Leaves of Anacardium humile are used in Brazilian traditional medicine for the treatment of intestinal disturbances and skin lesions. This study aimed to define leaf diagnostic structural characters, to propose a new method of phytochemical analysis of secretions, prospect flavonoids and alkaloids, and to evaluate their inhibitory activity on Candida albicans. Common anatomical, phytochemical, and microbiological methods were used. Leaves of Anacardium occidentale were used as a reference for the structural analyses. The main structural characters were closed vascular system, absence of ducts at the medulla, bilateral mesophyll, absence of bundle sheath extension, and secretory idioblasts at the xylem. The ducts present schizogenous origin, and secreting activity is restricted to the initial phases of leaf blade expansion. The proposed new phytochemical method is practical and inexpensive and has potential for wide application. The abundance of tannins and flavonoids is related to medicinal use. A single peak in high-performance liquid chromatography indicated the presence of a pure substance not previously reported. The extract had a strong inhibitory effect on C. albicans. The obtained results confirm the potential of A. humile for the prospection of new bioactive compounds.