Van Huy Le, Tanaka Chiaki, Imai Takashi, Yamasaki Sho, Miyamoto Tomofumi
Department of Natural Products Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka 812-8582, Japan.
Department of Molecular Immunology, Immunology Frontier Research Center, Osaka University, Osaka 565-0871, Japan.
ACS Med Chem Lett. 2018 Dec 13;10(1):44-49. doi: 10.1021/acsmedchemlett.8b00413. eCollection 2019 Jan 10.
Fifteen glycosyl-oxystearates were synthesized by Crich's 4,6-benzylidene and Köening-Knorr strategies. Assessment of structure-activity relationships using macrophage-inducible C-type lectin (Mincle) receptor cells expressing nuclear factor of activated T cells (NFAT)-green fluorescent protein (GFP) revealed that four dimannopyranosyl-oxystearate analogues were Mincle agonists and that 12--(2--α-d-mannopyranosyl)-α-d-mannopyranosyl-oxystearate was as an activator of both mouse and human Mincle.
通过克里奇（Crich）的4,6-亚苄基策略和柯宁-克诺尔（Köening-Knorr）策略合成了15种糖基-氧代硬脂酸酯。使用表达活化T细胞核因子（NFAT）-绿色荧光蛋白（GFP）的巨噬细胞诱导型C型凝集素（Mincle）受体细胞评估构效关系，结果显示四种二甘露吡喃糖基-氧代硬脂酸酯类似物是Mincle激动剂，并且12-（2-α-d-甘露吡喃糖基）-α-d-甘露吡喃糖基-氧代硬脂酸酯是小鼠和人Mincle的激活剂。
