N-Heterocyclic Carbene-Gold(I) Complexes Targeting Actin Polymerization

• Main Authors: Domenico Iacopetta, Jessica Ceramella, Camillo Rosano, Annaluisa Mariconda, Michele Pellegrino, Marco Sirignano, Carmela Saturnino, Alessia Catalano, Stefano Aquaro, Pasquale Longo, Maria Stefania Sinicropi
• Format: Article
• Language: English
• Published: MDPI AG 2021-06-01
• Series: Applied Sciences
• Subjects: NHC-gold complexes; actin; anticancer
• Online Access: https://www.mdpi.com/2076-3417/11/12/5626

Transition metal complexes are attracting attention because of their various chemical and biological properties. In particular, the NHC-gold complexes represent a productive field of research in medicinal chemistry, mostly as anticancer tools, displaying a broad range of targets. In addition to the already known biological targets, recently, an important activity in the organization of the cell cytoskeleton was discovered. In this paper, we demonstrated that two NHC-gold complexes (namely <b>AuL4</b> and <b>AuL7</b>) possessing good anticancer activity and multi-target properties, as stated in our previous studies, play a major role in regulating the actin polymerization, by the means of in silico and in vitro assays. Using immunofluorescence and direct enzymatic assays, we proved that both the complexes inhibited the actin polymerization reaction without promoting the depolymerization of actin filaments. Our outcomes may contribute toward deepening the knowledge of NHC-gold complexes, with the objective of producing more effective and safer drugs for treating cancer diseases.