Selective cytotoxicity of ent‐kaurene diterpenoids isolated from Baccharis lateralis and Baccharis retusa (Asteraceae)

摘要: This study presents the cytotoxic activity evaluation of the natural diterpenes ent‐kaurenoic acid (1) and its 15β‐hydroxy (2), 15β‐senecioyloxy (3), and 15β‐tiglinoyloxy (4) derivatives, isolated from Brazilian native plants, Baccharis retusa and B. lateralis (Asteraceae). Using the MTT (3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) colorimetric assay, it was observed that compound 1 displayed in vitro activity towards the aggressive MDA‐MB‐231 adenocarcinoma cell line and reduced toxicity against MCF‐10A nontumorigenic epithelial cells, indicating expressive selectivity. On the contrary, compounds 2–4 exhibited reduced toxicity and selectivity in both tested cell lines. Based on the chemical structures of compounds 1–4, it is suggested that the presence of additional functional groups at the C‐15 position—a hydroxyl group in compound 2 and isomeric isoprene units in compounds 3 and 4 …