Yarkoni E, Rapp H J, Polonsky J, Varenne J, Lederer E
Infect Immun. 1979 Nov;26(2):462-6. doi: 10.1128/iai.26.2.462-466.1979.
Intratumoral injection of ultrasonically prepared emulsions of the synthetic glycolipid methly 6-O-(2-tetradecyl-3-hydroxyoctadecanoyl)-alpha-D-glucopyranoside (designated C39) induced complete regression of transplants of a syngeneic murine fibrosarcoma in most of the treated animals as did 6,6'-di-O(2-tetradecyl-3-hydroxyoctadecanoyl)-alpha,alpha,-trehalose (designated C76) in a previous study. The C76 compound, about twice the molecular weight of C39, was more effective therapeutically than the smaller molecule. Ultrasonically prepared emulsions of C39 and C76 were not toxic when given intravenously. Intravenously administered emulsions of C39 prepared by mechanical grinding were more toxic, but less granulomagenic, than those containing C76. Squalane and squalene, but not peanut oil, were effective substitutes for mineral oil as carriers of C39 in the treatment of the tumor.
在大多数接受治疗的动物中,瘤内注射超声制备的合成糖脂6-O-(2-十四烷基-3-羟基十八烷酰基)-α-D-吡喃葡萄糖苷(命名为C39)的乳剂,能使同基因小鼠纤维肉瘤移植瘤完全消退,在先前的一项研究中,6,6'-二-O(2-十四烷基-3-羟基十八烷酰基)-α,α,-海藻糖(命名为C76)也有同样效果。C76化合物的分子量约为C39的两倍,在治疗上比小分子更有效。超声制备的C39和C76乳剂静脉注射时无毒。通过机械研磨制备的C39静脉注射乳剂比含C76的乳剂毒性更大,但致肉芽肿性更小。角鲨烷和角鲨烯,而非花生油,是治疗肿瘤时作为C39载体替代矿物油的有效物质。