Abstract 1974: Growth inhibition and antitumor activity of chikusetsusaponin IVa methyl ester, an oleanane-type triterpenoid from the root of Acyranthes japonica, in HCT 116 human colon cancer cells

Abstract

Abstract Chikusetsusaponin IVa methyl ester (CSME) is an oleanane-type triterpenoid isolated from the root of Acyranthes japonica (Amaranthaceae). In the present study, the growth inhibition and antitumor activity of CSME were investigated in cultured human colon cancer cell HCT 116. CSME inhibited the proliferation of cancer cells with an IC50 value of 22.4 μM. Flow cytometric analysis indicated that CSME markedly induced the accumulation of cells in the G0/G1 phase and the increase of cell population in sub-G1 phase. G0/G1 cell cycle arrest by CSME was associated with the down-regulation of the expression of cyclin D1, cyclin A, CDK4, CDK2, c-myc and Rb phosphorylation. The increase of sub-G1 peak by CSME was closely correlated with the induction of apoptosis, which was evidenced by the induction of cleaved poly-(ADP ribose) polymerase, activation of caspases, and suppression of Bid and Bcl-2 expression. Treatment of CSME (0.25, 1.0, or 3.0 mg/kg, i.p) also effectively suppressed tumor growth in the HCT 116 implanted xenograft nude mouse model without any overt toxicity. Taken together, these findings suggest that CSME might be a potential candidate for the development of cancer chemotherapeutic agents derived from natural products. (Acknowledgement; this study was supported by a grant Studies on the Identification of the Efficacy of Biologically Active Components from Oriental Herbal Medicines from the Korea Food and Drug Administration (2010)). Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 1974. doi:1538-7445.AM2012-1974