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

BACKGROUND

Seeds of Annona squamosa L. have been used in the south of China as a folk remedy to treat "malignant sores" (cancer).

OBJECTIVE

To investigate the chemical constituents and the anti-tumor activity of the standardized A. squamosa seeds extract in vitro and in vivo.

METHODS

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.

RESULTS

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.

CONCLUSIONS

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.