Three cytotoxic Annonaceous acetogenins from the seeds of Annona squamosa

Abstract Three new Annonaceous acetogenins, squamocin-IV ( 1 ), squamocin-V ( 2 ) and squamoxinone-E ( 3 ), together with seven other known Annonaceous acetogenins ( 4 – 10 ) were isolated from the seeds of Annona squamosa . The structures of all of the isolates were established and characterized through spectral and chemical methods. The new Annonaceous acetogenins 1–3 were evaluated for their cytotoxicity against the Hep-G2, SMMC-7721, BEL-7402, BGC-803 and H460 human cancer cell lines. Compound 3 exhibited the best cytotoxic activity, with IC 50 values of 0.103, 0.687, 4.19, 0.43 and 6.56 μg/mL, respectively for the cell lines above; meanwhile, Compound 1 showed selective cytotoxic activity against H460, with an IC 50 value of 0.049 μg/mL. The first mono-ACG ( 2 ) composed of 38 carbons was discovered.