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Design, synthesis, and evaluation of β-galactosylceramide mimics promoting β-glucocerebrosidase activity in keratinocytes

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
13
Issue
5
Identifiers
DOI: 10.1016/s0960-894x(03)00006-4
Disciplines
  • Medicine

Abstract

Abstract We have established an efficient synthesis of mimics of β-galactosylceramide (β-GalCer) increasing a β-glucocerebrosidase (β-GlcCer'ase) activity that associates with the skin barrier function. Among the synthetic β-GalCer analogues ( 6a–6e) described herein, compound 6e exhibited a potent effect on the activation of β-GlcCer'ase function in vitro and reduced the transepidermal water loss (TEWL) level in a UVB-induced barrier disrupted mice model. These findings indicated that compound 6e could be useful for cosmetics and medicines to improve skin barrier function.

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