Artificial Chemical Nuclease and Cytotoxic Activity of a Mononuclear Copper(I) Complex and a Related Binuclear Double‐Stranded Helicate. Issue 39 (30th September 2021)

• Record Type: Journal Article
• Authors: Levín, Pedro; Balsa, Lucía M.; Silva, Carlos P.; Herzog, Austin E.; Vega, Andrés; Pavez, Jorge; León, Ignacio E.; Lemus, Luis
• Is Part Of: European journal of inorganic chemistry. Issue 39(2021)
• Page Start: 4103
• Page End: 4112
• Publication Date: 2021-09-30
• Subjects: Anticancer activity -- Artificial nucleases -- Copper -- Hydroxyl radicals -- Structure elucidation; Chemistry, Inorganic -- Periodicals; Organometallic chemistry -- Periodicals; Bioinorganic chemistry -- Periodicals; Solid state chemistry -- Periodicals; 546
• DOI: 10.1002/ejic.202100673
• Languages: English
• ISSNs: 1434-1948

Abstract

Abstract: Copper complexes are promising candidates for anticancer drugs, because of their redox properties and the ability to generate ROS (reactive oxygen species) in the cellular media. Most of the reported complexes with anticancer properties are based on Cu(II), which must be reduced to Cu(I) to exert the therapeutic action. Here, we report on the synthesis and characterization of two novel copper(I) complexes, a mononuclear complex [Cu(L 1 )2 ](ClO4 ) (1) and a binuclear helicate [Cu2 (L 2 )2 ](ClO4 )2 (2) (L 1 =2‐ethoxy‐1, 10‐phenanthroline, L 2 =1, 2‐bis((1, 10‐phenanthrolin‐2‐yl)oxy)ethane), which were designed to be structurally comparable, in order to evaluate the effect of nuclearity on the artificial nuclease activity. The activity of helicate (2) was higher than that of the monometallic (1), and the DNA cleavage mechanism is through the generation of hydroxyl radical in a Fenton‐like reaction, which occurs after oxidation of Cu(I) by O2 . Also, helicate (2) showed a higher cytotoxic effect against different cancer cells lines, while both complexes are more active than cisplatin. Abstract : The role of the nuclearity and structure on the artificial nuclease activity of Cu(I) complexes is addressed by the study of a monometallic complex and a related bimetallic helicate. The nuclease activity of the helicate is much higher than the observed for the monometallic complex, and the same behavior is observed when the cytotoxicity against several cancer cells was evaluated.