The infusion of the aerial parts of Gentianella multicaulis (Gillies ex Griseb.) Fabris (Gentianaceae), locally known as 'nencia', is used in San Juan Province, Argentina, as stomachic and as a bitter tonic against digestive and liver problems. The bioassay-guided isolation of G. multicaulis extracts and structural elucidation of the main compounds responsible for the antifungal and free radical scavenging activities were performed. The extracts had strong free radical scavenging effects in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay (45-93% at 10 microg/mL) and ferric-reducing antioxidant power (FRAP) assay at 200 microg/mL. Demethylbellidifolin (4) had high antioxidant activity in the DPPH and FRAP assay. The dermatophytes Microsporum gypseum, Trichophyton mentagrophytes, and T. rubrum were moderately inhibited by the different extracts (MIC values of 125-250 microg/mL). Demethylbellidifolin (4), bellidifolin (5), and isobellidifolin (6) showed an antifungal effect (MIC values of 50 microg/mL), while swerchirin (3) was less active with a MIC value of 100 microg/mL. In addition, oleanolic acid (1) and ursolic acid (2) were also isolated. These findings demonstrate that Gentianella multicaulis collected in the mountains of the Province of San Juan, Argentina, is an important source of compounds with antifungal and antioxidant activities.