Person:
Marco Contelles, José Luis

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First Name
José Luis
Last Name
Marco Contelles
URI
https://hdl.handle.net/20.500.14352/83458
Affiliation
Universidad Complutense de Madrid
Faculty / Institute
Farmacia
Department
Area
Química Orgánica
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2014 - 201912020 - 20234
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Author: Ramos Alonso, Eva × Has files: true ×

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    Project number: 165
    Página web orientada a la evaluación “in silico” de nuevas sustancias con interés biológico IV
    (2021) Ramos Alonso, Eva; Romero Martínez, Manuel Alejandro; García Cantón, Carolina; Marco Contelles, José Luis; Pita Pita, Rene; Rodríguez Martín, Abigail; Rodríguez Talavera, María
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    Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer’s disease
    (European Journal of Medicinal Chemistry, 2014) Oset Gasque, María Jesús; González Prieto, María Del Pilar; Pérez Peña, Javier; García Font, Nuria; Romero Martínez, Manuel Alejandro; Pino Sans, Javier Del; Ramos Alonso, Eva; Hadjipavlou-Litina, Dimitra; Soriano, Elena; Chioua, Mourad; Samadi, Abdelouahid; Raghuvanshi, Dushyant S.; Singh, Krishna N.; Marco Contelles, José Luis
    The pharmacological analysis of racemic chromenotacrines (CT) 1e7, bearing the 11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ol ring skeleton, in a series of experiments targeted to explore their potential use for the treatment of Alzheimer’s disease (AD), is reported. The toxicological evaluation showed that among all these chromenotacrines, CT6 is much less hepatotoxic than tacrine in a range of concentrations from 1 to 300 mM, measured as cell viability in HepG2 cells. Moreover, CT6 did not significantly increase lactate dehydrogenase, aspartate transaminase, and alanine transaminase release in HepG2 cells. Besides,CT6treatment exerts a high protective effect against thelipid peroxidationinduced after H2O2-treated SHSY5Y cells, in a concentration-dependent manner. CT6 showed an excellent antioxidant profile in the AAPH test, and protects against the decrease in cell viability induced by respiratory chain inhibitors (Oligomicyn A/Rotenone)and NO donors in neuronal cultures. This effect could be due to a mixed antiapoptotic and antinecrotic neuroprotective effect at low and intermediate CT6 concentrations, respectively. CT1-7 are potent and selective inhibitors of EeAChE in the submicromolar range. CT3 [IC50 (EeAChE) ¼ 0.007 0.003 mM], and CT6 [IC50 (EeAChE) ¼ 0.041 0.001 mM] are the most potent AChE inhibitors. Kinetic studies on the non-toxic chromenotacrine CT6 showed that this compound behaves as a non-competitive inhibitor (Ki ¼ 0.047 0.003 mM),indicating that CT6 binds at the peripheral anionic site, a fact confirmed by molecular modeling analysis. In silico ADMET analysis showed also that CT6 should have a moderate BBB permeability. Consequently, non-toxic chromenotacrine CT6can be considered as an ttractivemultipotent molecule for the potential treatment of AD.
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    Project number: 150
    Página web orientada a la evaluación in silico de nuevas sustancias con interés biológico (parte V)
    (2022) Ramos Alonso, Eva; Romero Martínez, Manuel Alejandro; García Cantón, Carolina; Pita Pita, Rene; Rodríguez Martín, Abigail; Rodríguez Talavera, María; Marco Contelles, José Luis
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    Project number: 101
    Página web orientada a la evaluación “in silico” de nuevas sustancias con interés biológico. Parte III
    (2020) Ramos Alonso, Eva; Romero Martínez, Manuel Alejandro; Rodríguez Martín, Abigail; Rodríguez Talavera, María; Marco Contelles, José Luis; García Cantón, Carolina; Pita Pita, Rene
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    Project number: 190
    Página web orientada a la evaluación in silico de nuevas sustancias con interés biológico (parte VI)
    (2023) Ramos Alonso, Eva; Marco Contelles, José Luis; Pita Pita, Rene; Rodríguez Martín, Abigail; Rodriguez Talavera, María; Egea, Javier; Paramo Muñoz, Ana; Ríos, Cristóbal de los; Romero Martínez, Manuel Alejandro; García Cantón, Carolina
    En la línea de las ediciones anteriores, los resultados obtenidos con el proyecto "INSILITOX" han sido muy positivos. Por esta razón, el equipo se ha propuesto continuar optimizando la página web añadiendo nuevos recursos que apoyen la formación de los estudiantes, tanto de Grado como de Posgrado, en este entorno multilingüe de aprendizaje virtual adaptativo.