Bioactive triterpenoid saponins and phenolic compounds against glioma cells

Bioorg Med Chem Lett. 2014 Nov 15;24(22):5157-63. doi: 10.1016/j.bmcl.2014.09.087. Epub 2014 Oct 5.

Abstract

A total of 54 natural origin compounds were evaluated for their activity in inhibiting the proliferation of glioma cells. Results showed that four Aesculus polyhydroxylated triterpenoid saponins (3-6), six Gleditsia triterpenoid saponins (7-12), and five phenolic compounds (43-46, 51) had dose-dependent activity suppressing the proliferation of both C6 and U251 cells. Structure-activity relationship analysis suggested that the acetyl group at C-28 for the Aesculus saponins and the monoterpenic acid moiety for the Gleditsia saponins could be critical for the activity of these active compounds. Aesculioside H (4), gleditsioside A (7), and feuric acid 3,4-dihydroxyphenethyl ester (FADPE, 46) were the three most active compounds from the different types of the active compounds and induced apoptosis and necrosis in glioma cells.

Keywords: Inhibition of glioma cell proliferation; Phenolic compounds; Triterpenoid saponins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cell Survival / physiology
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor / methods
  • Glioma*
  • Humans
  • Phenols / chemistry
  • Phenols / isolation & purification
  • Phenols / pharmacology*
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Rats
  • Saponins / chemistry
  • Saponins / isolation & purification
  • Saponins / pharmacology*
  • Structure-Activity Relationship
  • Triterpenes / chemistry
  • Triterpenes / isolation & purification
  • Triterpenes / pharmacology*

Substances

  • Phenols
  • Plant Extracts
  • Saponins
  • Triterpenes