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目的对具有主动肝靶向性的去甲斑蝥素(NCTD)修饰物乳糖化-去甲斑蝥素(Lac-NCTD)的结构进行进一步的确证,同时对其进行小鼠腹腔注射给药的急性毒性研究。方法通过氢氢相关谱(1H-1HCOSY)和碳氢相关谱(13C-1HCOSY)进一步确证Lac-NCTD的结构,并以其能配制的最大浓度和最大给药体积对小鼠腹腔注射,测定一日内单次给药的最大耐受量(MTD)。结果1H-1HCOSY和13C-1HCOSY谱图表征了Lac-NCTD的结构,通过腹腔注射给药时,小鼠对Lac-NCTD的MTD大于4 g.kg-1,远大于人临床去甲斑蝥素的拟用量。结论新化合物Lac-NCTD结构确证,且安全性高,有望应用于临床。
OBJECTIVE: To further confirm the structure of Lac-NCTD, an NCTD modification with active liver targeting, and its acute toxicity to mice intraperitoneally the study. Methods The structure of Lac-NCTD was further confirmed by 1H-1HCOSY and 13C-1HCOSY. The mice were injected intraperitoneally with the maximum concentration and the maximum volume that can be formulated. The maximum tolerated dose (MTD) for a single daily dose. Results The structure of Lac-NCTD was characterized by 1H-1HCOSY and 13C-1HCOSY spectra. The MTD of Lac-NCTD in mice was higher than 4 g · kg-1 when administered intraperitoneally, much larger than that of human norcantharidin Proposed usage. Conclusions The new compound Lac-NCTD has confirmed the structure and high safety and is expected to be used clinically.