| 川楝素水解与氢化还原产物的结构鉴定及其对肉毒毒素解毒作用研究 |
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| 引用本文： | 李海涛,董铭心,朱卫国,余云舟,舒国欣,戴秋云.川楝素水解与氢化还原产物的结构鉴定及其对肉毒毒素解毒作用研究[J].军事医学,2012,36(5):376-380. |
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| 作者姓名： | 李海涛 董铭心 朱卫国 余云舟 舒国欣 戴秋云 |
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| 作者单位： | 李海涛 (湘潭大学化学学院,湖南湘潭,411105) ； 董铭心 (军事医学科学院生物工程研究所,北京,100071) ； 朱卫国 (军事医学科学院生物工程研究所,北京,100071) ； 余云舟 (湘潭大学化学学院,湖南湘潭,411105) ； 舒国欣 (军事医学科学院生物工程研究所,北京,100071) ； 戴秋云 (军事医学科学院微生物流行病研究所,北京,100071) ； |
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| 基金项目： | 国家自然科学基金资助项目 |
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| 摘 要： | 目的鉴定川楝素水解及氢化还原产物的结构,并测定其对肉毒毒素的解毒效果。方法用一定比例的稀氨水水解川楝素,用氢化铝锂还原川楝素的环氧键,然后用高效液相色谱纯化各产物,用质谱、核磁共振氢谱鉴定产物结构;解毒活性测定中,小鼠用2LD50的A型肉毒毒素攻毒,腹腔注射不同剂量的川楝素水解及氢化产物后,4 d内观察小鼠死亡情况。结果与结论除全脱乙酰基产物外,获得2个川楝素单脱乙酰基产物及全脱乙酰基并环氧键还原的新产物,这些产物的毒性及对肉毒毒素的解毒活性降低。该工作为川楝素的体内药代产物鉴定及应用奠定了一定的基础。
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| 关 键 词： | 川楝素 水解作用 氢化还原 A型肉毒毒素 解毒 |
Structure identification and anti-botulinum effect of hydrolytic and hydrogenated reductive products of toosendanin |
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| Authors: | LI Hai-tao DONG Ming-xin ZHU Wei-guo YU Yun-zhou SHU Guo-xin DAI Qiu-yun |
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| Institution: | 1.College of Chemistry,Xiangtan University,Xiangtan,Hunan 411105,China;2.Institute of Biotechnology,Academy of Military Medical Sciences,Beijing 100071,China;3.Institute of Microbiology and Epidemiology,Academy of Military Medical Sciences,Beijing 100071,China) |
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| Abstract: | Objective To identify the structure of products of hydrolysis and hydrogenation reduction of toosendanin and examine their anti-botulinum neurotoxin(anti-BoNT) activities.Methods Toosendanin was hydrolyzed by ammonia and reduced by lithium aluminium tetrahydride.The products were purified by HPLC and characterized by FAB-MS and 1H-NMR.Their detoxification activities to botulinum A(BoNT/A) were determined after the intraperitoneal administration of 2LD50 BoNT/A into mice.The survival rate was recorded for 4 days.Results and Conclusion Two mono-deacetylated products and one epoxy opening product were obtained and characterized.The toxicity and detoxification activities to botulinum A of these products decreased significantly.This work will contribute to the toosendanin pharmacokinetics in vivo and application. |
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| Keywords: | toosendanin hydrolysis hydrogenation-reduction botulinum neurotoxins A detoxification |
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