Cytotoxicity of Triptolide and Triptolide loaded polymeric micelles in vitro

Toxicol In Vitro. 2011 Dec;25(8):1557-67. doi: 10.1016/j.tiv.2011.05.020. Epub 2011 May 27.


Triptolide (TP), a diterpenoid triepoxide purified from the Chinese herb Tripterygium wilfordii Hook F is characterized by strong anti-tumor effects on various cancer cells. Except its anti-tumor effects, TP also shows multiple pharmacological side activities, such as anti-inflammatory, immune-suppressive and male anti-fertility. In order to reduce these side effects, especially the immuno-suppressive activity when used to cure cancer, a novel polymeric micelle system containing TP (TP-PM) was constructed. The immune-modulation effects of TP-PM have been evaluated by previous studies. In this study, we compared the cytotoxicity of TP and TP-PM on Jurkat and HT29 cells. Therefore, we determined the cell viability, membrane integrity, cell proliferation, apoptosis, and caspase 3/7 activity after exposure to TP and TP-PM. The results demonstrated that actually low concentrated TP and TP-PM could induce an inhibition of cell growth and proliferation as well as membrane damage in both tumor cell lines. TP and TP-PM induced apoptosis and caused activation of caspase 3/7 even at low concentrations. Both formulations destroyed the membrane of Jurkat cells, nevertheless, TP-PM showed stronger pernicious effects. In general, TP-PM induced in both tested cell lines stronger effects than TP. Therefore, polymeric micelles can be considered as promising carriers for TP in cancer therapy.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Alkylating / toxicity*
  • Apoptosis / drug effects
  • Caspase 3 / metabolism
  • Caspase 7 / metabolism
  • Cell Line
  • Cell Line, Tumor
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Diterpenes / toxicity*
  • Drug Carriers / toxicity*
  • Drugs, Chinese Herbal / toxicity
  • Epoxy Compounds / toxicity
  • Humans
  • Immunosuppressive Agents / toxicity*
  • L-Lactate Dehydrogenase / metabolism
  • Micelles
  • Phenanthrenes / toxicity*
  • Polyesters / toxicity*
  • Polyethylene Glycols / toxicity*


  • Antineoplastic Agents, Alkylating
  • Diterpenes
  • Drug Carriers
  • Drugs, Chinese Herbal
  • Epoxy Compounds
  • Immunosuppressive Agents
  • Micelles
  • Phenanthrenes
  • Polyesters
  • methoxy poly(ethylene glycol)-block-poly(lactic acid)
  • triptolide
  • Polyethylene Glycols
  • L-Lactate Dehydrogenase
  • Caspase 3
  • Caspase 7