Seven xanthanolides, xanthinosin, xanthatin, 4-hydroxyxanthinosin, xanthinin, 4-epiisoxanthanol, 4-epixanthanol, 2-hydroxyxanthinosin and 4-oxobedfordia acid, were isolated from the fruits of Xanthium macrocarpum. A valuation of the antifungal activity of these xanthanolides against Candida albicans, Candida glabrata and Aspergillus fumigatus and of their antileishmanial activity against Leishmania infantum and Leishmania mexicana is presented.