Antituberculosis activity of alkylated mulinane diterpenoids |
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| Authors: | Gloria María Molina-Salinas Jorge Bórquez Salvador Said-Fernández Luis Alberto Loyola Alejandro Yam-Puc Pola Becerril-Montes Fabiola Escalante-Erosa Luis Manuel Peña-Rodríguez |
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| Institution: | 1. Grupo de Química Orgánica, Unidad de Biotecnología del Centro de Investigación Científica de Yucatán, Calle 43 No 130, Colonia Chuburná, Mérida, Yucatán, 97200 México;2. División de Biología Celular y Molecular, Centro de Investigación Biomédica del Noreste, Instituto Mexicano del Seguro Social, San Luis Potosí y Dos de Abril, Colonia Independencia, Monterrey, Nuevo León, 64720 México;3. Laboratorio de Productos Naturales, Departamento de Química, Facultad de Ciencias Básicas, Universidad de Antofagasta, Camino a Coloso S/N, Antofagasta, 02800 Chile |
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| Abstract: | Natural azorellane and mulinane diterpenoids show antituberculosis activity, which is increased by methylation of their free carboxyl group. We have systematically investigated the effect of alkylation in this class of diterpenoids and found that the profile of bioactivity is relatively unaffected by the introduction of short alkyl groups, both linear and branched. In this investigation, three semisynthetic diterpenoids, 13 hydroxy-mulin-11-en-20-oic acid n-propyl ester (3) and the n-propyl (19) and n-butyl (20) esters of isomulinic acid, showed the strongest antituberculosis activity (MIC = 6.25 μg/mL) against a drug-resistant strain of Mycobacterium tuberculosis. |
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| Keywords: | Azorella Mulinum Mulinane Alkyl esters Antituberculosis activity Mycobacterium tuberculosis |
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