Ethnopharmacologic relevance: The history of health benefits of Tagetes (Asteraceae) dates back at least to the 12 th century. Tagetes erecta, an important specie from this genus, was widely known for its traditional medicine. Different parts of T. erecta are used in folk medicine to cure various types of diseases. Aim of the study: Considering the lack of scientific studies of Tagetes, the present study was aimed to evaluate the chemical composition, antifungal activity of its essential oil against fungi responsible for human infections, as well as its cytotoxicity on HepG2 human liver carcinoma cell lines. Materials and methods: Clevenger-type was performed to hydrodistillate EOs and chemically analyzed by combination of GC and MS technique, followed by the evaluation of antifungal activity by using the broth microdilution method. The cytotoxicity was evaluated through MTT assay against HepG2 and expressed as IC 50. Results: One hundred and eleven compounds of the total EOs were identified from three parts (shoot, flower, and root). For the first time, more than 60 new compounds such as iso-bergapten, bergapten, (3)-thujanol acetate, sylvestrene, α-vetivone, tridecenol acetate, β-atlantol, and p-cymenene have been isolated from T. erecta. Among all yeasts, C. albicans was the most sensitive with MICs of 0.08, 0.04, 0.16 µL mL-1 for TES, TEF, and TER oil respectively. In addition, maximum apoptosis rate of up to 90% was observed for HepG2 cell line at concentrations ranging between 82 and 122 µg/ml, with IC 50 value from 11.58 µg mL-1 to 19.86 µg mL-1 Conclusion: The findings from this study showed that the chemical composition of T. erecta EO varies, depending on the geographical situation, extraction method, environmental factors, and plant