Identification and evaluation of apoptotic compounds from Garcinia oligantha

Xue Mei Gao*, Ting Yu, Ming Zhu Cui, Jian Xin Pu, Xue Du, Simon Q B HAN, Qiu Fen Hu, Tian Cheng Liu, Kathy Qian Luo, Hong Xi Xu

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

33 Citations (Scopus)

Abstract

Four new compounds, oliganthins A-D (1-4), and one known caged xanthone gaudichaudione H (5) were isolated from the stems of Garcinia oligantha. The structures of the new compounds were elucidated by spectroscopic evidences. All of the five compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which have been genetically engineered to produce a fluorescent biosensor capable of detecting caspase-3 activation. All of them induced cell apoptosis at 10 μM or lower concentrations. The apoptotic activity of oliganthins A, B and gaudichaudione H were further confirmed by detecting the cleavage of PARP, which is the substrate of activated caspase-3, in these compounds-treated cells using the method of Western blot. Moreover, the values of IC 50 were measured for all five compounds on HeLa cells using the MTT assay. Among them, gaudichaudione H had the lowest IC 50 value of 0.90 μM, while the other four new compounds had IC 50 values of 1.58, 1.52, 4.15, and 7.82 μM, respectively. These results show that gaudichaudione H has the strongest apoptosis-inducing effect and cell growth inhibition effect among these xanthones and it may have the potential to be developed into a new anticancer agent.

Original languageEnglish
Pages (from-to)2350-2353
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number6
DOIs
Publication statusPublished - 15 Mar 2012

Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

User-Defined Keywords

  • Anticancer drug
  • Apoptosis
  • Caspase-3
  • Garcinia oligantha
  • Xanthone

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