Globotriaosylceramide-induced reduction of KCa1.1 channel activity and activation of the Notch1 signaling pathway in skin fibroblasts of male Fabry patients with pain

Exp Neurol. 2020 Feb:324:113134. doi: 10.1016/j.expneurol.2019.113134. Epub 2019 Nov 25.

Abstract

Background: Fabry disease (FD) is an X-linked lysosomal storage disorder that leads to cellular globotriaosylceramide (Gb3) accumulation due to mutations in the gene encoding α-galactosidase A. Trigger-induced acral burning pain is an early FD symptom of unknown pathophysiology. We aimed at investigating the potential role of skin fibroblasts in nociceptor sensitization.

Patients and methods: We enrolled 40 adult FD patients and ten healthy controls, who underwent a 6-mm skin punch biopsy at the lower leg. Dermal fibroblasts were cultivated and analyzed for Gb3 load. Fibroblast electrical activity was assessed using patch-clamp analysis at baseline and upon incubation with agalsidase-α for 24 h. We investigated gene expression of CC motif chemokine ligand 2 (CCL2), Ca2+activated K+-channel 1.1 (KCa1.1), interferone-γ (IFN-γ), transforming growth factor-β1 (TGF-β1), and transmembrane receptor notch homolog 1 (Notch1) using quantitative real-time-PCR, and protein levels of KCa1.1 by ELISA. Gene expression was determined at baseline and after fibroblast stimulation with tumor necrosis factor-α (TNF), modeling inflammation as a common pain trigger in FD.

Results: Total Gb3 load was higher in FD fibroblasts than in control fibroblasts (p < .01). Upon increase of intracellular Ca2+ concentrations, we detected differential electrical activity of KCa1.1 in fibroblasts obtained from patients with FD. Gene expression (p < .05) and protein levels of KCa1.1 (p < .05) were higher in fibroblasts from FD patients compared to control fibroblasts, whereas electric channel activity was lower in FD fibroblasts. After incubation with agalsidase-α, we observed an over-proportionate increase of KCa1.1 activity in FD fibroblasts reaching 7-fold the currents of control cells (p < .01). Gene expression studies revealed higher mRNA levels of CCL2, INF-γ, and Notch1 in FD fibroblasts compared to controls at baseline and after TNF incubation (p < .05 each), while TGF-β1 was higher in FD fibroblasts only after incubation with TNF (p < .05).

Conclusions: Gb3 deposition in skin fibroblasts may impair KCa1.1 activity and activate the Notch1 signaling pathway. The resulting increase in pro-inflammatory mediator expression may contribute to cutaneous nociceptor sensitization as a potential mechanism of FD-associated pain.

Keywords: Fabry disease; Fabry pain; Fibroblast; KCa1.1 channel; Patch clamp;Notch1; Skin punch biopsy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Animals
  • Chemokine CCL2 / metabolism
  • Fabry Disease / drug therapy*
  • Fabry Disease / metabolism
  • Fabry Disease / pathology
  • Female
  • Fibroblasts / drug effects*
  • Fibroblasts / pathology
  • Gene Expression / drug effects
  • Humans
  • Large-Conductance Calcium-Activated Potassium Channel alpha Subunits / antagonists & inhibitors*
  • Large-Conductance Calcium-Activated Potassium Channel alpha Subunits / genetics
  • Mice
  • Middle Aged
  • Pain
  • Potassium Channel Blockers / pharmacology*
  • Primary Cell Culture
  • Receptor, Notch1 / drug effects*
  • Signal Transduction / drug effects*
  • Skin / pathology
  • Transcription Factor RelA / metabolism
  • Trihexosylceramides / antagonists & inhibitors
  • Trihexosylceramides / genetics
  • Trihexosylceramides / metabolism*
  • Young Adult

Substances

  • CCL2 protein, human
  • Chemokine CCL2
  • KCNMA1 protein, human
  • Large-Conductance Calcium-Activated Potassium Channel alpha Subunits
  • NOTCH1 protein, human
  • Potassium Channel Blockers
  • Receptor, Notch1
  • Transcription Factor RelA
  • Trihexosylceramides
  • globotriaosylceramide