Ponpipom M M, Hagmann W K, O'Grady L A, Jackson J J, Wood D D, Zweerink H J
Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
J Med Chem. 1990 Feb;33(2):861-7. doi: 10.1021/jm00164a062.
6-(5-Cholesten-3 beta-yloxy)hexyl 1-thio-beta-D-mannopyranoside (L-644,257) enhances natural host resistance in cyclophosphamide-treated mice against Pseudomonas aeruginosa in a dose-dependent manner. It is active sc, im, and ip but not orally. L-644,257 is substantially more protective against P. aeruginosa than its alpha anomer. The beta-L-fucose glycolipid is more effective when given im and ip than sc. The lactose and beta-D-glucose glycolipids were only marginally effective to nonprotective. The 17 beta-steroidal side chain of L-644,257 can be modified without substantial loss of protective activity.
6-(5-胆甾烯-3β-基氧基)己基 1-硫代-β-D-甘露吡喃糖苷（L-644,257）以剂量依赖方式增强环磷酰胺处理小鼠对铜绿假单胞菌的天然宿主抵抗力。它经皮下、肌肉和腹腔注射有活性，但口服无活性。L-644,257 对铜绿假单胞菌的保护作用比其 α 端基异构体强得多。β-L-岩藻糖糖脂经肌肉和腹腔注射给药时比皮下注射更有效。乳糖和 β-D-葡萄糖糖脂仅具有微弱至无保护作用。L-644,257 的 17β-甾体侧链可进行修饰而不会大幅丧失保护活性。
