Kusumoto Shoichi, Fukase Koichi
Suntory Institute for Bioorganic Research, 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan.
Chem Rec. 2006;6(6):333-43. doi: 10.1002/tcr.20098.
A new stage of endotoxin research was brought about by structure elucidation and chemical synthesis of lipid A, the lipophilic partial structure of the lipopolysaccharide (LPS) of Gram-negative bacteria. Synthetic lipid A exhibited full endotoxic activity, which gave unequivocal evidence for the concept that lipid A is the active entity of endotoxin. Various lipid A analogues, as well as their radiolabeled derivatives and more complex partial structures of LPS, were also synthesized. By the use of these synthetic homogeneous preparations, not only simple studies on structure-activity relationships but precise and detailed analyses became possible on how this typical bacterial component is recognized by the innate immune receptor complex of mammalian cells.
革兰氏阴性菌脂多糖（LPS）的亲脂性部分结构脂质A的结构阐明和化学合成开启了内毒素研究的新阶段。合成脂质A表现出完全的内毒素活性，这为脂质A是内毒素的活性实体这一概念提供了明确证据。还合成了各种脂质A类似物及其放射性标记衍生物以及更复杂的LPS部分结构。通过使用这些合成的均一制剂，不仅可以对构效关系进行简单研究，还能够对这种典型细菌成分如何被哺乳动物细胞的天然免疫受体复合物识别进行精确而详细的分析。
