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Article

Antikinetoplastid Activity of Indolocarbazoles from Streptomyces sanyensis

1
Instituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Universidad de La Laguna (ULL), Avda. Astrofísico F. Sánchez 2, 38206 La Laguna, Tenerife, Spain
2
Departamento de Química y Ciencias Exactas, Sección Química Básica y Aplicada, Universidad Técnica Particular de Loja (UTPL), San Cayetano alto s/n, A.P. 1101608, Loja, Ecuador
3
Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Departamento de Obstetricia y Ginecología, Pediatría, Medicina Preventiva y Salud Pública, Toxicología, Medicina Legal y Forense y Parasitología, Universidad de La Laguna, Avda. Astrofísico F. Sánchez s/n, 38206 La Laguna, Tenerife, Spain
4
Departamento de Química Orgánica, Universidad de La Laguna (ULL), Avda. Astrofísico F. Sánchez, 2, 38206 La Laguna, Tenerife, Spain
*
Authors to whom correspondence should be addressed.
L. Cartuche and I. Sifaoui contributed equally to this work.
Biomolecules 2020, 10(4), 657; https://doi.org/10.3390/biom10040657
Received: 18 February 2020 / Revised: 15 April 2020 / Accepted: 17 April 2020 / Published: 24 April 2020
(This article belongs to the Special Issue Bioactives from Marine Products)
Chagas disease and leishmaniasis are neglected tropical diseases caused by kinetoplastid parasites of Trypanosoma and Leishmania genera that affect poor and remote populations in developing countries. These parasites share similar complex life cycles and modes of infection. It has been demonstrated that the particular group of phosphorylating enzymes, protein kinases (PKs), are essential for the infective mechanisms and for parasite survival. The natural indolocarbazole staurosporine (STS, 1) has been extensively used as a PKC inhibitor and its antiparasitic effects described. In this research, we analyze the antikinetoplastid activities of three indolocarbazole (ICZs) alkaloids of the family of staurosporine STS, 24, and the commercial ICZs rebeccamycin (5), K252a (6), K252b (7), K252c (8), and arcyriaflavin A (9) in order to establish a plausive approach to the mode of action and to provide a preliminary qualitative structure–activity analysis. The most active compound was 7-oxostaurosporine (7OSTS, 2) that showed IC50 values of 3.58 ± 1.10; 0.56 ± 0.06 and 1.58 ± 0.52 µM against L. amazonensis; L. donovani and T. cruzi, and a Selectivity Index (CC50/IC50) of 52 against amastigotes of L. amazonensis compared to the J774A.1 cell line of mouse macrophages. View Full-Text
Keywords: Indolocarbazole; kinetoplastid; Streptomyces; leishmanicidal; trypanocidal Indolocarbazole; kinetoplastid; Streptomyces; leishmanicidal; trypanocidal
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MDPI and ACS Style

Cartuche, L.; Sifaoui, I.; López-Arencibia, A.; Bethencourt-Estrella, C.J.; San Nicolás-Hernández, D.; Lorenzo-Morales, J.; Piñero, J.E.; Díaz-Marrero, A.R.; Fernández, J.J. Antikinetoplastid Activity of Indolocarbazoles from Streptomyces sanyensis. Biomolecules 2020, 10, 657. https://doi.org/10.3390/biom10040657

AMA Style

Cartuche L, Sifaoui I, López-Arencibia A, Bethencourt-Estrella CJ, San Nicolás-Hernández D, Lorenzo-Morales J, Piñero JE, Díaz-Marrero AR, Fernández JJ. Antikinetoplastid Activity of Indolocarbazoles from Streptomyces sanyensis. Biomolecules. 2020; 10(4):657. https://doi.org/10.3390/biom10040657

Chicago/Turabian Style

Cartuche, Luis; Sifaoui, Ines; López-Arencibia, Atteneri; Bethencourt-Estrella, Carlos J.; San Nicolás-Hernández, Desirée; Lorenzo-Morales, Jacob; Piñero, José E.; Díaz-Marrero, Ana R.; Fernández, José J. 2020. "Antikinetoplastid Activity of Indolocarbazoles from Streptomyces sanyensis" Biomolecules 10, no. 4: 657. https://doi.org/10.3390/biom10040657

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