
Química Orgánica
Identifiers
11 results
Search Results
Now showing 1 - 10 of 11
Item Quinones as Neuroprotective Agents(Antioxidants, 2023) Cores Esperón, Ángel; Carmona Zafra, Noelia; Clerigué Louzado, José; Villacampa Sanz, Mercedes; Menéndez Ramos, José CarlosQuinones can in principle be viewed as a double-edged sword in the treatment of neurodegenerative diseases, since they are often cytoprotective but can also be cytotoxic due to covalent and redox modification of biomolecules. Nevertheless, low doses of moderately electrophilic quinones are generally cytoprotective, mainly due to their ability to activate the Keap1/Nrf2 pathway and thus induce the expression of detoxifying enzymes. Some natural quinones have relevant roles in important physiological processes. One of them is coenzyme Q10, which takes part in the oxidative phosphorylation processes involved in cell energy production, as a proton and electron carrier in the mitochondrial respiratory chain, and shows neuroprotective effects relevant to Alzheimer’s and Parkinson’s diseases. Additional neuroprotective quinones that can be regarded as coenzyme Q10 analogues are idobenone, mitoquinone and plastoquinone. Other endogenous quinones with neuroprotective activities include tocopherol-derived quinones, most notably vatiquinone, and vitamin K. A final group of non-endogenous quinones with neuroprotective activity is discussed, comprising embelin, APX-3330, cannabinoid-derived quinones, asterriquinones and other indolylquinones, pyrroloquinolinequinone and its analogues, geldanamycin and its analogues, rifampicin quinone, memoquin and a number of hybrid structures combining quinones with amino acids, cholinesterase inhibitors and non-steroidal anti-inflammatory drugs.- Project number: 377
Item Empleo de Software libre para la enseñanza en el área de la Química Orgánica(2022) González Matilla, Juan Francisco; Gómez-Carpintero Jiménez, Jorge; Menéndez Ramos, José Carlos; Ramos García, María Teresa; Villacampa Sanz, Mercedes; Sanchez Cebrián, Juan Domingo Item Bisavenathramide Analogues as Nrf2 Inductors and Neuroprotectors in In Vitro Models of Oxidative Stress and Hyperphosphorylation(Antioxidants, 2021) Cores Esperón, Ángel; Abril Comesaña, Sheila; Michalska Dziama, Patrycja; Duarte, Pablo; Olives Barba, Ana Isabel; Martín Carmona, María Antonia; Villacampa Sanz, Mercedes; León Martínez, Rafael; Menéndez Ramos, José CarlosOxidative stress is crucial to the outbreak and advancement of neurodegenerative diseases and is a common factor to many of them. We describe the synthesis of a library of derivatives of the 4-arylmethylen-2-pyrrolin-5-one framework by sequential application of a three-component reaction of primary amines, β-dicarbonyl compounds, and α-haloketones and a Knoevenagel condensation. These compounds can be viewed as cyclic amides of caffeic and ferulic acids, and are also structurally related to the bisavenanthramide family of natural antioxidants. Most members of the library showed low cytotoxicity and good activity as inductors of Nrf2, a transcription factor that acts as the master regulator of the antioxidant response associated with activation of the antioxidant response element (ARE). Nrf2-dependent protein expression was also proved by the significant increase in the levels of the HMOX1 and NQO1 proteins. Some compounds exerted neuroprotective properties in oxidative stress situations, such as rotenone/oligomycin-induced toxicity, and also against protein hyperphosphorylation induced by the phosphatase inhibitor okadaic acid. Compound 3i, which can be considered a good candidate for further hit-to-lead development against neurodegenerative diseases due to its well-balanced multitarget profile, was further characterized by proving its ability to reduce phosphorylated Tau levels.Item NRF2 Regulation Processes as a Source of Potential Drug Targets against Neurodegenerative Diseases(Biomolecules, 2020) Cores Esperón, Ángel; Piquero Martí, Marta; Villacampa Sanz, Mercedes; León Martínez, Rafael; Menéndez Ramos, José CarlosNRF2 acts by controlling gene expression, being the master regulator of the Phase II antioxidant response, and also being key to the control of neuroinflammation. NRF2 activity is regulated at several levels, including protein degradation by the proteasome, transcription, and post-transcription. The purpose of this review is to offer a concise and critical overview of the main mechanisms of NRF2 regulation and their actual or potential use as targets for the treatment of neurodegenerative diseases.Item Curcumin-Piperlongumine Hybrids with a Multitarget Profile Elicit Neuroprotection in In Vitro Models of Oxidative Stress and Hyperphosphorylation(Antioxidants, 2021) Cores Esperón, Ángel; Carmona Zafra, Noelia; Martín Cámara, Olmo; Sánchez Cebrián, Juan Domingo; Duarte, Pablo; Villacampa Sanz, Mercedes; Bermejo Bescos, María De La Paloma; Martín-Aragón Álvarez, Sagrario; León Martínez, Rafael; Menéndez Ramos, José CarlosCurcumin shows a broad spectrum of activities of relevance in the treatment of Alzheimer’s disease (AD); however, it is poorly absorbed and is also chemically and metabolically unstable, leading to a very low oral bioavailability. A small library of hybrid compounds designed as curcumin analogues and incorporating the key structural fragment of piperlongumine, a natural neuroinflammation inhibitor, were synthesized by a two-step route that combines a three-component reaction between primary amines, β-ketoesters and α-haloesters and a base-promoted acylation with cinnamoyl chlorides. These compounds were predicted to have good oral absorption and CNS permeation, had good scavenging properties in the in vitro DPPH experiment and in a cellular assay based on the oxidation of dichlorofluorescin to a fluorescent species. The compounds showed low toxicity in two cellular models, were potent inductors of the Nrf2-ARE phase II antioxidant response, inhibited PHF6 peptide aggregation, closely related to Tau protein aggregation and were active against the LPS-induced inflammatory response. They also afforded neuroprotection against an oxidative insult induced by inhibition of the mitochondrial respiratory chain with the rotenone-oligomycin A combination and against Tau hyperphosphorylation induced by the phosphatase inhibitor okadaic acid. This multitarget pharmacological profile is highly promising in the development of treatments for AD and provides a good hit structure for future optimization efforts.- Project number: 96
Item El podcast como recurso didáctico en las asignaturas de Química Orgánica y Farmacéutica en el Grado de Farmacia y doble Grado de Farmacia y Nutrición Humana y dietética(2023) Ruiz Serrano, Miriam; Sánchez Cebrián, Juan Domingo; López-Alvarado Gutiérrez, María Pilar; Ramos García, María Teresa; Villacampa Sanz, Mercedes; Menéndez Ramos, José Carlos; Giorgi Poletti, Giorgio; Sarabia Vallejo, Álvaro; Cores Esperón, Ángel; Clerigué Louzado, José; León Martínez, Rafael; Herrero Gómez, Natalia; Rodríguez Cordero, María Luisa; Solera Viana, María; Cledera Crespo, María Pilar; Polo Parra, Sonia; Rico Arjona, RocíoEste proyecto tiene como objetivo la creación, divulgación y uso didáctico de los podcasts como herramienta de difusión de contenidos científicos para el estudio y la profundización de las asignaturas de Química Orgánica y Química Farmacéutica. En este sentido, se pretende que el alumnado, habituado al uso de medios tecnológicos y redes sociales, aprenda a utilizar este recurso no sólo como un instrumento de entretenimiento, sino como un potente medio para el aprendizaje. Item Enantioselective Synthesis and Pharmacological Evaluation of Aza-CGP37157–Lipoic Acid Hybrids for the Treatment of Alzheimer’s Disease(Antioxidants, 2022) Cores Esperón, Ángel; Michalska Dziama, Patrycja; Pérez Moreno, José Miguel; Crisman Vigil, Enrique; Gómez Serrano, Clara; Villacampa Sanz, Mercedes; Menéndez Ramos, José Carlos; León Martínez, RafaelHybrids based on an aza-analogue of CGP37157, a mitochondrial Na+/Ca2+ exchanger antagonist, and lipoic acid were obtained in order to combine in a single molecule the antioxidant and NRF2 induction properties of lipoic acid and the neuroprotective activity of CGP37157. The four possible enantiomers of the hybrid structure were synthesized by using as the key step a fully diastereoselective reduction induced by Ellman’s chiral auxiliary. After computational druggability studies that predicted good ADME profiles and blood–brain permeation for all compounds, the DPPH assay showed moderate oxidant scavenger capacity. Following a cytotoxicity evaluation that proved the compounds to be non-neurotoxic at the concentrations tested, they were assayed for NRF2 induction capacity and for anti-inflammatory properties and measured by their ability to inhibit nitrite production in the lipopolysaccharide-stimulated BV2 microglial cell model. Moreover, the compounds were studied for their neuroprotective effect in a model of oxidative stress achieved by treatment of SH-SY5Y neuroblastoma cells with the rotenone–oligomycin combination and also in a model of hyperphosphorylation induced by treatment with okadaic acid. The stereocenter configuration showed a critical influence in NRF2 induction properties, and also in the neuroprotection against oxidative stress experiment, leading to the identification of the compound with S and R configuration as an interesting hit with a good neuroprotective profile against oxidative stress and hyperphosphorylation, together with a relevant anti-neuroinflammatory activity. This interesting multitarget profile will be further characterized in future work.- Project number: PIMCD282/23-24
Item El podcast como herramienta de aprendizaje: Contribuciones de la Química Farmacéutica en el entorno “One Health”(2024) Ruiz Serrano, Miriam; Menéndez Ramos, José Carlos; López-Alvarado Gutiérrez, María Pilar; Villacampa Sanz, Mercedes; González Matilla, Juan Francisco; Sánchez Cebrián, Juan Domingo; Sarabia Vallejo, Álvaro; Carmona Zafra, Noelia; Rodríguez Cordero, María Luisa; Herrero Gómez, Natalia; Solera Viana, María; Polo Parra, Sonia; Sánchez Cledera, Jaime; Ramos García, María TeresaEste proyecto se presenta como continuación del proyecto de innovación docente Nº 96 (2022/2023) y tiene como objetivo crear un modelo didáctico basado en el aprendizaje autónomo y práctico del alumnado mediante la escucha, elaboración y/o edición de podcasts, abordando temas relacionados con la importancia de la Química Farmacéutica en el campo de la salud y el bienestar. - Project number: 143
Item Uso del vídeo tutorial como soporte multimedia para la comprensión de los mecanismos de las reacciones químicas en las competencias de la Química Orgánica(2020) Cuesta Elósegui, Elena De La; Menéndez Ramos, José Carlos; López-Alvarado Gutiérrez, María Pilar; Ramos García, María Teresa; Villacampa Sanz, Mercedes; González Matilla, Juan Francisco; Cledera Crespo, María Pilar; Blázquez Barbadillo, Cristina; Sánchez Cebrián, Juan Domingo - Project number: 111
Item Desarrollo del aula virtual como soporte del aprendizaje flexible, de las competencias relacionadas con la determinación estructural de compuestos orgánicos(2019) González Matilla, Juan Francisco; Cuesta Elósegui, Elena De La; Menéndez Ramos, José Carlos; Villacampa Sanz, Mercedes; Ramos García, María Teresa; Cores Esperón, ÁngelLa mejora en la actividad docente y la eficacia del tiempo dedicado al aprendizaje por el alumno, están estrechamente ligadas al tiempo que dedica el alumno al aprendizaje fuera del aula. Con el desarrollo y avance de las TIC, en los últimos tiempos ha ganado terreno una práctica de aprendizaje que tiene su origen en la educación a distancia y que se conoce hoy como e-learning, educación virtual o, educación en línea. En este sentido hemos diseñado y elaborado una serie de fichas de problemas sobre determinación estructural de compuestos orgánicos. En este proyecto también se han elaborado vídeos tutoriales donde se indican las pautas necesarias para resolver los problemas de determinación estructural.