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

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

Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine (2011-08-09)
Gabrieli L Parrilha, Rafael P Vieira, Paula P Campos, Grácia Divina F Silva, Lucienir P Duarte, Silvia P Andrade, Heloisa Beraldo
ZUSAMMENFASSUNG

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 BiCl(3) 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.

MATERIALIEN
Produktnummer
Marke
Produktbeschreibung

Sigma-Aldrich
Lapachol, 98%