Satoh T, Miyataka H, Yamamoto K, Hirano T
Department of Bio-organic Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Japan.
Chem Pharm Bull (Tokyo). 2001 Aug;49(8):948-53. doi: 10.1248/cpb.49.948.
Vitamin E glycosides were synthesized and enzymatic hydrolysis was examined for use as potential pro-drugs, however, the glycoside bond was found to be stable. On the other hand, among the glycosides synthesized, dl-alpha-tocopherylglucoside (6b) and dl-alpha-tocopherylmannoside (6c) showed strong inhibitory action on histamine release from mast cells. In addition, 6c also showed a suppressive action on IgE antibody formation. Thus, tocopheryl glycoside showed new properties compared to tocopherol (vitamin E). In particular, 6c was shown to be a novel lead compound with excellent manifold anti-allergic activity and anti-inflammatory activity.
合成了维生素E糖苷，并对其酶促水解作为潜在前药的用途进行了研究，然而，发现糖苷键是稳定的。另一方面，在合成的糖苷中，dl-α-生育酚葡萄糖苷（6b）和dl-α-生育酚甘露糖苷（6c）对肥大细胞释放组胺具有强烈的抑制作用。此外，6c对IgE抗体形成也有抑制作用。因此，生育酚糖苷与生育酚（维生素E）相比表现出了新的特性。特别是，6c被证明是一种具有优异多种抗过敏活性和抗炎活性的新型先导化合物。
