RT Journal Article
T1 Evaluation of anticancer and anti-inflammatory activities of some synthetic rearranged abietanes
A1 Ait El Had, Mustapha
A1 Zentar, Houda
A1 Ruiz-Muñoz, Blanca
A1 Sainz, Juan
A1 Guardia, Juan J.
A1 Fernandez, Antonio
A1 Justicia, José
A1 Alvarez-Manzaneda, Enrique
A1 Reyes-Zurita, Fernando J.
A1 Chahboun, Rachid
K1 Cáncer - Tratamiento
AB Synthesis of the rearranged abietane diterpenes pygmaeocins C and D, viridoquinone,saprorthoquinone, and 1-deoxyviroxocine has been successfully achieved. The anticancer andanti-inflammatory activities of selected orthoquinonic compounds 5, 7, 13, and 19, as well as pygmaeocinC (17), were evaluated for the first time. The antitumor properties were assessed usingthree cancer cell lines: HT29 colon cancer cells, Hep G2 hepatocellular carcinoma cells, and B16-F10 murine melanoma cells. Compounds 5 and 13 showed the highest cytotoxicity in HT29 cells(IC50 = 6.69   1.2  g/mL and IC50 = 2.7   0.8  g/mL, respectively). Cytometric studies showedthat this growth inhibition involved phase S cell cycle arrest and apoptosis induction, possiblythrough the activation of the intrinsic apoptotic pathway. Morphological apoptotic changes, includingnuclear fragmentation and chromatin condensation, were also observed. Furthermore, theanti-inflammatory activity of these compounds was evaluated on the basis of their ability to inhibit nitricoxide production on the lipopolysaccharide activated RAW 264.7 macrophage cell line. Althoughall compounds showed high anti-inflammatory activity, with percentages between 40 and 100%, thehighest anti-inflammatory potential was obtained by pygmaeocin B (5) (IC50NO = 33.0   0.8 ng/mL).Our results suggest that due to their dual roles, this type of compound could represent a new strategy,contributing to the development of novel anticancer agents.
PB MDPI
YR 2023
FD 2023-09-01
LK https://hdl.handle.net/10630/28793
UL https://hdl.handle.net/10630/28793
LA eng
NO Had, M. A. E., Zentar, H., Ruiz-Muñoz, B., Sainz, J., Guardia, J. J., Fernández, A., Justicia, J., Alvarez‐Manzaneda, E., Reyes‐Zurita, F. J., & Chahboun, R. (2023). Evaluation of anticancer and Anti-Inflammatory activities of some synthetic rearranged abietanes. International Journal of Molecular Sciences, 24(17), 13583. https://doi.org/10.3390/ijms241713583
DS RIUMA. Repositorio Institucional de la Universidad de Málaga
RD 6 abr 2026