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Article

In Vitro and Computational Studies of Perezone and Perezone Angelate as Potential Anti-Glioblastoma Multiforme Agents

by
Maricarmen Hernández-Rodríguez
1,
Pablo I. Mendoza Sánchez
2,
Joel Martínez
3,
Martha E. Macías Pérez
4,
Erika Rosales Cruz
5,
Teresa Żołek
6,
Dorota Maciejewska
6,
René Miranda Ruvalcaba
2,
Elvia Mera Jiménez
1,* and
María I. Nicolás-Vázquez
2,*
1
Laboratorio de Cultivo Celular, Escuela Superior de Medicina, IPN, Salvador Díaz Mirón esq. Plan de San Luis s/n, Casco de Santo Tomas, Miguel Hidalgo, Ciudad de Mexico 11340, Mexico
2
Departamento de Ciencias Químicas, Facultad de Estudios Superiores Cuautitlán Campo 1, UNAM. Av. Primero de Mayo S/N, Sta María Guadalupe las Torres, Cuautitlán Izcalli 54740, Mexico
3
Facultad de Ciencias Químicas, Universidad Autónoma de San Luis Potosí, San Luis Potosí 78210, Mexico
4
Unidad de Investigación Biomédica de Zacatecas (UIBMZ) del Instituto Mexicano del Seguro Social (IMSS), Alameda Trinidad García de La Cadena 438_2436A436, Zacatecas Centro, Zacatecas 98000, Mexico
5
Laboratorio de Hematopatología, Escuela Nacional de Ciencias Biológicas, IPN, Prolongación de Carpio y, Calle Plan de Ayala s/n, Santo Tomás, Miguel Hidalgo, Ciudad de Mexico 11340, Mexico
6
Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Żwirki i Wigury 61, 02-091 Warszawa, Poland
*
Authors to whom correspondence should be addressed.
Molecules 2022, 27(5), 1565; https://doi.org/10.3390/molecules27051565
Submission received: 6 February 2022 / Revised: 22 February 2022 / Accepted: 23 February 2022 / Published: 26 February 2022
(This article belongs to the Special Issue Current Approaches of Medicinal Chemistry in Neurological and Psychiatric Diseases)
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Abstract

Glioblastoma multiforme (GBM) represents the most malignant type of astrocytoma, with a life expectancy of two years. It has been shown that Poly (ADP-ribose) polymerase 1 (PARP-1) protein is over-expressed in GBM cells, while its expression in healthy tissue is low. In addition, perezone, a phyto-compound, is a PARP-1 inhibitor with anti-neoplastic activity. As a consequence, in the present study, both in vitro and computational evaluations of perezone and its chemically related compound, perezone angelate, as anti-GBM agents were performed. Hence, the anti-proliferative assay showed that perezone angelate induces higher cytotoxicity in the GBM cell line (U373 IC50 = 6.44 μM) than perezone (U373 IC50 = 51.20 μM) by induction of apoptosis. In addition, perezone angelate showed low cytotoxic activity in rat glial cells (IC50 = 173.66 μM). PARP-1 inhibitory activity (IC50 = 5.25 μM) and oxidative stress induction by perezone angelate were corroborated employing in vitro studies. In the other hand, the performed docking studies allowed explaining the PARP-1 inhibitory activity of perezone angelate, and ADMET studies showed its probability to permeate cell membranes and the blood–brain barrier, which is an essential characteristic of drugs to treat neurological diseases. Finally, it is essential to highlight that the results confirm perezone angelate as a potential anti-GBM agent.
Keywords: phyto-compounds; computational studies; drug-likeness; anti-neoplastic activity; glioblastoma multiforme phyto-compounds; computational studies; drug-likeness; anti-neoplastic activity; glioblastoma multiforme
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MDPI and ACS Style

Hernández-Rodríguez, M.; Mendoza Sánchez, P.I.; Martínez, J.; Macías Pérez, M.E.; Rosales Cruz, E.; Żołek, T.; Maciejewska, D.; Miranda Ruvalcaba, R.; Mera Jiménez, E.; Nicolás-Vázquez, M.I. In Vitro and Computational Studies of Perezone and Perezone Angelate as Potential Anti-Glioblastoma Multiforme Agents. Molecules 2022, 27, 1565. https://doi.org/10.3390/molecules27051565

AMA Style

Hernández-Rodríguez M, Mendoza Sánchez PI, Martínez J, Macías Pérez ME, Rosales Cruz E, Żołek T, Maciejewska D, Miranda Ruvalcaba R, Mera Jiménez E, Nicolás-Vázquez MI. In Vitro and Computational Studies of Perezone and Perezone Angelate as Potential Anti-Glioblastoma Multiforme Agents. Molecules. 2022; 27(5):1565. https://doi.org/10.3390/molecules27051565

Chicago/Turabian Style

Hernández-Rodríguez, Maricarmen, Pablo I. Mendoza Sánchez, Joel Martínez, Martha E. Macías Pérez, Erika Rosales Cruz, Teresa Żołek, Dorota Maciejewska, René Miranda Ruvalcaba, Elvia Mera Jiménez, and María I. Nicolás-Vázquez. 2022. "In Vitro and Computational Studies of Perezone and Perezone Angelate as Potential Anti-Glioblastoma Multiforme Agents" Molecules 27, no. 5: 1565. https://doi.org/10.3390/molecules27051565

APA Style

Hernández-Rodríguez, M., Mendoza Sánchez, P. I., Martínez, J., Macías Pérez, M. E., Rosales Cruz, E., Żołek, T., Maciejewska, D., Miranda Ruvalcaba, R., Mera Jiménez, E., & Nicolás-Vázquez, M. I. (2022). In Vitro and Computational Studies of Perezone and Perezone Angelate as Potential Anti-Glioblastoma Multiforme Agents. Molecules, 27(5), 1565. https://doi.org/10.3390/molecules27051565

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