pH directly regulates epidermal permeability barrier homeostasis, and stratum corneum integrity/cohesion

J Invest Dermatol. 2003 Aug;121(2):345-53. doi: 10.1046/j.1523-1747.2003.12365.x.

Abstract

Both exposure of stratum corneum to neutral pH buffers and blockade of acidification mechanisms disturb cutaneous permeability barrier homeostasis and stratum corneum integrity/cohesion, but these approaches all introduce potentially confounding variables. To study the consequences of stratum corneum neutralization, independent of hydration, we applied two chemically unrelated superbases, 1,1,3,3-tetramethylguanidine or 1,8-diazabicyclo [5,4,0] undec-7-ene, in propylene glycol:ethanol (7:3) to hairless mouse skin and assessed whether discrete pH changes alone regulate cutaneous permeability barrier function and stratum corneum integrity/cohesion, as well as the responsible mechanisms. Both 1,1,3,3-tetramethylguanidine and 1,8-diazabicyclo [5,4,0] undec-7-ene applications increased skin surface pH in parallel with abnormalities in both barrier homeostasis and stratum corneum integrity/cohesion. The latter was attributable to rapid activation (<20 min) of serine proteases, assessed by in situ zymography, followed by serine-protease-mediated degradation of corneodesmosomes. Western blotting revealed degradation of desmoglein 1, a key corneodesmosome structural protein, in parallel with loss of corneodesmosomes. Coapplication of serine protease inhibitors with the superbase normalized stratum corneum integrity/cohesion. The superbases also delayed permeability barrier recovery, attributable to decreased beta-glucocerebrosidase activity, assessed zymographically, resulting in a lipid-processing defect on electron microscopy. These studies demonstrate unequivocally that stratum corneum neutralization alone provokes stratum corneum functional abnormalities, including aberrant permeability barrier homeostasis and decreased stratum corneum integrity/cohesion, as well as the mechanisms responsible for these abnormalities.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology
  • Desmosomes / ultrastructure
  • Enzyme Activation
  • Epidermis / metabolism
  • Epidermis / physiology*
  • Epidermis / ultrastructure
  • Guanidines / pharmacology
  • Homeostasis*
  • Hydrogen-Ion Concentration
  • Male
  • Mice
  • Mice, Hairless
  • Permeability
  • Protons*
  • Recovery of Function / drug effects
  • Serine Endopeptidases / metabolism
  • Time Factors

Substances

  • Bridged Bicyclo Compounds, Heterocyclic
  • Guanidines
  • Protons
  • Serine Endopeptidases
  • 1,8-diazabicyclo(5.4.0)undec-7-ene
  • 1,1,3,3-tetramethylguanidine