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Cytotoxic and Apoptosis‐Inducing Properties of Auriculoside A in Tumor Cells

The C21‐steroidal glycoside auriculoside A (1), recently isolated from the roots of Cynanchum auriculatum, was found to inhibit the growth of several human tumor cell lines and to induce apoptosis in human breast cancer (MCF‐7) cells. Compound 1 was evaluated for its in vitro cytotoxicity against MCF‐7, HO‐8910, and Bel‐7402 cells, and for its in vivo antitumor effects on implanted sarcoma‐180 (S180) tumors in mice. It showed significant, concentration‐dependent inhibition of the cancer cells, both in vitro and in vivo. MCF‐7 Cells exposed to 1 displayed typical morphological apoptosis characteristics such as cytoplasm contraction and nuclear‐chromatin condensation. Flow‐cytometric analysis showed that the MCF‐7 cell cycle was arrested at the G0/G1 phase. When treated with 40 μg/ml of 1 for 24, 48, and 72 h, respectively, the apoptotic rates of the cells were ca. 5, 8, and 18.5%, respectively.