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TRIAZENOS: CLIVAGEM DO DNA, ATIVIDADE ANTIBACTERIANA E TOXICIDADE FRENTE À Artemia Salina LEACH. / TRIAZENES: DNA CLEAVAGE, ANTIBACTERIAL ACTIVITY AND TOXICITY FRONT TO Artemia Salina

In this work, six triazene compounds are assayed to DNA cleavage activity. The same six triazenes and the drug Asercit® (dacarbazine) are assayed to antibacterial activity and toxicity to Artemia salina Leach.: 1,3-bis-(phenyl)triazene-1-N-hidroxide (T1), 1-(4-bromophenyl)-3-(4-nitrophenyl)triazene, (T2), 1-(4-azophenyl)-3-(4-nitrophenyl)triazene (T3) ,1,3-bis-(4-azophenyl-triazene) (T4), 1,3-bis-(2-bromophenyl)triazene (T5), 1-(4-carboxyphenyl)-3-(4-azophenyl)triazene (T6) and 5-(3,3-dimethyl-1-triazenyl)imidazol-4-carboxamide (dacarbazine, Asercit®). Triazene T1 cleaves approximately 50 % of plasmid DNA (pBSKII and pUC18, 3.75 mM, 50ºC/24 hours, Tris.HCl buffer 200 mM pH 8.0). Hydroxyl radical scavengers (glycerol 0.1 and 1.0 %, DMSO 0.04 M and tiourea 0.04 M) and argon atmosphere not interfere in DNA cleavage by T1. The Kb of T1 determinated by spectrofotometric titrations with DNA are 4.50 x 101 M-1 (pH 6,5), 1.00 x 102 M-1 (pH 7,0) e 2.33 x 102 M-1 (pH 8,0). T1, T6 and Asercit® are the more actives in antibacterial activity with CIM/CBM of even 16/64 μg/ml. LC50 more lower determinated by toxicity to A. salina are to T1 (0.081 ± 0.008 μg/ml), T5 (0.076 ± 0.011 μg/ml) and T6 (0.077 ± 0.007 μg/ml). Theses studies show the wide biological activity conferred by triazene compounds. / Neste estudo, seis compostos triazenos são avaliados quanto à atividade de clivagem do DNA. Os mesmos seis triazenos e o medicamento Asercit® (dacarbazina) são avaliados quanto à atividade antibacteriana e toxicidade frente à Artemia salina Leach.: 1,3-bis-(fenil)triazeno-1-N-hidróxido (T1), 1-(4-bromofenil)-3- (4-nitrofenil)triazeno (T2), 1-(4-azofenil)-3-(4-nitrofenil)triazeno (T3), 1,3-bis-(4- azofenil)triazeno (T4), 1,3-bis-(2-bromofenil)triazeno (T5), 1-(4-carbóxifenil)-3-(4-
azofenil)triazeno (T6) e 5-(3,3-dimetil-1-triazenil)imidazol-4-carboxamida (dacarbazina, Asercit®). O triazeno T1 cliva aproximadamente 50 % do DNA plasmidial (pBSKII e pUC18, a 3,75 mM, 50 ºC/24 horas, tampão Tris.HCl 200 mM
pH 8,0). Seqüestradores de radicais hidroxil (glicerol 0,1 e 1 %, DMSO 0,04 M e tiouréia 0,04 M) e atmosfera de argônio não interferem na clivagem do DNA por T1. Os Kb de T1 determinados por titulação espectrofotométrica com DNA são 4,50 x 101 M-1 (pH 6,5), 1,00 x 102 M-1 (pH 7,0) e 2,33 x 102 M-1 (pH 8,0). T1, T6 e o Asercit® são os mais ativos na atividade antibacteriana com CIM/CBM de até 16/64 μg/ml. As
LC50 mais baixas determinadas pela toxicidade para A. salina são para T1 (0,081 ± 0,008 μg/ml), T5 (0,076 ± 0,011 μg/ml) e T6 (0,077 ± 0,007 μg/ml). Esses estudos mostram a ampla atividade biológica conferida pelos compostos triazenos.

Identiferoai:union.ndltd.org:IBICT/oai:repositorio.ufsm.br:1/5874
Date13 December 2007
CreatorsParaginski, Gustavo Luiz
ContributorsHorner, Rosmari, Manfron, Melânia Palermo, Hörner, Manfredo
PublisherUniversidade Federal de Santa Maria, Programa de Pós-Graduação em Ciências Farmacêuticas, UFSM, BR, Farmacologia
Source SetsIBICT Brazilian ETDs
LanguagePortuguese
Detected LanguageEnglish
Typeinfo:eu-repo/semantics/publishedVersion, info:eu-repo/semantics/masterThesis
Formatapplication/pdf
Sourcereponame:Repositório Institucional da UFSM, instname:Universidade Federal de Santa Maria, instacron:UFSM
Rightsinfo:eu-repo/semantics/openAccess
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