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

Overview

Journal Pharmaceutics

Publisher MDPI

Date 2022 Nov 11

PMID 36365097

Authors

Wilson Castrillon-Lopez

Angie Herrera-Ramirez

Gustavo Moreno-Quintero

Juan Carlos Coa

Tonny W Naranjo

Wilson Cardona-Galeano

Affiliations

Soon will be listed here.

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 and displayed the highest cytotoxic activity with IC values of = 6.5 ± 1.9 µM and 19.0 ± 1.4 µM, respectively, on SW480 cells. In addition, hybrid also exhibited activity on SW620 cells with an IC 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 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.

Citing Articles

Synthesis, Structural Properties and Biological Activities of Novel Hydrazones of 2-, 3-, 4-Iodobenzoic Acid.

Czyzewska I, Mazur L, Biernasiuk A, Hordyjewska A, Popiolek L Molecules. 2024; 29(16).

PMID: 39202893 PMC: 11356900. DOI: 10.3390/molecules29163814.

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