Anti-tumor activity of Annona squamosa seeds extract containing annonaceous acetogenin compounds

Seeds of Annona squamosa L. have been used in the south of China as a folk remedy to treat “malignant sores” (cancer). To investigate the chemical constituents and the anti-tumor activity of the standardized A. squamosa seeds extract in vitro and in vivo. Annonaceous acetogenin profiles of the standardized extract were determined by using Fourier transform infrared (FT-IR) and high performance liquid chromatography (HPLC) techniques. The anti-tumor activity of the extract was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) cytotoxicity in vitro and H 22 hepatoma cells transplantation tumor model in vivo. The FT-IR spectroscopy showed the presence of annonaceous acetogenin compounds in the extract. Two major annonaceous acetogenins: 12, 15- cis -squamostatin-A and bullatacin were identified and quantified by HPLC. The seed extract showed significant anti-tumor activity against four human tumor cell lines, especially for MCF-7 (IC 50. 0.25 μg/ml) and Hep G2 (IC 50. 0.36 μg/ml) cells in vitro. The extract inhibited the growth of H 22 tumor cells in mice with a maximum inhibitory rate of 69.55% by oral administration. A. squamosa seed extract showed significant anti-tumor activities against human hepatoma cells in vitro and in vivo, indicating a potential for developing the extract as a novel anti-liver cancer drug.