Extracts from Hypericum brasiliense, a herb growing in the southern and southeastern part of Brazil, have pharmacological properties because the presence of known bioactive compounds. In this study bioactive substances from roots of H. brasiliense were isolated and identified as 1,5-dihydroxyxanthone, isouliginosin B and betulinic acid. The production of these substances by plants of H. brasiliense was then characterized in different developmental stages (vegetative, flowering and fructification), and in different parts (roots, shoot tips, internal upper part and internal lower part of the shoots). Quercetin and rutin were identified during the analysis of the shoots and their concentrations were also determined. 1,5-Dihydroxyxanthone was found in all plant parts and its concentration was high at fructification. Betulinic acid was more abundant during fructification, in the apices of the branches, probably because of the presence of fruits. Isouliginosin B, an acyl-phloroglucinol, rutin and quercetin were present in higher concentrations during the flowering stage. However, while rutin and quercetin accumulated more in the shoots, the acyl-phloroglucinol was exclusively detected in the roots. Considering the class of the substances, the highest concentration of phenolic compounds (1,5-dihydroxyxanthone, isouliginosin B, rutin and quercetin) was found during flowering, and terpenes (betulinic acid) during fructification. (C) 2004 Elsevier Ireland Ltd. All rights reserved.