Abstract
We have established an efficient synthesis of mimics of beta-galactosylceramide (beta-GalCer) increasing a beta-glucocerebrosidase (beta-GlcCer'ase) activity that associates with the skin barrier function. Among the synthetic beta-GalCer analogues (6a-6e) described herein, compound 6e exhibited a potent effect on the activation of beta-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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Biomimetic Materials / chemical synthesis*
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Biomimetic Materials / pharmacology*
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Cells, Cultured
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Drug Design
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Enzyme Activation / drug effects
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Epidermis / drug effects
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Epidermis / metabolism
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Epidermis / radiation effects
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Galactosylceramides / chemical synthesis*
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Galactosylceramides / pharmacology*
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Glucosylceramidase / metabolism*
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Humans
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Keratinocytes / drug effects*
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Keratinocytes / enzymology
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Keratinocytes / radiation effects
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Mice
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Structure-Activity Relationship
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Ultraviolet Rays
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Water Loss, Insensible / drug effects
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Water Loss, Insensible / radiation effects
Substances
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Galactosylceramides
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Glucosylceramidase