目的:应用高效液相制备色谱技术特异性去除北细辛中的毒性成分黄樟醚。方法:采用高效液相制备色谱技术对北细辛正己烷提取物中的强毒性成分黄樟醚进行目标去除,并保留其它活性成分。采用霍恩氏法(Hom's法)和二甲苯所致小鼠耳壳肿胀试验对去除黄樟醚前后的提取物进行急性毒性及抗炎活性检测。结果:HPLC检测结果显示黄樟醚已基本被去除。北细辛的LD50值由去除前的 1．47ml·kg-1(可信限为0．951-2．27)增大为2．37 ml·kg-1(可信限为1．48-3．80),毒性明显降低;对二甲苯所致小鼠耳壳肿胀的抑制率由40．00％增大为84．28％,抗炎活性明显增强。结论:采用高效液相制备色谱技术可以在基本保留其他活性成分的基础上特异性地去除中药毒性成分,从而达到减毒增效的目的。

Objective To get rid of safrole,a toxic component in the Chinese medicinal plant Asarum Heterotropoides Fr.var. mandshuricum (Maxim.)Kitag.by preparative HPLCtechnology. Method To take away the strongly toxic safrole from the extract of hexane in Asarum Heterotropoides by the preparative HPLC technology and preserve its active constituents and then test the acute toxicity and auti-inflammatory activity of the extracts with and without doing away safrole res-pertively by Horm's method and the experiment of inducing auricular edema of mice by dimenthyl benzene. Result The HPLC analysis indicates that safrole is basically done away from the extract. The LD50 value of Asarum Heterotropoides rises to 2.37ml·Kg-1 (with 1.48ml·Kg-1-3.80ml·Kg-1 of confidence limit)in extract through desafrole from 1.47ml ·Kg-1 (with0.951ml·Kg-1-2.27ml·Kg-1 of confidence limit)in the extract without desafrole and hence its anti-inflammatory activity can be remarkably strengthened. Conclusion The preparative HPL...更多C technology can afford to get away the toxic components of Chinese drugs tangibly while keeping their other active constituents in order to attain the goal of reducing the toxicity and increasing the effect of Chinese medicine.

中科院知识创新工程重要方向性项目(KGCX2-SW-213-02)基于现代理论和技术的复方中药系统研究