摘要
目的对制备获得的4-表河豚毒素(4-epiTTX)高纯样品进行结构确证与毒性测定。方法采用LCFLD检测法测定4-epiTTX样品纯度,采用HRMS、1 H NMR和13 C NMR对样品进行结构表征;开展4-epiTTX对小鼠的急性毒性试验。结果4-epiTTX样品纯度为98.72%,样品的HRMS图谱信息与4-epiTTX相对分子质量吻合,1 H NMR和13 C NMR数据与文献报道相符;测得4-epiTTX对小鼠的半数致死量(LD50)为(350.83±4.11)μg·kg-1。结论4-epiTTX与河豚毒素(TTX)的结构差别仅在于C-4上羟基为直立键。4-epiTTX有很强的毒性,但明显低于TTX的毒性,表明C-4上羟基的空间位置差异会影响毒素分子与受体的结合程度。
Objective To identify the chemical structure and determine the acute toxicity of 4-epiTTX. Methods The purity of 4-epiTTX sample was determined by LC-FLD and its chemical structure was i- dentified on the basis of HRMS, 1H NMR and 13C NMR. Its acute toxicity was evaluated on mice. Re- suits The purity of 4-epiTTX sample was 98. 72%. The mass spectrum was in very well agreement with the relative molecular mass of 4-epiTTX. The 1 H NMR and 13 C NMR spectra were similar to the litera- ture. LDs0 of 4-epiTTX to mice was （350.83±4.11）μg·kg-1. Conclusion The structural difference compared with TTX is that the （2-4 hydroxyl of 4-epiTTX is on the axial position. 4-epiTTX has a strong toxicity to mice, hut it is remarkably lower than TTX. It indicates that the spatial position difference of （2-4 hydroxyl would affect the binding degree of the toxin molecule with the reeontor
出处
《中国海洋药物》
CAS
CSCD
北大核心
2013年第5期73-76,共4页
Chinese Journal of Marine Drugs
基金
国家科技支撑计划项目(2011BAK04B09)
海洋公益性行业科研专项(200905022)资助
