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Biological Activities of Violacein, a New Antitumoral Indole Derivative, in an Inclusion Complex with β-Cyclodextrin

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Abstract

Violacein is a poorly water-soluble antitumoraland antibacterial drug. The solubility can be enhanced by complexation withβ-cyclodextrin. The inclusion complex was prepared by the co-precipitation method in molarratios of 1 : 1 and 1 : 2 of violacein/β-cyclodextrin, respectively. The acutetoxicity (E. coli strain) of violacein did not changeup to 400 μM, either in thepresence or absence of cyclodextrin. Cytotoxicity (V-79 cellculture) through DNA and MTT assays was significantlydecreased in the presence of the 1 : 2 molar ratio complex.Studies on erythrocyte lipid peroxidation by the thiobarbituricacid (TBA) methodshowed that violacein and violacein/β-CD (1 : 2) at100 μM cause 50% and 80% inhibition, respectively. At 500 μM theviolacein/β-CD complexinhibited lipid peroxidation completely; however, withfree violacein only 65% inhibition was reached at that concentration.

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Authors and Affiliations

  1. Biological Chemistry Laboratory, Instituto de Química, Brazil

    Mariângela B. M. De Azevedo, Ana O. Souza, Daniel Rettori & Marcio A. Torsoni

  2. Organic Chemistry Department, Universidad de Concepción Concepcion, Chile

    Joel Alderete

  3. Instituto de Biologia, Biochemistry Department, Universidade Estadual de Campinas, C.P. 6154, CEP 13083-970, Campinas-S.P., Brazil

    Jaime A. Rodriguez

  4. Biochemistry Department, Universidade de São Paulo, S.P., Brazil

    Adelaide Faljoni-Alario

  5. Instituto de Biologia, Biochemistry Department, Universidade Estadual de Campinas, C.P. 6154, CEP 13083-970, Campinas-S.P., Brazil

    Marcela Haun

  6. Instituto de Química, Biological Chemistry Laboratory, Universidade Estadual de Campinas, C. P. 6154, CEP 13083-970, Campinas, Brazil

    Nelson Durân

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  1. Mariângela B. M. De Azevedo
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  2. Joel Alderete
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  3. Jaime A. Rodriguez
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  4. Ana O. Souza
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  5. Daniel Rettori
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  6. Marcio A. Torsoni
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  7. Adelaide Faljoni-Alario
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  8. Marcela Haun
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  9. Nelson Durân
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Correspondence to Nelson Durân.

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De Azevedo, M.B.M., Alderete, J., Rodriguez, J.A. et al. Biological Activities of Violacein, a New Antitumoral Indole Derivative, in an Inclusion Complex with β-Cyclodextrin. Journal of Inclusion Phenomena 37, 93–101 (2000). https://doi.org/10.1023/A:1008138807481

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