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Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures

Indolocarbazoles are a family of natural alkaloids characterized by their potent protein kinase and topoisomerase I inhibitory activity. Among them, staurosporine (1) has exhibited promising inhibitory activity against parasites. Based on new insights on the activity and mechanism of action of STS i...

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Autores principales: Cartuche, Luis, Reyes-Batlle, María, Sifaoui, Ines, Arberas-Jiménez, Iñigo, Piñero, José E., Fernández, José J., Lorenzo-Morales, Jacob, Díaz-Marrero, Ana R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836125/
https://www.ncbi.nlm.nih.gov/pubmed/31627366
http://dx.doi.org/10.3390/md17100588
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author Cartuche, Luis
Reyes-Batlle, María
Sifaoui, Ines
Arberas-Jiménez, Iñigo
Piñero, José E.
Fernández, José J.
Lorenzo-Morales, Jacob
Díaz-Marrero, Ana R.
author_facet Cartuche, Luis
Reyes-Batlle, María
Sifaoui, Ines
Arberas-Jiménez, Iñigo
Piñero, José E.
Fernández, José J.
Lorenzo-Morales, Jacob
Díaz-Marrero, Ana R.
author_sort Cartuche, Luis
collection PubMed
description Indolocarbazoles are a family of natural alkaloids characterized by their potent protein kinase and topoisomerase I inhibitory activity. Among them, staurosporine (1) has exhibited promising inhibitory activity against parasites. Based on new insights on the activity and mechanism of action of STS in Acanthamoeba parasites, this work reports the isolation, identification, and the anti-Acanthamoeba activity of the minor metabolites 7-oxostaurosporine (2), 4′-demethylamino-4′-oxostaurosporine (3), and streptocarbazole B (4), isolated from cultures of the mangrove strain Streptomyces sanyensis. A clear correlation between the antiparasitic activities and the structural elements and conformations of the indolocarbazoles 1–4 was observed. Also, the study reveals that 7-oxostaurosporine (2) affects membrane permeability and causes mitochondrial damages on trophozoites of A. castellanii Neff.
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spelling pubmed-68361252019-11-25 Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures Cartuche, Luis Reyes-Batlle, María Sifaoui, Ines Arberas-Jiménez, Iñigo Piñero, José E. Fernández, José J. Lorenzo-Morales, Jacob Díaz-Marrero, Ana R. Mar Drugs Article Indolocarbazoles are a family of natural alkaloids characterized by their potent protein kinase and topoisomerase I inhibitory activity. Among them, staurosporine (1) has exhibited promising inhibitory activity against parasites. Based on new insights on the activity and mechanism of action of STS in Acanthamoeba parasites, this work reports the isolation, identification, and the anti-Acanthamoeba activity of the minor metabolites 7-oxostaurosporine (2), 4′-demethylamino-4′-oxostaurosporine (3), and streptocarbazole B (4), isolated from cultures of the mangrove strain Streptomyces sanyensis. A clear correlation between the antiparasitic activities and the structural elements and conformations of the indolocarbazoles 1–4 was observed. Also, the study reveals that 7-oxostaurosporine (2) affects membrane permeability and causes mitochondrial damages on trophozoites of A. castellanii Neff. MDPI 2019-10-17 /pmc/articles/PMC6836125/ /pubmed/31627366 http://dx.doi.org/10.3390/md17100588 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Cartuche, Luis
Reyes-Batlle, María
Sifaoui, Ines
Arberas-Jiménez, Iñigo
Piñero, José E.
Fernández, José J.
Lorenzo-Morales, Jacob
Díaz-Marrero, Ana R.
Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
title Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
title_full Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
title_fullStr Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
title_full_unstemmed Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
title_short Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
title_sort antiamoebic activities of indolocarbazole metabolites isolated from streptomyces sanyensis cultures
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836125/
https://www.ncbi.nlm.nih.gov/pubmed/31627366
http://dx.doi.org/10.3390/md17100588
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