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.
Xuewei Ye  1 ,  Siran Yu  1 ,  Ying Liang  1 ,  Haocai Huang  1 ,  Xiao-Yuan Lian  2 ,  Zhizhen Zhang  3
Affiliations
  • 1. Ocean College, Zhejiang University, Hangzhou 310058, China.
  • 2. College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. Electronic address: [email protected].
  • 3. Ocean College, Zhejiang University, Hangzhou 310058, China. Electronic address: [email protected].
PMID: 25442304 DOI: 10.1016/j.bmcl.2014.09.087
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.
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