Analysis of Mitochondrial Function in Cell Membranes as Indicator of Tissue Vulnerability to Drugs in Humans
dc.contributor.author | Elexpe, Ane | |
dc.contributor.author | Sánchez-Sánchez, Laura | |
dc.contributor.author | Tolentino-Cortez, Tarson | |
dc.contributor.author | Astigarraga Arribas, Egoitz | |
dc.contributor.author | Torrecilla Sesma, María | |
dc.contributor.author | Barreda Gómez, Gabriel | |
dc.date.accessioned | 2022-05-30T09:50:22Z | |
dc.date.available | 2022-05-30T09:50:22Z | |
dc.date.issued | 2022-04-23 | |
dc.identifier.citation | Biomedicines 10(5) : (2022) // Article ID 980 | es_ES |
dc.identifier.issn | 2227-9059 | |
dc.identifier.uri | http://hdl.handle.net/10810/56786 | |
dc.description.abstract | Drug side effects are one of the main reasons for treatment withdrawal during clinical trials. Reactive oxygen species formation is involved in many of the drug side effects, mainly by interacting with the components of the cellular respiration. Thus, the early detection of these effects in the drug discovery process is a key aspect for the optimization of pharmacological research. To this end, the superoxide formation of a series of drugs and compounds with antidepressant, antipsychotic, anticholinergic, narcotic, and analgesic properties was evaluated in isolated bovine heart membranes and on cell membrane microarrays from a collection of human tissues, together with specific inhibitors of the mitochondrial electron transport chain. Fluphenazine and PB28 promoted similar effects to those of rotenone, but with lower potency, indicating a direct action on mitochondrial complex I. Moreover, nefazodone, a drug withdrawn from the market due to its mitochondrial hepatotoxic effects, evoked the highest superoxide formation in human liver cell membranes, suggesting the potential of this technology to anticipate adverse effects in preclinical phases. | es_ES |
dc.description.sponsorship | This work has been partially supported by a grant from the Ministry of Economy and Competitiveness (DIN2019-010902) and the Basque Government Department of Economic Development, Sustainability and Environment (Bikaintek program: 48-AF-W2-2019-00007). | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | MDPI | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | es_ES |
dc.rights.uri | http://creativecommons.org/licenses/by/3.0/es/ | |
dc.subject | microarray | es_ES |
dc.subject | superoxide | es_ES |
dc.subject | antipsychotic | es_ES |
dc.subject | mitochondria | es_ES |
dc.title | Analysis of Mitochondrial Function in Cell Membranes as Indicator of Tissue Vulnerability to Drugs in Humans | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.date.updated | 2022-05-27T13:36:51Z | |
dc.rights.holder | 2022 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 (https://creativecommons.org/licenses/by/4.0/). | es_ES |
dc.relation.publisherversion | https://www.mdpi.com/2227-9059/10/5/980/htm | es_ES |
dc.identifier.doi | 10.3390/biomedicines10050980 | |
dc.departamentoes | Farmacología | |
dc.departamentoeu | Farmakologia |
Files in this item
This item appears in the following Collection(s)
Except where otherwise noted, this item's license is described as 2022 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 (https://creativecommons.org/licenses/by/4.0/).