Antileishmanial activity and cytotoxicity of ent-beyerene diterpenoids |
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| Authors: | Jilmar A. Murillo Juan F. Gil Yulieth A. Upegui Adriana M. Restrepo Sara M. Robledo Winston Quiñones Fernando Echeverri Aurelio San Martin Horacio F. Olivo Gustavo Escobar |
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| Affiliation: | 1. QOPN Grupo Química Orgánica de Productos Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia;2. PECET, Instituto de Investigaciones Médicas, Facultad de Medicina, Universidad de Antioquia, Calle 70 No. 52-21, Postal Code 0500100, Medellín, Colombia;3. Facultad de Ciencias, Universidad de Magallanes, Punta Arenas, Chile;4. Division of Medicinal and Natural Products Chemistry, The University of Iowa, Iowa City, IA 52242, USA |
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| Abstract: | We describe the in vitro activity of two natural isomeric ent-beyerene diterpenes, several derivatives and synthetic intermediates. Beyerenols 1 and 2 showed EC50 of 4.6?±?9.4 and 5.3?±?9.4?μg/mL against amastigotes of L. (V) brazilensis, with SI of 5.1 and 7.7, respectively. Beyerenol 1 was synthesized from stevioside. In vivo experiments with bereyenols showed cure in 50% of hamsters infected with L. (V) brazilensis topically applied as Cream I (beyerenol 1, 0.81%, w/w) and Cream III (beyerenol 2, 1.96%, w/w). These results suggest that beyerenols are potential candidates for cutaneous leishmaniasis chemotherapy by topical application. In vitro assays of amastigotes of L. (V) brazilensis showed EC50 of 1.1?±?0.1 and 1.3?±?0.04?μg/mL, with SI of 3.1 and 3.5 for hydrazone intermediates 10 and 11, respectively. |
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| Keywords: | Antileishmanial Semisynthesis Steviol |
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