| Summary: | Indolocarbazoles are a family of natural alkaloids characterized by their potent protein kinase and topoisomerase I inhibitory activity. Among them, staurosporine (<b>1</b>) has exhibited promising inhibitory activity against parasites. Based on new insights on the activity and mechanism of action of STS in <i>Acanthamoeba</i> parasites, this work reports the isolation, identification, and the anti-<i>Acanthamoeba</i> activity of the minor metabolites 7-oxostaurosporine (<b>2</b>), 4′-demethylamino-4′-oxostaurosporine (<b>3</b>), and streptocarbazole B (<b>4</b>), isolated from cultures of the mangrove strain <i>Streptomyces sanyensis.</i> A clear correlation between the antiparasitic activities and the structural elements and conformations of the indolocarbazoles <b>1</b>−<b>4</b> was observed. Also, the study reveals that 7-oxostaurosporine (<b>2</b>) affects membrane permeability and causes mitochondrial damages on trophozoites of <i>A. castellanii</i> Neff.
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