Effects of fluoranthene, a polycyclic aromatic hydrocarbon, on cAMP-dependent anion secretion in human airway epithelia

J Pharmacol Exp Ther. 2004 Feb;308(2):651-7. doi: 10.1124/jpet.103.059089. Epub 2003 Nov 10.

Abstract

The human respiratory tract is constantly exposed to polycyclic aromatic hydrocarbons (PAHs) through inhalation of atmospheric pollutants. We examined the effects of three PAHs (benzo[a]pyrene, anthracene, and fluoranthene) on the airway ion transport, which is essential for lung defense and normal airway function, using human airway epithelia (Calu-3). These three PAHs had no significant effect on the basal short-circuit current (I(sc)). However, fluoranthene (1-100 microM) applied in the apical compartment potentiated I(sc) in response to cAMP-related agents (isoproterenol, forskolin, and 8-bromo-cAMP). The effects of fluoranthene were unaffected by ellipticine, a PAH receptor antagonist. Estimation of the anionic composition of I(sc) revealed that isoproterenol increased both HCO(3)(-) and Cl(-) transport in the control, whereas it potentiated only Cl(-) transport in the presence of fluoranthene. The fluoranthene-induced modulations of these anion transporters were counteracted by charybdotoxin (ChTx, a hIK-1 channel blocker). Fluoranthene gradually augmented the ChTx-sensitive K(+) current (I(K)) across the basolateral membrane, accompanied by a sustained increase in the cytosolic Ca(2+) concentration ([Ca(2+)](i)). In the presence of fluoranthene, however, a much larger hIK-1-dependent I(K) was identified by the application of 8-bromo-cAMP without concomitant elevation of [Ca(2+)](i). These results suggest that fluoranthene switches from cAMP-dependent HCO(3)(-) secretion to Cl(-) secretion through the hIK-1 channel, whose sensitivity to protein kinase A may be up-regulated by the sustained [Ca(2+)](i) elevation produced by this chemical.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anions / metabolism*
  • Calcium / metabolism
  • Cells, Cultured
  • Chloride Channels / metabolism
  • Cyclic AMP / chemistry
  • Cyclic AMP / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Epithelium / drug effects*
  • Epithelium / metabolism
  • Fluorenes / pharmacology*
  • Humans
  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • Organic Anion Transporters / drug effects
  • Organic Anion Transporters / metabolism
  • Polycyclic Aromatic Hydrocarbons / pharmacology
  • Potassium Channels / drug effects
  • Potassium Channels / metabolism
  • Potassium Channels, Calcium-Activated*
  • Respiratory System / cytology

Substances

  • Anions
  • Chloride Channels
  • Enzyme Inhibitors
  • Fluorenes
  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • KCNN4 protein, human
  • Organic Anion Transporters
  • Polycyclic Aromatic Hydrocarbons
  • Potassium Channels
  • Potassium Channels, Calcium-Activated
  • fluoranthene
  • Cyclic AMP
  • Calcium