{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,2,21]],"date-time":"2025-02-21T20:29:29Z","timestamp":1740169769370,"version":"3.37.3"},"reference-count":28,"publisher":"Wiley","license":[{"start":{"date-parts":[[2017,1,1]],"date-time":"2017-01-01T00:00:00Z","timestamp":1483228800000},"content-version":"unspecified","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["BioMed Research International"],"published-print":{"date-parts":[[2017]]},"abstract":"<jats:p>The therapeutic options for Chagas disease are limited and its treatment presents a number of drawbacks including toxicity, drug resistance, and insufficient effectiveness against the chronic stage of the disease. Therefore, new therapeutical options are mandatory. In the present work, we evaluated the effect of a phenyl-<jats:italic>tert<\/jats:italic>-butylnitrone (PBN) derivate, LQB 123, against<jats:italic>Trypanosoma cruzi<\/jats:italic>forms. LQB 123 presented a trypanocidal effect against bloodstream trypomastigotes (IC<jats:sub>50<\/jats:sub>=<mml:math xmlns:mml=\"http:\/\/www.w3.org\/1998\/Math\/MathML\" id=\"M1\"><mml:mn fontstyle=\"italic\">259.4<\/mml:mn><mml:mo>\u00b1<\/mml:mo><mml:mn fontstyle=\"italic\">6.1<\/mml:mn><\/mml:math>\u2009<jats:italic>\u03bc<\/jats:italic>M) and intracellular amastigotes infecting peritoneal macrophages (IC<jats:sub>50<\/jats:sub>=<mml:math xmlns:mml=\"http:\/\/www.w3.org\/1998\/Math\/MathML\" id=\"M2\"><mml:mn fontstyle=\"italic\">188.2<\/mml:mn><mml:mo>\u00b1<\/mml:mo><mml:mn fontstyle=\"italic\">47.5<\/mml:mn><\/mml:math>\u2009<jats:italic>\u03bc<\/jats:italic>M), with no harmful effects upon the mammalian cells (CC<jats:sub>50<\/jats:sub>values greater than 4\u2009mM), resulting in a high selectivity index (CC<jats:sub>50<\/jats:sub>\/IC<jats:sub>50<\/jats:sub>&gt; 20). Additionally, metacyclic trypomastigotes submitted to LQB 123 presented an IC<jats:sub>50<\/jats:sub>of about<mml:math xmlns:mml=\"http:\/\/www.w3.org\/1998\/Math\/MathML\" id=\"M3\"><mml:mn fontstyle=\"italic\">191.8<\/mml:mn><mml:mo>\u00b1<\/mml:mo><mml:mn fontstyle=\"italic\">10.5<\/mml:mn><\/mml:math>\u2009<jats:italic>\u03bc<\/jats:italic>M and epimastigotes forms incubated with different concentrations of LQB 123 presented an inhibition of parasite growth with an IC<jats:sub>50<\/jats:sub>of<mml:math xmlns:mml=\"http:\/\/www.w3.org\/1998\/Math\/MathML\" id=\"M4\"><mml:mn fontstyle=\"italic\">255.1<\/mml:mn><mml:mo>\u00b1<\/mml:mo><mml:mn fontstyle=\"italic\">3.6<\/mml:mn><\/mml:math>\u2009<jats:italic>\u03bc<\/jats:italic>M. Finally, we investigated the mutagenic potential of the nitrone by the<jats:italic>Salmonella<\/jats:italic>\/microsome assay and observed no induction of mutagenicity even in concentrations as high as 33000\u2009<jats:italic>\u03bc<\/jats:italic>M. Taken together, these results present a nonmutagenic compound, with trypanocidal activity against all relevant forms of<jats:italic>T. cruzi<\/jats:italic>, offering new insights into CD treatment suggesting additional in vivo tests.<\/jats:p>","DOI":"10.1155\/2017\/2483652","type":"journal-article","created":{"date-parts":[[2017,2,16]],"date-time":"2017-02-16T02:03:21Z","timestamp":1487210601000},"page":"1-8","source":"Crossref","is-referenced-by-count":1,"title":["Mutagenic and Cytotoxicity LQB 123 Profile: Safety and Tripanocidal Effect of a Phenyl-t-Butylnitrone Derivative"],"prefix":"10.1155","volume":"2017","author":[{"given":"Mauricio Peixoto","family":"Cupello","sequence":"first","affiliation":[{"name":"Laborat\u00f3rio de Intera\u00e7\u00e3o Tripanossomat\u00eddeos e Vetores, Departamento de Bioqu\u00edmica, Instituto de Biologia Roberto Alcantara Gomes, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ, Brazil"},{"name":"Unidade de Desenvolvimento Tecnol\u00f3gico (UDT) de Triagem de Compostos Qu\u00edmicos para Doen\u00e7as Negligenciadas com \u00canfase Farmacol\u00f3gica contra a Doen\u00e7a de Chagas, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Francis Monique","family":"Saraiva","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de Intera\u00e7\u00e3o Tripanossomat\u00eddeos e Vetores, Departamento de Bioqu\u00edmica, Instituto de Biologia Roberto Alcantara Gomes, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ, Brazil"},{"name":"Unidade de Desenvolvimento Tecnol\u00f3gico (UDT) de Triagem de Compostos Qu\u00edmicos para Doen\u00e7as Negligenciadas com \u00canfase Farmacol\u00f3gica contra a Doen\u00e7a de Chagas, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ, 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