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Open AccessArticle
Exploring the Anticancer Potential of Phenolic nor-Triterpenes from Celastraceae Species
by
Carolina P. Reyes
Carolina P. Reyes 1
,
Alejandro Ardiles
Alejandro Ardiles 2
,
Laura Anaissi-Afonso
Laura Anaissi-Afonso 3,
Aday González-Bakker
Aday González-Bakker 4
,
José M. Padrón
José M. Padrón 4
,
Ignacio A. Jiménez
Ignacio A. Jiménez 5,
Félix Machín
Félix Machín 3,6,7,*
and
Isabel L. Bazzocchi
Isabel L. Bazzocchi 5,*
1
Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Bioquímica Microbiología, Biología Celular y Genética, Universidad de La Laguna, Av. Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain
2
Departamento de Ciencias Básicas, Facultad de Ciencias, Universidad Santo Tomás, Avenida Iquique, Antofagasta 3991, Chile
3
Unidad de Investigación, Hospital Universitario Ntra Sra de Candelaria, Ctra del Rosario 145, 38010 Santa Cruz de Tenerife, Spain
4
Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, Av. Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain
5
Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Universidad de La Laguna, Av. Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain
6
Instituto de Tecnologías Biomédicas, Universidad de La Laguna, 38200 La Laguna, Spain
7
Facultad de Ciencias de la Salud, Universidad Fernando Pessoa Canarias, 35450 Las Palmas de Gran Canaria, Spain
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2024, 25(17), 9470; https://doi.org/10.3390/ijms25179470 (registering DOI)
Submission received: 22 July 2024
/
Revised: 23 August 2024
/
Accepted: 28 August 2024
/
Published: 30 August 2024
Abstract
To explore new compounds with antitumour activity, fifteen phenolic nor-tripterpenes isolated from Celastraceae species, Maytenus jelskii, Maytenus cuzcoina, and Celastrus vulcanicola, have been studied. Their chemical structures were elucidated through spectroscopic and spectrometric techniques, resulting in the identification of three novel chemical compounds. Evaluation on human tumour cell lines (A549 and SW1573, non-small cell lung; HBL-100 and T-47D, breast; HeLa, cervix, and WiDr, colon) revealed that three compounds, named 6-oxo-pristimerol, demethyl-zeylasteral, and zeylasteral, exhibited significant activity (GI50 ranging from 0.45 to 8.6 µM) on at least five of the cell lines tested. Continuous live cell imaging identified apoptosis as the mode of action of selective cell killing in HeLa cells. Furthermore, their effect on a drug-sensitive Saccharomyces cerevisiae strain has been investigated to deepen on their mechanism of action. In dose-response growth curves, zeylasteral and 7α-hydroxy-blepharodol were markedly active. Additionally, halo assays were conducted to assess the involvement of oxidative stress and/or mitochondrial function in the anticancer profile, ruling out these modes of action for the active compounds. Finally, we also delve into the structure-activity relationship, providing insights into how the molecular structure of these compounds influences their biological activity. This comprehensive analysis enhances our understanding of the therapeutic potential of this triterpene type and underscores its relevance for further research in this field.
Share and Cite
MDPI and ACS Style
Reyes, C.P.; Ardiles, A.; Anaissi-Afonso, L.; González-Bakker, A.; Padrón, J.M.; Jiménez, I.A.; Machín, F.; Bazzocchi, I.L.
Exploring the Anticancer Potential of Phenolic nor-Triterpenes from Celastraceae Species. Int. J. Mol. Sci. 2024, 25, 9470.
https://doi.org/10.3390/ijms25179470
AMA Style
Reyes CP, Ardiles A, Anaissi-Afonso L, González-Bakker A, Padrón JM, Jiménez IA, Machín F, Bazzocchi IL.
Exploring the Anticancer Potential of Phenolic nor-Triterpenes from Celastraceae Species. International Journal of Molecular Sciences. 2024; 25(17):9470.
https://doi.org/10.3390/ijms25179470
Chicago/Turabian Style
Reyes, Carolina P., Alejandro Ardiles, Laura Anaissi-Afonso, Aday González-Bakker, José M. Padrón, Ignacio A. Jiménez, Félix Machín, and Isabel L. Bazzocchi.
2024. "Exploring the Anticancer Potential of Phenolic nor-Triterpenes from Celastraceae Species" International Journal of Molecular Sciences 25, no. 17: 9470.
https://doi.org/10.3390/ijms25179470
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