| Summary: | The plant <i>Zanthoxylum zanthoxyloides</i> (Lam.) Zepern. & Timler is one of the most important medicinal species of the genus <i>Zanthoxylum</i> on the African continent. It is used in the treatment and management of parasitic diseases in sub-Saharan Africa. These properties have inspired scientists to investigate species within the genus for bioactive compounds. However, a study, which details a spectroscopic, spectrometric and bioactivity guided extraction and isolation of antiparasitic compounds from the genus <i>Zanthoxylum</i> is currently non-existent. Tortozanthoxylamide (<b>1</b>), which is a derivative of the known compound armatamide was isolated from <i>Z. zanthoxyloides</i> and the full structure determined using UV, IR, 1D/2D-NMR and high-resolution liquid chromatography tandem mass spectrometry (HRESI-LC-MS) data. When tested against <i>Trypanosoma brucei</i> subsp. <i>brucei</i>, the parasite responsible for animal African trypanosomiasis in sub-Saharan Africa, <b>1</b> (IC<sub>50</sub> 7.78 µM) was just four times less active than the commercially available drug diminazene aceturate (IC<sub>50</sub> 1.88 µM). Diminazene aceturate is a potent drug for the treatment of animal African trypanosomiasis. Tortozanthoxylamide (<b>1</b>) exhibits a significant antitrypanosomal activity through remarkable alteration of the cell cycle in <i>T. brucei</i> subsp. <i>brucei</i>, but it is selectively non-toxic to mouse macrophages RAW 264.7 cell lines. This suggests that <b>1</b> may be considered as a scaffold for the further development of natural antitrypanosomal compounds.
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