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Biological Effects in Cancer Cells of Mono- and Bidentate Conjugation of Cisplatin on PAMAM Dendrimers: A Comparative Study

2023Journal article Open access
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dc.contributor.authorCamacho, Cláudia
dc.contributor.authorMaciel, Dina
dc.contributor.authorTomás, Helena
dc.contributor.authorRodrigues, João
dc.date.accessioned2024-01-26T14:46:39Z
dc.date.available2024-01-26T14:46:39Z
dc.date.issued2023
dc.description.abstractCisplatin (cis-diamminedichloroplatinum(II)) is a potent chemotherapeutic agent com monly used to treat cancer. However, its use also leads to serious side effects, such as nephrotoxicity, ototoxicity, and cardiotoxicity, which limit the dose that can be safely administered to patients. To minimize these problems, dendrimers may be used as carriers for cisplatin through the coordination of their terminal functional groups to platinum. Here, cisplatin was conjugated to half-generation anionic PAMAM dendrimers in mono- and bidentate forms, and their biological effects were as sessed in vitro. After preparation and characterization of the metallodendrimers, their cytotoxicity was evaluated against several cancer cell lines (A2780, A2780cisR, MCF-7, and CACO-2 cells) and a non-cancer cell line (BJ cells). The results showed that all the metallodendrimers were cytotoxic and that the cytotoxicity level depended on the cell line and the type of coordination mode (mono- or bidentate). Although, in this study, a correlation between dendrimer generation (number of carried metallic fragments) and cytotoxicity could not be completely established, the monodentate coordina tion form of cisplatin resulted in lower IC50 values, thus revealing a more accessible cisplatin release from the dendritic scaffold. Moreover, most of the metallodendrimers were more potent than the cisplatin, especially for the A2780 and A2780cisR cell lines, which showed higher selectivity than for non-cancer cells (BJ cells). The monodentate G0.5COO(Pt(NH3 )2Cl)8 and G2.5COO(Pt(NH3 )2Cl)32 metallodendrimers, as well as the bidentate G2.5COO(Pt(NH3 )2 )16 metallodendrimer, were even more active towards the cisplatin-resistant cell line (A2780cisR cells) than the correspondent cisplatin sensitive one (A2780 cells). Finally, the effect of the metallodendrimers on the hemolysis of human erythrocytes was neglectable, and metallodendrimers’ interaction with calf thymus DNA seemed to be stronger than that of free cisplatin.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citation: Camacho, C.; Maciel, D.; Tomás, H.; Rodrigues, J. Biological Effects in Cancer Cells of Mono- and Bidentate Conjugation of Cisplatin on PAMAM Dendrimers: A Comparative Study. Pharmaceutics 2023, 15, 689. https://doi.org/10.3390/ pharmaceutics15020689pt_PT
dc.identifier.doi10.3390/pharmaceutics15020689pt_PT
dc.identifier.urihttp://hdl.handle.net/10400.13/5491
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationMadeira Chemistry Research Centre
dc.relationMadeira Chemistry Research Centre
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectCisplatinpt_PT
dc.subjectAnionic PAMAM dendrimerpt_PT
dc.subjectMonodentatept_PT
dc.subjectBidentatept_PT
dc.subjectAnticancerpt_PT
dc.subjectMetallodendrimerpt_PT
dc.subject.pt_PT
dc.subjectFaculdade de Ciências Exatas e da Engenhariapt_PT
dc.subjectCentro de Química da Madeira
dc.titleBiological Effects in Cancer Cells of Mono- and Bidentate Conjugation of Cisplatin on PAMAM Dendrimers: A Comparative Studypt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleMadeira Chemistry Research Centre
oaire.awardTitleMadeira Chemistry Research Centre
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F00674%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F00674%2F2020/PT
oaire.citation.issue2pt_PT
oaire.citation.startPage689pt_PT
oaire.citation.titlePharmaceuticspt_PT
oaire.citation.volume15pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
person.familyNameCamacho
person.familyNameMaciel
person.familyNameTomás
person.familyNameRodrigues
person.givenNameCláudia Sofia
person.givenNameDina
person.givenNameHelena
person.givenNameJoão
person.identifier556975
person.identifier.ciencia-id6C1E-7D62-56D1
person.identifier.ciencia-id211C-6048-FB1A
person.identifier.ciencia-id4D14-D31E-A8BE
person.identifier.ciencia-idA81C-620E-DD6A
person.identifier.orcid0000-0001-8684-6100
person.identifier.orcid0000-0002-7856-2041
person.identifier.orcid0000-0003-4552-1953
person.identifier.ridE-5991-2010
person.identifier.ridB-6816-2008
person.identifier.scopus-author-id54781586200
person.identifier.scopus-author-id6508104177
person.identifier.scopus-author-id9233278800
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
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