Novel acylselenourea derivatives: dual molecules with anticancer and radical scavenging activity

Astráin-Redín, Nora; Raza, Asif; Encío Martínez, Ignacio; Sharma, Arun K.; Plano, Daniel; Sanmartín, Carmen

Novel acylselenourea derivatives: dual molecules with anticancer and radical scavenging activity

dc.contributor.author	Astráin-Redín, Nora
dc.contributor.author	Raza, Asif
dc.contributor.author	Encío Martínez, Ignacio
dc.contributor.author	Sharma, Arun K.
dc.contributor.author	Plano, Daniel
dc.contributor.author	Sanmartín, Carmen
dc.contributor.department	Ciencias de la Salud	es_ES
dc.contributor.department	Osasun Zientziak	eu
dc.date.accessioned	2023-10-17T17:12:52Z
dc.date.available	2023-10-17T17:12:52Z
dc.date.issued	2023
dc.date.updated	2023-10-17T16:55:04Z
dc.description.abstract	Oxidative stress surrounding cancer cells provides them with certain growth and survival advantages necessary for disease progression. In this context, Se-containing molecules have gained attention due to their anticancer and antioxidant activity. In our previous work, we synthesized a library of 39 selenoesters containing functional groups commonly present in natural products (NP), which showed potent anticancer activity, but did not demonstrate high radical scavenger activity. Thus, 20 novel Se derivatives resembling NP have been synthesized presenting acylselenourea functionality in their structures. Radical scavenger activity was tested using DPPH assay and in vitro protective effects against ROS-induced cell death caused by H2O2. Additionally, antiproliferative activity was evaluated in prostate, colon, lung, and breast cancer cell lines, along with their ability to induce apoptosis. Compounds 1.I and 5.I showed potent cytotoxicity against the tested cancer cell lines, along with high selectivity indexes and induction of caspase-mediated apoptosis. These compounds exhibited potent and concentration-dependent radical scavenging activity achieving DPPH inhibition similar to ascorbic acid and trolox. To conclude, we have demonstrated that the introduction of Se in the form of acylselenourea into small molecules provides strong radical scavengers in vitro and antiproliferative activity, which may lead to the development of promising dual compounds.	en
dc.description.sponsorship	Research was funded by PIUNA (refs 2018–2019), UNED-Caja Navarra Fundación La Caixa, and the Department of Pharmacology and Penn State Cancer Institute of the Penn State College of Medicine. N.A.-R. acknowledges the FPU program from the Spanish Ministry of Universities for a Ph.D. fellowship (FPU20/00175).	en
dc.format.mimetype	application/pdf	en
dc.format.mimetype	application/zip	en
dc.identifier.citation	Astrain-Redin, N., Raza, A., Encío, I., Sharma, A. K., Plano, D., Sanmartín, C. (2023) Novel acylselenourea derivatives: dual molecules with anticancer and radical scavenging activity. Antioxidants, 12(7), 1-23. https://doi.org/10.3390/antiox12071331.	en
dc.identifier.doi	10.3390/antiox12071331
dc.identifier.issn	2076-3921
dc.identifier.uri	https://academica-e.unavarra.es/handle/2454/46532
dc.language.iso	eng	en
dc.publisher	MDPI	en
dc.relation.ispartof	Antioxidants 2023, 12(7), 1331	en
dc.relation.publisherversion	https://doi.org/10.3390/antiox12071331
dc.rights	© 2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.	en
dc.rights.accessRights	info:eu-repo/semantics/openAccess
dc.rights.uri	https://creativecommons.org/licenses/by/4.0/
dc.subject	Acylselenourea	en
dc.subject	Antioxidant	en
dc.subject	Cancer	en
dc.subject	Garlic	en
dc.subject	Natural products	en
dc.subject	Selenium	en
dc.title	Novel acylselenourea derivatives: dual molecules with anticancer and radical scavenging activity	en
dc.type	info:eu-repo/semantics/article
dc.type.version	info:eu-repo/semantics/publishedVersion
dspace.entity.type	Publication
relation.isAuthorOfPublication	599ca381-1fd2-4a23-93ab-4373837eb6e0
relation.isAuthorOfPublication.latestForDiscovery	599ca381-1fd2-4a23-93ab-4373837eb6e0