Cytotoxic and antineoplastic activity of timosaponin A-III for human colon cancer cells

You Jin Kang, Hwa Jin Chung, Joo Won Nam, Hyen Joo Park, Eun Kyoung Seo, Yeong Shik Kim, Dongho Lee, Sang Kook Lee

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63 Citations (Scopus)

Abstract

The potential antitumor activity of timosaponin A-III (1), a steroidal saponin from the rhizomes of Anemarrhena asphodeloides, was investigated in human colorectal cancer HCT-15 cells both in cell culture and in an in vivo murine xenograft model. Compound 1 inhibited the proliferation of cancer cells with cell-cycle arrest and induction of apoptosis. Cell-cycle arrest in the G0/G1 and G2/M phase by 1 was correlated with the down-regulation of cyclin A, cyclin B1, cyclin-dependent kinase 2 (CDK2), CDK4, proliferating cell nuclear antigen, and c-Myc. The increase of the sub-G1 peak by 1 was also closely related to the induction of apoptosis, which was evidenced by the induction of DNA fragmentation, activation of caspases, induction of cleaved poly-(ADP ribose) polymerase, and suppression of Bcl-xL and Bcl-2 expression. In an in vivo xenograft model, treatment with 1 (2 or 5 mg/kg body weight, three times/week, ip administration) for four weeks significantly suppressed tumor growth in athymic nude mice bearing HCT-15 cells, without any overt toxicity. Cell-cycle arrest and induction of apoptosis might be plausible mechanisms of actions for the observed antineoplastic activity of 1.

Original languageEnglish
Pages (from-to)701-706
Number of pages6
JournalJournal of Natural Products
Volume74
Issue number4
DOIs
Publication statusPublished - 2011 Apr 25

ASJC Scopus subject areas

  • Complementary and alternative medicine
  • Molecular Medicine
  • Organic Chemistry
  • Analytical Chemistry
  • Pharmaceutical Science
  • Pharmacology
  • Drug Discovery

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  • Cite this

    Kang, Y. J., Chung, H. J., Nam, J. W., Park, H. J., Seo, E. K., Kim, Y. S., Lee, D., & Lee, S. K. (2011). Cytotoxic and antineoplastic activity of timosaponin A-III for human colon cancer cells. Journal of Natural Products, 74(4), 701-706. https://doi.org/10.1021/np1007735