摘要
目的通过简单工艺除去大部分士的宁制备马钱子优化总生物碱以实现减毒增效。方法利用马钱子碱与士的宁在50%乙醇中的溶解度相差悬殊的原理除去马钱子总生物碱中的大部分士的宁制备马钱子优化总生物碱。酸性染料法测定纯度,HPLC法测定其中马钱子碱和士的宁的含量变化,比较优化前后马钱子总生物碱的急性毒性以及对小鼠耳肿胀的抑制作用。结果制得的马钱子优化总生物碱以马钱子碱计,纯度为(100.66±1.84)%(n=3),优化前后马钱子碱与士的宁的含量比例从1∶1.8上升到2.7∶1。优化后马钱子总生物碱的毒性显著下降,LD50比优化前提高了4.8倍。马钱子优化总生物碱的抑制耳肿胀活性显著优于马钱子总生物碱。结论马钱子优化总生物碱可以实现减毒增效,提高治疗指数。
Objective To attenuate noxious and increase therapeutic efficiency, by removing most strychnine to prepare Strychnou nux-vomica L. optimization of total alkaloids with simple process. Methods Making use of the different solubili- ty in the 50% ethanol, the content of strychnine was significantly reduced in the composition of total alkaloids to obtain the modified total alkaloids （MTA）. The purity of MTA was determined by the acidic dyecolorimetry. The contents of strychnine and brucine in TA and MTA were determined and compared by HPLC. The acute toxicity and antiflammatory activity were further investigated and compared. Results The purity of MTA was determined to be （100.66±1.84）% （n = 3）. After removing most strychnine, the mass ratio of brucine to strychnine increased from 1：1.8 in TA to 2.7：1 in MTA. The LD50 val- ue of MTA increased about 4.8-fold compared with that of TA. Moreover, the antiflammatory activity of MTA also in- creased significantly compared to that of TA. Conclusion Compared with TA, MTA possesses the higher therapeutic index.
出处
《中国医药导报》
CAS
2012年第36期35-37,共3页
China Medical Herald
关键词
马钱子
总生物碱
士的宁
马钱子碱
急性毒性
Strychnou nux-vomica L.
Total alkaloids
Strychnine
Brucine
Acute toxicity
