Abstract
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.
Highlights
Indolocarbazoles (ICZs) are a large family of alkaloid natural compounds characterized by their protein kinase, tyrosine kinase, inhibitory activity
Streptomyces sanyensis PBLC04 strain was isolated from sediment samples collected in Jambelí mangrove at the southwest coast of Ecuador
Cultures of S. sanyensis were centrifuged, and the biomass pellet was extracted using a mixture of MeOH:EtOAc:Acetone (2:7:3)
Summary
Indolocarbazoles (ICZs) are a large family of alkaloid natural compounds characterized by their protein kinase, tyrosine kinase, inhibitory activity. These enzymes are responsible for regulating essential aspects of cell metabolism including cell cycle progression; ICZs exert potent cytotoxic effect on cancer cells [1,2,3]. ICZs have been isolated from several sources including bacteria, slime molds, cyanobacteria, and marine invertebrates [1]. The first isolated compound, staurosporine (STS), was obtained from a culture of a soil actinomycete (Streptomyces staurosporeus) in 1977 [4] at the Kitasato Institute
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