Small-molecule anthracene-induced cytotoxicity and induction of apoptosis through generation of reactive oxygen species

Rong Fu Chen, Chung Long Chou, Ming Ren Wang, Chieh Fu Chen, Jyh Fei Liao, Li Kang Ho, Chi Wei Tao, Hsu Shan Huang

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)


A series of anthracene derivatives have been synthesized, and their potential individual cytotoxicity was evaluated using Jurkat T cells and peripheral blood mononuclear cells (PBMCs) in vitro. These compounds, except for 2l, showed less cytotoxicity in PBMCs than mitoxantrone. We also analyzed the antiproliferative activity of these derivatives using the annexin V/propidium iodide assay. These synthetic compounds induced apoptosis, thus leading to antitumor effects. Compounds 2b, 2e, 2f, 2g, 2h, 2i, 2j, and mitoxantrone produced dose-dependent cytotoxicity, while the antiproliferative activity of the anthracene pharmacophore was retained in Jurkat T cells base on the detection of DNA degradation and membrane unpacking. These clearly indicate a correlation between cytotoxicity and antitumor activity. Unlike mitoxantrone, cytotoxic properties were observed, as documented by the reactivity of these novel compounds against Jurkat T cells and PBMCs as normal cells, respectively. Various concentrations of 2b, 2e, 2f, 2g, 2h, 2i, and 2j preparations also inhibited Jurkat T cell proliferation and induced apoptosis of Jurkat T cells, potentially confirmed through the detection of DNA degradation and membrane unpacking. In the present report we also investigated the antiinflammatory activity against phorbol-12-myristate-13-acetate induced superoxide anion production, a marker for an inflammatory mediator produced by neutrophils, with IC50 (μM) values of 2b, 2h, 2l, and 2o of 4.28±0.89, 3.31±0.88, 4.38±0.25, and 5.45±1.78, respectively. These results suggest that, in addition to the specific chromosomal aberrations and cell death, elevated apoptosis could also be a marker for exposure to anthracene derivatives.

Original languageEnglish
Pages (from-to)838-845
Number of pages8
JournalBiological and Pharmaceutical Bulletin
Issue number6
Publication statusPublished - Jun 2004
Externally publishedYes


  • Anthracene
  • Apoptosis
  • Flow cytometry
  • Jurkat T cell
  • Peripheral blood mononuclear cell
  • Propidium iodide

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)


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