Document Detail

Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: in silico, in vitro and in vivo activity studies.
MedLine Citation:
PMID:  18192088     Owner:  NLM     Status:  MEDLINE    
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.
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
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-11-19
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  43     ISSN:  0223-5234     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2008 Sep 
Date Detail:
Created Date:  2008-09-12     Completed Date:  2008-12-09     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  1797-807     Citation Subset:  IM    
Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Av.Gral. Flores 2124, CC 1157, Montevideo 11800, Uruguay.
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MeSH Terms
Antiprotozoal Agents / chemistry,  pharmacology*,  therapeutic use*
Bibenzyls / chemistry,  pharmacology*,  therapeutic use
Cell Line
Computational Biology*
Extracellular Space / drug effects
Inhibitory Concentration 50
Intracellular Space / drug effects
Leishmania / cytology,  drug effects*
Leishmaniasis / drug therapy
Phenols / chemistry,  pharmacology*,  therapeutic use
Trypanosoma cruzi / drug effects*
Reg. No./Substance:
0/14-hydroxylunularin; 0/Antiprotozoal Agents; 0/Bibenzyls; 0/Phenols

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