Artemisinin: an alternative treatment for oral squamous cell carcinoma

Anticancer Res. 2004 Jul-Aug;24(4):2153-60.

Abstract

Artemisinin (AR) is a widely used antimalarial drug. Recently, additional uses for AR as an anticancer drug were discovered. Using TUNEL, immunohistochemistry (IHS) markers and flow cytometry techniques, we evaluated the effect of AR and 5-FU on HPV 16 immortalized and transformed human gingival epithelial (IHGK) cells. The results of TUNEL showed that AR-treated IHGK cells consisted of 82% positive cells, while 5-FU-treated cells consisted of 18% positive cells. The IHS markers demonstrated positive staining with Bax p53, CD40 and CD40L in AR-treated cells and negative staining with Bcl-2. 5-FU-treated cells demonstrated a profile similar to AR but with less intensity. Cell cycle by flow cytometry results showed that only 5-FU-treated cells demonstrated a significant S-phase rate increase to 45%. In conclusion, our results indicate that AR is cytotoxic to transformed oral epithelial cells through apoptosis, while 5-FU is cytotoxic primarily through cell toxicity.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Artemisinins / pharmacology*
  • CD40 Antigens / metabolism
  • CD40 Ligand / metabolism
  • Carcinoma, Squamous Cell / drug therapy*
  • Carcinoma, Squamous Cell / metabolism
  • Carcinoma, Squamous Cell / pathology
  • Cell Cycle / drug effects
  • Dose-Response Relationship, Drug
  • Flow Cytometry
  • Fluorouracil / pharmacology
  • Humans
  • Immunohistochemistry
  • In Situ Nick-End Labeling
  • Mouth Neoplasms / drug therapy*
  • Mouth Neoplasms / metabolism
  • Mouth Neoplasms / pathology
  • Proto-Oncogene Proteins / metabolism
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Sesquiterpenes / pharmacology*
  • Tumor Suppressor Protein p53 / metabolism
  • bcl-2-Associated X Protein

Substances

  • Antineoplastic Agents
  • Artemisinins
  • BAX protein, human
  • CD40 Antigens
  • Proto-Oncogene Proteins
  • Proto-Oncogene Proteins c-bcl-2
  • Sesquiterpenes
  • Tumor Suppressor Protein p53
  • bcl-2-Associated X Protein
  • CD40 Ligand
  • artemisinin
  • Fluorouracil