Cytotoxic aryltetralin lignans and sesquiterpene lactones from the flowers of Tithonia diversifolia
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https://doi.org/10.15625/2525-2518/22395Keywords:
Tithonia diversifolia, aryltetralin lignan, sesquiterpene lactone, cytotoxicityAbstract
Tithonia diversifolia (Hemsl.) A. Gray has been utilized traditionally to treat various diseases, including cancer, acne, acute enteritis, and gastritis. The ethyl acetate extract derived from the flowers of this plant demonstrated potent cytotoxic activity against KB cells, exhibiting 96 % inhibition at a concentration of 1 µg/mL. As a result, phytochemical investigation of the flower extract of Tithonia diversifolia led to the isolation of two lignans (1–2) and six sesquiterpene lactones (3–8). Their chemical structures were identified as cleiseberharside A (1), cleisindoside A (2), tirotundin (3), 2β-methoxydesoxytagitinin B (4), tagitinin C (5), 1β,2α-epoxytagitinin C (6), tagitinin G (7), and tagitinin H (8) by the spectroscopic analyses, including ESI-MS, 1D, and 2D NMR spectra, and comparison with the literature data. Notably, compounds 1 and 2 were discovered from the Tithonia genus for the first time. Compounds 3-6 displayed significant cytotoxicity against KB, MCF7, HepG2, and A549 cell lines, with IC50 values ranging from 0.28 to 3.76 µM. Especially, tagitinin C (5) exhibited the strongest cytotoxic effect against all four tested human cancer cell lines (KB, MCF7, HepG2, A549), with IC50 values of 0.28, 1.18, 1.38, and 1.15 µM, respectively, comparable to the reference compound ellipticine.
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