The therapeutic potential of Baccharis anomala DC. extracts was evaluated through its cytotoxic and antiproliferative effect and their phenotypic reversion property in activated hepatic stellate cells (HSCs). Baccharis anomala is distributed in Brazil (southeastern and south regions) and used for diuretic effect in folk medicine. Four fractions were obtained from the fractionation of the methanolic extract. Fractions III and IV decreased cell proliferation without increasing cell necrosis markers levels and induced cell cycle arrest in G1 phase. Fraction III induced phenotypic reversion through PPAR-gamma activation pathway, while fraction IV did not alter PPAR-alpha/gamma expression levels, suggesting that there is an independent PPAR-alpha/gamma pathway involved. Hydroxybenzoic, chlorogenic and coumaric acids were identified. Fractions III and IV showed antiproliferative effect and ability to induce reversion of activated phenotype of HSCs.