Gallic Acid: A Natural Phenolic Compound Exerting Antitumoral Activities in Colorectal Cancer via Interaction with G-Quadruplexes
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Sánchez Martín, Victoria; Plaza Calonge, María del Carmen; Soriano Lerma, Ana del Carmen; Ortiz González, Matilde; Linde Rodríguez, Ángel; Pérez Carrasco, Virginia; Ramírez Macías, Inmaculada; Cuadros Celorrio, Marta Eugenia; Gutiérrez Fernández, José; Murciano Calles, Javier; Rodríguez Manzaneque, Juan Carlos; Soriano, Miguel; García Salcedo, José AntonioEditorial
MDPI
Materia
G-quadruplex Phenol Gallic acid Cancer Colorectal cancer
Date
2022-05-26Referencia bibliográfica
Sanchez-Martin, V... [et al.]. Gallic Acid: A Natural Phenolic Compound Exerting Antitumoral Activities in Colorectal Cancer via Interaction with G-Quadruplexes. Cancers 2022, 14, 2648. [https://doi.org/10.3390/cancers14112648]
Sponsorship
Instituto de Salud Carlos III; European Commission PI21/00497 AC18/00008; Next generation EU, Plan de Recuperacion Transformacion y Resiliencia, Agencia Estatal de Investigacion PLEC2021-008094; Ministerio de Ciencia e Innovacion from Government of Spain PID2019-104416RB-I00 PID2020-120481RB-I00; Ministerio de Universidades from Government of Spain FPU16/05822 FPU17/05413 FPU20/03952; University of Almeria FPI-201102Abstract
Natural phenolic compounds have gained momentum for the prevention and treatment
of cancer, but their antitumoral mechanism of action is not yet well understood. In the present
study, we screened the antitumoral potential of several phenolic compounds in a cellular model of
colorectal cancer (CRC).We selected gallic acid (GA) as a candidate in terms of potency and selectivity
and extensively evaluated its biological activity. We report on the role of GA as a ligand of DNA
G-quadruplexes (G4s), explaining several of its antitumoral effects, including the transcriptional
inhibition of ribosomal and CMYC genes. In addition, GA shared with other established G4 ligands
some effects such as cell cycle arrest, nucleolar stress, and induction of DNA damage. We further
confirmed the antitumoral and G4-stabilizing properties of GA using a xenograft model of CRC.
Finally, we succinctly demonstrate that GA could be explored as a therapeutic agent in a patient
cohort with CRC. Our work reveals that GA, a natural bioactive compound present in the diet, affects
gene expression by interaction with G4s both in vitro and in vivo and paves the way towards G4s
targeting with phenolic compounds.