Intervention of sulfur mustard toxicity by downregulation of cell proliferation and metabolic rates

J Appl Toxicol. 2000 Dec:20 Suppl 1:S87-91. doi: 10.1002/1099-1263(200012)20:1+<::aid-jat683>3.0.co;2-n.

Abstract

Metabolically active and proliferating basal cells in the skin are most sensitive to the potent skin blistering chemical warfare compound HD (bis-(2-chloroethyl) sulfide). We previously described a Ca2+-dependent mechanism of HD (0.3-1 mM) toxicity that was inhibited by the cell-permeant Ca2+ chelator BAPTA AM (1,2-bis(O-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid acetoxymethyl ester). We describe some cellular effects of BAPTA AM that suggest a mechanism for its protective action. Monolayer log-phase normal human epidermal keratinocytes were incubated (37 degrees C) first in keratinocyte growth medium (KGM) containing BAPTA AM (10-40 microM) for 30 min and then in KGM alone overnight prior to evaluation. The BAPTA AM inhibited cell growth in a concentration-dependent manner with some cellular degeneration above 30 microM (light microscopy). At 20-30 microM, BAPTA AM also inhibited cellular metabolic processes, as evidenced by a lower incorporation of [3H]-thymidine (DNA synthesis, 54 +/- 5%), [3H]-uridine (RNA synthesis, 29 +/- 6%) and [14C]-valine (protein synthesis, 12 +/- 2%) as well as a lower protein content per culture (30 +/- 3%) compared with corresponding untreated controls. However, 20-30 microM BAPTA AM did not cause any demonstrable cytopathology based on morphological (electron microscopy) as well as biochemical (lactate dehydrogenase release, an indicator of cell viability loss) criteria, indicating a lack of acute toxicity. These results suggest that a mechanism of protection by BAPTA AM against HD may be via decreasing some metabolic, and therefore proliferative, rates.

MeSH terms

  • Cell Culture Techniques
  • Cell Division / drug effects*
  • Chelating Agents / pharmacology*
  • Dermatologic Agents / toxicity*
  • Down-Regulation
  • Egtazic Acid / analogs & derivatives
  • Egtazic Acid / pharmacology*
  • Humans
  • Keratinocytes / drug effects*
  • Keratinocytes / physiology
  • L-Lactate Dehydrogenase / analysis
  • Microscopy, Electron
  • Mustard Gas / toxicity*
  • Poisoning / prevention & control
  • Protective Agents / pharmacology*
  • Protein Biosynthesis

Substances

  • Chelating Agents
  • Dermatologic Agents
  • Protective Agents
  • 1,2-bis(2-aminophenoxy)ethane N,N,N',N'-tetraacetic acid acetoxymethyl ester
  • Egtazic Acid
  • L-Lactate Dehydrogenase
  • Mustard Gas