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

被引：16
|
作者：
Fukunaga, K
Yoshida, M
Nakajima, F
Uematsu, R
Hara, M
Inoue, S
Kondo, H
Nishimura, SI
机构：
[1] Kanebo Ltd, Basic Res Lab, Odawara, Kanagawa 2500002, Japan
[2] Hokkaido Univ, Japan Bioind Assoc, Sapporo Lab Glycocluster Project, Sapporo, Hokkaido 0600810, Japan
[3] Nippon Organon Ltd, Dept Chem, Miyakojima Ku, Osaka, Japan
[4] Hokkaido Univ, Grad Sch Sci, Div Biol Sci, Lab Biomacromol Chem, Sapporo, Hokkaido 0600810, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 05期
关键词：
D O I：
10.1016/S0960-894X(03)00006-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：813 / 815
页数：3
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