Effects of retinoic acid receptor-selective agonists on human nasal epithelial cell differentiation

Am J Respir Cell Mol Biol. 2001 Dec;25(6):744-50. doi: 10.1165/ajrcmb.25.6.4549.

Abstract

Retinoids play a critical role in the maintenance of the mucociliary phenotype of epithelial cells in the upper respiratory tract. To determine the role of retinoic acid receptors (RARs) in the regulation of epithelial differentiation, we tested the effect of the synthetic retinoids CD336, CD2019, and CD666, selective agonists for RARalpha, RARbeta, and RARgamma, respectively, during differentiation of human nasal epithelial (HNE) cells in vitro. Using glutamylated tubulin and transglutaminase I (Tg I) as markers of ciliated cell and squamous cell differentiation, respectively, we showed that retinoic acid (RA) stimulated mucociliary differentiation and, in parallel, inhibited squamous cell differentiation. The agonists of the three RARs independently induced ciliogenesis and inhibited squamous cell differentiation by downregulating Tg I expression in a dose- and time-dependent manner. Antagonists specific for the three RARs abolished the effects of the corresponding agonists, demonstrating an RAR-specific mediated effect. Moreover, treatment of retinoid-deficient cultures with RAR agonists induced conversion of the squamous-like phenotype into a ciliated phenotype. In conclusion, all three RARs are potentially involved in the differentiating effects of RA in respiratory epithelial cells.

MeSH terms

  • Benzoates / pharmacology*
  • Biomarkers
  • Cell Differentiation / drug effects
  • Cell Nucleus / metabolism
  • Cilia / ultrastructure
  • Epithelial Cells / cytology
  • Epithelial Cells / drug effects
  • Gene Expression Regulation, Enzymologic / drug effects
  • Humans
  • Microscopy, Electron, Scanning
  • Naphthalenes / pharmacology*
  • Nasal Mucosa / cytology
  • Nasal Mucosa / drug effects*
  • Nasal Polyps / pathology
  • Receptors, Retinoic Acid / agonists*
  • Receptors, Retinoic Acid / physiology
  • Retinoic Acid Receptor alpha
  • Retinoic Acid Receptor gamma
  • Retinoids / pharmacology*
  • Tetrahydronaphthalenes / pharmacology*
  • Transglutaminases / analysis
  • Tubulin / analysis

Substances

  • Benzoates
  • Biomarkers
  • CD 2019
  • CD 666
  • Naphthalenes
  • RARA protein, human
  • Receptors, Retinoic Acid
  • Retinoic Acid Receptor alpha
  • Retinoids
  • Tetrahydronaphthalenes
  • Tubulin
  • retinoic acid receptor beta
  • Am 580
  • Transglutaminases
  • transglutaminase 1