1078718-89-4Relevant academic research and scientific papers
Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: In silico, in vitro and in vivo activity studies
Roldos, Virginia,Nakayama, Hector,Rolon, Miriam,Montero-Torres, Alina,Trucco, Fernando,Torres, Susana,Vega, Celeste,Marrero-Ponce, Yovanni,Heguaburu, Viviana,Yaluff, Gloria,Gomez-Barrio, Alicia,Sanabria, Luis,Ferreira, Maria Elena,Rojas de Arias, Antonieta,Pandolfi, Enrique
, p. 1797 - 1807 (2008)
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.
