Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: In silico, in vitro and in vivo activity studies

Virginia Roldos, Hector Nakayama, Miriam Rolón, Alina Montero-Torres, Fernando Trucco, Susana Torres, Celeste Vega, Yovanni Marrero-Ponce, Viviana Heguaburu, Gloria Yaluff, Alicia Gómez-Barrio, Luis Sanabria, Maria Elena Ferreira, Antonieta Rojas de Arias, Enrique Pandolfi

Producción científica: Contribución a una revistaArtículorevisión exhaustiva

73 Citas (Scopus)

Resumen

The synthesis and potent antiprotozoal activity of 14-hydroxylunularin, a natural hydroxybibenzyl bryophyte constituent is reported. 14-Hydroxylunularin was highly active in vitro assays against culture and intracellular forms of Leishmania spp. and Trypanosoma. cruzi, in absence of cytotoxicity against mammalian cells. Preliminary structure-activity relationship studies showed that the reported bioactivity depends on hybridization at the carbon-carbon bridge, position and number of free hydroxy group on the aromatic rings. The reported results were also in agreement with the in silico prediction using Non-Stochastic Quadratic Fingerprints-based algorithms. The same compound also showed antiprotozoal activity in Leishmania spp. infected mice by oral and subcutaneous administration routes, with an optimal treatment of a daily subcutaneous administration of 10 mg/kg of body weight for 15 days. This study suggested that 14-hydroxylunularin may be chosen as a new candidate in the development of leishmanicidal therapy.

Idioma originalInglés
Páginas (desde-hasta)1797-1807
Número de páginas11
PublicaciónEuropean Journal of Medicinal Chemistry
Volumen43
N.º9
DOI
EstadoPublicada - sep. 2008
Publicado de forma externa

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