Ursolic acid is a natural compound, a pentacyclic triterpene, found in abundance in Many species of native wild flora. The experimental study was intended to extract ursolic acid from Calluna vulgaris, L. Hull, (Ericaceae) and its derivatization to obtain dipeptide compounds with potential biological activity. For this purpose, three dipeptides were used: alanyl-glycine, glycyl-leucine and leucyl-glycine. The biological activity of ursoloil-glycyl-leucine has been tested on several cancer cells lines, A2780, A431, HeLa and MCF-7.