Growth-inhibitory effects of tris-(1,10-phenanthroline) iron (II) against Mycobacterium tuberculosis in vitro and in vivo

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dc.contributor.authorSolcia, Mariana Cristina [UNESP]
dc.contributor.authorCampos, Débora Leite [UNESP]
dc.contributor.authorGrecco, Júlia Araújo [UNESP]
dc.contributor.authorPaiva Silva, Caio Sander [UNESP]
dc.contributor.authorBento da Silva, Patrícia [UNESP]
dc.contributor.authorCristiane da Silva, Isabel [UNESP]
dc.contributor.authorBalduino da Silva, Ana Paula [UNESP]
dc.contributor.authorSilva, Joás [UNESP]
dc.contributor.authorOda, Fernando Bombarda [UNESP]
dc.contributor.authorGonzaga dos Santos, André [UNESP]
dc.contributor.authorPavan, Fernando Rogério [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2021-06-25T11:00:32Z
dc.date.available2021-06-25T11:00:32Z
dc.date.issued2021-05-01
dc.description.abstractMycobacterium tuberculosis is the major etiological agent for tuberculosis (TB), which is the leading cause of single pathogen infection-related deaths worldwide. The End TB Strategy of the World Health Organization aimed to decrease the incidence of TB by 20% between 2015 and 2020, which was not achieved. Here, the growth-inhibitory effects of tris-(1,10-phenanthroline) iron (II) complex ([Fe(phen)3]2+), a known commercially available cheap chemical substance, were examined. The best in vitro results showed great activity with MIC ranging from 0.77 to 3.06 μM against clinical strains and at low pH (mimicking the granuloma) with MIC of 0.21 μM. Preliminary safety analysis revealed that the complex did not exhibit cytotoxic activity against different cell lines or mutagenic activity in vitro. The complex was orally bioavailable after 2 h of administration in vivo. Additionally, the results of the acute toxicity test revealed that the complex did not exert toxic effects in female BALB/c mice. The mechanism of action was performed using D29 mycobacteriophages where the treatment with different concentrations of the complex inhibited viral protein synthesis, which indicated that the anti-TB mechanisms of the complex involve protein synthesis inhibition. These findings suggested that [Fe(phen)3]2+ is a potential novel therapeutic for TB.en
dc.description.affiliationSão Paulo State University (UNESP) School of Pharmaceutical Sciences Tuberculosis Research Laboratory, Araraquara
dc.description.affiliationSão Paulo State University (UNESP) School of Pharmaceutical Sciences Department of Drugs and Medicines, Araraquara
dc.description.affiliationUnespSão Paulo State University (UNESP) School of Pharmaceutical Sciences Tuberculosis Research Laboratory, Araraquara
dc.description.affiliationUnespSão Paulo State University (UNESP) School of Pharmaceutical Sciences Department of Drugs and Medicines, Araraquara
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 2016/24633–0
dc.description.sponsorshipIdFAPESP: 2017/12419–7
dc.description.sponsorshipIdFAPESP: 2018/00163–0
dc.description.sponsorshipIdFAPESP: 2018/12135–1
dc.description.sponsorshipIdFAPESP: 2018/12270–6
dc.description.sponsorshipIdFAPESP: 2018/21778–3
dc.description.sponsorshipIdFAPESP: 2020/13497–4
dc.identifierhttp://dx.doi.org/10.1016/j.tube.2021.102087
dc.identifier.citationTuberculosis, v. 128.
dc.identifier.doi10.1016/j.tube.2021.102087
dc.identifier.issn1873-281X
dc.identifier.issn1472-9792
dc.identifier.scopus2-s2.0-85106287699
dc.identifier.urihttp://hdl.handle.net/11449/207757
dc.language.isoeng
dc.relation.ispartofTuberculosis
dc.sourceScopus
dc.subjectDrug repurposing
dc.subjectEfficacy
dc.subjectMycobacterium tuberculosis
dc.subjectSafety
dc.subjectTris-(1,10-phenanthroline) iron (II)
dc.titleGrowth-inhibitory effects of tris-(1,10-phenanthroline) iron (II) against Mycobacterium tuberculosis in vitro and in vivoen
dc.typeArtigo
unesp.author.orcid0000-0001-9617-9858[6]

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