Bioorganic & Medicinal Chemistry 2009-07-01

Cytotoxic activity and inhibitory effect on nitric oxide production of triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae).

Rosa Tundis, Marco Bonesi, Brigitte Deguin, Monica R Loizzo, Federica Menichini, Filomena Conforti, François Tillequin, Francesco Menichini

Index: Bioorg. Med. Chem. 17 , 4542-7, (2009)

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Abstract

Three triterpene saponins isolated from the roots of Physospermum verticillatum and identified as saikosaponin a (1), buddlejasaponin IV (2), and songarosaponin D (3) were investigated in vitro for their cytotoxic activity against a panel of seven different cancer cell lines including ACHN, C32, Caco-2, COR-L23, A375, A549, and Huh-7D12 cell lines. The hydrolysis of sugar unit was performed on saikosaponin a (1) to obtain saikosapogenin a (4). All isolated saponins exhibited strong cytotoxic activity against COR-L23 cell line with IC(50) values ranged from 0.4 to 0.6 microM. A similar activity was recorded for saikogenin a (4). None of the tested compounds affected the proliferation of skin fibroblasts 142BR suggesting a selective action against cancer cells. Moreover, buddlejasaponin IV (2) and songarosaponin D (3) exerted significant inhibition of NO production in LPS induced RAW 264.7 macrophages with IC(50) of 4.2 and 10.4 microM, respectively.