1. Academic Validation
  2. 13,28-Epoxy triterpenoid saponins from Ardisia japonica selectively inhibit proliferation of liver cancer cells without affecting normal liver cells

13,28-Epoxy triterpenoid saponins from Ardisia japonica selectively inhibit proliferation of liver cancer cells without affecting normal liver cells

  • Bioorg Med Chem Lett. 2012 Oct 1;22(19):6120-5. doi: 10.1016/j.bmcl.2012.08.027.
Qin Li 1 Wei Li Lin-Ping Hui Chen-Yang Zhao Lin He Kazuo Koike
Affiliations

Affiliation

  • 1 Laboratory Center, The Fourth Affiliated Hospital, China Medical University, #4 Chongshan East Road, Shenyang 110032, PR China. qinli75@hotmail.com
Abstract

Twenty 13,28-epoxy and related triterpenoid saponins from Ardisia japonica were evaluated for their anti-proliferative activity on human liver Cancer cells and normal liver cells. Eight saponins selectively inhibited the growth of liver Cancer Bel-7402 and HepG-2 cells without affecting the survival of normal liver HL-7702 cells. The structure-activity relationship analyses indicated that the 13,28-epoxy, 16α-hydroxy, and C-30 methyl moieties in the sapogenin parts and the glycosyl moiety consisting from tetra- to hepta-saccharide units are important for this activity. Among the active saponins, ardisianoside B (2) and 3β-O-β-d-glucopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→2)-β-d-glucopyranosyl-(1→4)]-α-l-arabinopyranosyl-13β,28-epoxy-16α-hydroxyoleanane (3) showed the most potent anti-proliferative activity against Bel-7402 cells in a dose- and time-dependent manner. The selective anti-proliferative activity is attributed to the different cellular responses (CDKs and cyclins levels, cell cycle arrest and Apoptosis) between tumor and normal liver cells. Exposure to 2 and 3 selectively led to cell cycle arrest and Apoptosis in Bel-7402 cells together with the increased pro-apoptotic Caspase-8 and the decreased anti-apoptotic Cdc25A levels.

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