Antileishmanial and Cytotoxic Activity of Synthetic Aromatic Monoterpens

ABSTRACT: The in vitro activity of synthetic monoterpens were evaluated against promastigotes and amastigotes of L. (V.) panamensis and compared to Glucantime®. Cytotoxic activity was determined against U-937 cells. Seven compounds showed low toxicity to U-937 cells (LC50 >100.0 μg/ml) and four of them were active against amastigotes form (EC50 <60.0 μg/ml). No correlation was found between promastigote and amastigote activities, suggesting again that the chemotherapeutic potential of anti-leishma-nial drugs depend on their action against amastigotes. The 3-isopropyl-2,5-dimethoxy-6-methyl-pheny-lamine (T6) compound was the most active showing activity at concentrations similar to those reached in serum by pentavalent antimonials (13.6 μg/ml) but the 5-isopropyl-4-methoxy-2-methyl-3-nitro-phenol (T4) compound was the most selective for Leishmania rather than mammal cells (SI = 8.7). This study concludes that monoterpen derivatives show promising antileishmanial potential and could be considered as new lead structures in the search for novel antileishmanial drugs.

• Autores: Osorio Durango, Edison; Arango Acosta, Gabriel Jaime; Jaramillo Pérez, Luz Marina; Muñoz Herrera, Diana Lorena; Velez, Iván Darío; Robledo, Sara Maria; Mora Arango, Cristina Lucía
• Tipo de recurso: Article of investigation
• Fecha de publicación: 2006
• Institución: Universidad de Antioquia
• Repositorio: Repositorio UdeA
• Idioma: eng
• OAI Identifier: oai:bibliotecadigital.udea.edu.co:10495/36200
• Acceso en línea: https://hdl.handle.net/10495/36200; http://www.latamjpharm.org/
• Palabra clave: Monoterpenos; Monoterpenes; Citotoxinas; Cytotoxins; Enfermedades Endémicas; Endemic Diseases; Leishmania; Leishmania
• Rights: openAccess
• License: https://creativecommons.org/licenses/by-nc-nd/4.0/