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Coordination of lapachol to bismuth(III) improves its anti-inflammatory and anti-angiogenic activities

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Abstract

Complex [Bi(Lp)2]Cl was obtained with 4-hydroxy-3-(3-methylbut-2-enyl)naphthalene-1,2-dione, “lapachol” (HLp). Lapachol, [Bi(Lp)2]Cl and BiCl3 were evaluated in a murine model of inflammatory angiogenesis induced by subcutaneous implantation of polyether polyurethane sponge discs. Intraperitoneal (i.p.) administration of lapachol or [Bi(Lp)2]Cl reduced the hemoglobin content in the implants suggesting that reduction of neo-vascularization was caused by lapachol. In the per os treatment only [Bi(Lp)2]Cl decreased the hemoglobin content in the implants. Likewise, N-acetylglucosaminidase (NAG) activity decreased in the implants of the groups i.p. treated with lapachol and [Bi(Lp)2]Cl while in the per os treatment inhibition was observed only for [Bi(Lp)2]Cl. Histological analysis showed that the components of the fibro-vascular tissue (vascularization and inflammatory cell population) were decreased in lapachol- and complex-treated groups. Our results suggest that both lapachol and [Bi(Lp)2]Cl exhibit anti-angiogenic and anti-inflammatory activities which have been attributed to the presence of the lapachol ligand. However, coordination to bismuth(III) could be an interesting strategy for improvement of lapachol’s therapeutic properties.

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Acknowledgment

This work was supported by CNPq and INCT-INOFAR (Proc. CNPq 573.364/2008-6).

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Authors and Affiliations

  1. Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, 31270-901, Brazil

    Gabrieli L. Parrilha, Rafael P. Vieira, Grácia Divina F. Silva, Lucienir P. Duarte & Heloisa Beraldo

  2. Departamento de Fisiologia e Biofísica Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, 31270-901, Brazil

    Paula P. Campos & Silvia P. Andrade

Authors
  1. Gabrieli L. Parrilha
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  2. Rafael P. Vieira
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  3. Paula P. Campos
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  4. Grácia Divina F. Silva
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  5. Lucienir P. Duarte
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  6. Silvia P. Andrade
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  7. Heloisa Beraldo
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Correspondence to Silvia P. Andrade or Heloisa Beraldo.

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Parrilha, G.L., Vieira, R.P., Campos, P.P. et al. Coordination of lapachol to bismuth(III) improves its anti-inflammatory and anti-angiogenic activities. Biometals 25, 55–62 (2012). https://doi.org/10.1007/s10534-011-9481-y

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  • DOI: https://doi.org/10.1007/s10534-011-9481-y

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