Identificador persistente para citar o vincular este elemento: http://hdl.handle.net/10553/42249
Título: Lawsone, juglone, and β-Lapachone derivatives with enhanced mitochondrial-based toxicity
Autores/as: Anaissi-Afonso, Laura
Oramas-Royo, Sandra
Ayra-Plasencia, Jessel
Martín Rodríguez, Patricia 
García-Luis, Jonay
Lorenzo-Castrillejo, Isabel
Fernández Pérez, Leandro Fco 
Estévez-Braun, Ana
Machín, Félix
Clasificación UNESCO: 32 Ciencias médicas
Palabras clave: Saccharomyces-Cerevisiae
Oxidative Stress
Cytotoxicity
Yeast
Naphthoquinones, et al.
Fecha de publicación: 2018
Editor/a: 1554-8929
Publicación seriada: ACS Chemical Biology 
Resumen: Naphthoquinones are among the most active natural products obtained from plants and microorganisms. Naphthoquinones exert their biological activities through pleiotropic mechanisms that include reactivity against cell nucleophiles, generation of reactive oxygen species (ROS), and inhibition of proteins. Here, we report a mechanistic antiproliferative study performed in the yeast Saccharomyces cerevisiae for several derivatives of three important natural naphthoquinones: lawsone, juglone, and beta-lapachone. We have found that (i) the free hydroxyl group of lawsone and juglone modulates toxicity; (ii) lawsone and juglone derivatives differ in their mechanisms of action, with ROS generation being more important for the former; and (iii) a subset of derivatives possess the capability to disrupt mitochondrial function, with beta-lapachones being the most potent compounds in this respect. In addition, we have cross-compared yeast results with antibacterial and antitumor activities. We discuss the relationship between the mechanistic findings, the antiproliferative activities, and the physicochemical properties of the naphthoquinones.
URI: http://hdl.handle.net/10553/42249
ISSN: 1554-8929
DOI: 10.1021/acschembio.8b00306
Fuente: ACS Chemical Biology [ISSN 1554-8929], v. 13 (8), p. 1950-1957
Colección:Artículos
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