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5 results on '"López-Montero, Eulogio"'

1. Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity

Author

Uliassi, Elisa, Fiorani, Giulia, Krauth-Siegel, R. Luise, Bergamini, Christian, Fato, Romana, Bianchini, Giulia, Carlos Menéndez, J., Molina, Maria Teresa, López-Montero, Eulogio, Falchi, Federico, Cavalli, Andrea, Gul, Sheraz, Kuzikov, Maria, Ellinger, Bernhard, Witt, Gesa, Moraes, Carolina B., Freitas-Junior, Lucio H., Borsari, Chiara, Costi, Maria Paola, and Bolognesi, Maria Laura

Published
2017
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2. Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase ( Tb GAPDH) and Trypanosoma cruzi trypanothione reductase ( Tc TR) and display trypanocidal activity

Author

Uliassi, Elisa, primary, Fiorani, Giulia, additional, Krauth-Siegel, R. Luise, additional, Bergamini, Christian, additional, Fato, Romana, additional, Bianchini, Giulia, additional, Carlos Menéndez, J., additional, Molina, Maria Teresa, additional, López-Montero, Eulogio, additional, Falchi, Federico, additional, Cavalli, Andrea, additional, Gul, Sheraz, additional, Kuzikov, Maria, additional, Ellinger, Bernhard, additional, Witt, Gesa, additional, Moraes, Carolina B., additional, Freitas-Junior, Lucio H., additional, Borsari, Chiara, additional, Costi, Maria Paola, additional, and Bolognesi, Maria Laura, additional

Published
2017
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3. Activities of naphthoquinones against Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae), vector of dengue and Biomphalaria glabrata (Say, 1818), intermediate host of Schistosoma mansoni

Author

Ribeiro, Karlos A. L., Carvalho, Cenira Monteiro de, Molina Orden, María Teresa, Pereira Lima, Estelita, López-Montero, Eulogio, Farias de Oliveira, Maria Beatriz, Ventura Pinto, Antonio, Santana, Antônio Euzébio G., Goulart, Marília O. F., Reys, José Rui M., Ribeiro, Karlos A. L., Carvalho, Cenira Monteiro de, Molina Orden, María Teresa, Pereira Lima, Estelita, López-Montero, Eulogio, Farias de Oliveira, Maria Beatriz, Ventura Pinto, Antonio, Santana, Antônio Euzébio G., Goulart, Marília O. F., and Reys, José Rui M.

Abstract

Larvicidal (against Aedes aegypti Linnaeus, 1762) and molluscicidal (against Biomphalaria glabrata Say,1818) activities of several natural and synthetic naphthoquinoneswere measured, with significant results. The best larvicidal compound is 3-bromojuglone, while the better molluscicides are 2-bromo- and 3- bromo-5-acetoxy-1,4-naphthoquinones together with the 3-bromo-5-methoxy derivative. The present results reinforce the potential use of substituted hydroxyquinones, their salts and halogenated quinones as very promising compounds against 4th instar larves of Aedes aegypti, the vector of dengue and against adult snail of Biomphalaria glabrata.

Published
2009

4. Activities of naphthoquinones against Aedes aegypti (Linnaeus, 1762) (Diptera: Culicidae), vector of dengue and Biomphalaria glabrata (Say, 1818), intermediate host of Schistosoma mansoni

Author

Ribeiro, Karlos A.L., primary, de Carvalho, Cenira Monteiro, additional, Molina, Maria Teresa, additional, Lima, Estelita Pereira, additional, López-Montero, Eulogio, additional, Reys, José Rui M., additional, de Oliveira, Maria Beatriz Farias, additional, Pinto, Antonio Ventura, additional, Santana, Antônio Euzébio G., additional, and Goulart, Marília O.F., additional

Published
2009
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5. Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity

Author

Giulia Bianchini, Bernhard Ellinger, Lucio H. Freitas-Junior, Giulia Fiorani, Eulogio López-Montero, Maria Laura Bolognesi, Maria Teresa Molina, Gesa Witt, Elisa Uliassi, R. Luise Krauth-Siegel, Maria Paola Costi, Romana Fato, Christian Bergamini, Federico Falchi, Sheraz Gul, J. Carlos Menéndez, Carolina B. Moraes, Maria Kuzikov, Andrea Cavalli, Chiara Borsari, DIPARTIMENTO DI FARMACIA E BIOTECNOLOGIE, Facolta' di MEDICINA e CHIRURGIA, AREA MIN. 03 - Scienze chimiche, AREA MIN. 05 - Scienze biologiche, Publica, Uliassi, Elisa, Fiorani, Giulia, Krauth-Siegel, R. Luise, Bergamini, Christian, Fato, Romana, Bianchini, Giulia, Carlos Menéndez, J., Molina, Maria Teresa, López-Montero, Eulogio, Falchi, Federico, Cavalli, Andrea, Gul, Sheraz, Kuzikov, Maria, Ellinger, Bernhard, Witt, Gesa, Moraes, Carolina B., Freitas-Junior, Lucio H., Borsari, Chiara, Costi, Maria Paola, and Bolognesi, Maria Laura

Subjects
0301 basic medicine, Parasitic Sensitivity Test, Models, Molecular, Crassiflorone, Trypanosomiasi, Dehydrogenase, 01 natural sciences, NADPH Oxidoreductases, chemistry.chemical_compound, Parasitic Sensitivity Tests, Coumarins, Models, Drug Discovery, NADH, NADPH Oxidoreductases, Leishmaniasis, Glyceraldehyde 3-phosphate dehydrogenase, Natural products, Tumor, biology, Trypanocidal Agent, Molecular Structure, Quinones, Glyceraldehyde-3-Phosphate Dehydrogenases, General Medicine, Trypanocidal Agents, Biochemistry, Quinone, Glyceraldehyde-3-phosphate dehydrogenase, Diospyros crassiflora, Drug, Human, Leishmaniasi, Trypanosoma cruzi, Trypanosoma brucei brucei, Trypanosoma brucei, Coumarin, Natural product, Cell Line, Dose-Response Relationship, 03 medical and health sciences, Structure-Activity Relationship, Trypanosomiasis, Cell Line, Tumor, Structure–activity relationship, Humans, Trypanocidal agent, Trypanocidal activity, Pharmacology, Dose-Response Relationship, Drug, 010405 organic chemistry, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, Molecular, biology.organism_classification, 0104 chemical sciences, 030104 developmental biology, Trypanothione reductase, chemistry, NADH, biology.protein, NADH, NADPH Oxidoreductase
Abstract

none 20 si Crassiflorone is a natural product with anti-mycobacterial and anti-gonorrhoeal properties, isolated from the stem bark of the African ebony tree Diospyros crassiflora. We noticed that its pentacyclic core possesses structural resemblance to the quinone-coumarin hybrid 3, which we reported to exhibit a dual-targeted inhibitory profile towards Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR). Following this basic idea, we synthesized a small library of crassiflorone derivatives 15-23 and investigated their potential as anti-trypanosomatid agents. 19 is the only compound of the series showing a balanced dual profile at 10 μM (% inhibitionTbGAPDH= 64% and % inhibitionTcTR= 65%). In phenotypic assay, the most active compounds were 18 and 21, which at 5 μM inhibited Tb bloodstream-form growth by 29% and 38%, respectively. Notably, all the newly synthesized compounds at 10 μM did not affect viability and the status of mitochondria in human A549 and 786-O cell lines, respectively. However, further optimization that addresses metabolic liabilities including solubility, as well as cytochromes P450 (CYP1A2, CYP2C9, CYP2C19, and CYP2D6) inhibition, is required before this class of natural product-derived compounds can be further progressed. Uliassi, Elisa; Fiorani, Giulia; Krauth-Siegel, R. Luise; Bergamini, Christian; Fato, Romana; Bianchini, Giulia; Carlos Menéndez, J.; Molina, Maria Teresa; López-Montero, Eulogio; Falchi, Federico; Cavalli, Andrea; Gul, Sheraz; Kuzikov, Maria; Ellinger, Bernhard; Witt, Gesa; Moraes, Carolina B.; Freitas-Junior, Lucio H.; Borsari, Chiara; Costi, Maria Paola; Bolognesi, Maria Laura* Uliassi, Elisa; Fiorani, Giulia; Krauth-Siegel, R. Luise; Bergamini, Christian; Fato, Romana; Bianchini, Giulia; Carlos Menéndez, J.; Molina, Maria Teresa; López-Montero, Eulogio; Falchi, Federico; Cavalli, Andrea; Gul, Sheraz; Kuzikov, Maria; Ellinger, Bernhard; Witt, Gesa; Moraes, Carolina B.; Freitas-Junior, Lucio H.; Borsari, Chiara; Costi, Maria Paola; Bolognesi, Maria Laura*

Published
2017

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