Resveratrol/Hydrazone Hybrids: Synthesis and Chemopreventive Activity against Colorectal Cancer Cells

ABSTRACT: A series of resveratrol/hydrazone hybrids were obtained and elucidated by spectroscopic analysis. All compounds were evaluated against colorectal cancer cells (SW480 and Sw620) and nonmalignant cell lines (HaCaT and CHO-K1) to establish the selectivity index. Among the hybrids evaluated, compounds 6e and 7 displayed the highest cytotoxic activity with IC50 values of = 6.5 ± 1.9 µM and 19.0 ± 1.4 µM, respectively, on SW480 cells. In addition, hybrid 7 also exhibited activity on SW620 cells with an IC50 value of 38.41 ± 3.3 µM. Both compounds were even more toxic against these malignant cells in comparison to the nonmalignant ones, as evidenced by higher selectivity indices 48 h after treatment. These compounds displayed better activity and selectivity than parental compounds (PIH and Resveratrol) and the reference drug (5-FU). In addition, it was observed that both compounds caused antiproliferative activity probably exerted by cell cycle arrest at the G2/M or G0/G1 phases, with the formation of cells in the subG0/G1 phase. Furthermore, it was noticed that compound 7 induced mitochondrial depolarization in SW480 cells and positive staining for propidium iodide in both cancer cell lines, suggesting cell membrane damage involving either apoptosis or other processes of death.

• Autores: Castrillón López, Wilson Andrés; Herrera Ramírez, Angie; Moreno Quintero, Gustavo Alberto; Coa Acuña, Juan Carlos; Cardona Galeano, Wilson; Tonny Williams, Naranjo Preciado
• Tipo de recurso: Article of investigation
• Fecha de publicación: 2022
• Institución: Universidad de Antioquia
• Repositorio: Repositorio UdeA
• Idioma: eng
• OAI Identifier: oai:bibliotecadigital.udea.edu.co:10495/41405
• Acceso en línea: https://hdl.handle.net/10495/41405
• Palabra clave: Neoplasias Colorrectales; Colorectal Neoplasms; Resveratrol; Hydrazones; Hidrazonas; Apoptosis; https://id.nlm.nih.gov/mesh/D015179; https://id.nlm.nih.gov/mesh/D000077185; https://id.nlm.nih.gov/mesh/D006835; https://id.nlm.nih.gov/mesh/D017209
• Rights: openAccess
• License: http://creativecommons.org/licenses/by/2.5/co/