抗肿瘤有效成分20(R)-25-OCH_3-原人参二醇的结晶法分离  

Crystallization separation of antitumor constituent 20(R)-25-OCH_3-PPD

作　　者：张赛楠[1] 赵余庆[1,2] 

机构地区：[1]沈阳药科大学,辽宁沈阳110016 [2]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中草药》2014年第6期770-773,共4页Chinese Traditional and Herbal Drugs

基　　金："十一五"国家重大新药创制项目(2009ZX09102-114);中药标准提取物的工业化色谱制备平台建设(2009ZX09301-012-105B);国家自然科学基金资助项目(81273389)

摘　　要：目的从25-OCH3-原人参二醇(25-OCH3-PPD)非消旋体混合物中分离得到抗肿瘤有效成分20(R)-25-OCH3-PPD(AD-1)。方法采用结晶法拆分25-OCH3-PPD非消旋体混合物中的AD-1,并对所用溶剂的种类、用量及结晶温度等分离条件进行了优化,探讨溶剂的介电常数和25-OCH3-PPD非消旋体混合物的S/R比例间的关系。结果 25-OCH3-PPD非消旋体混合物(R:59.34%;S:38.35%),在最优条件下,丙酮26 mL、4℃时,可以获得AD-1的产率与纯度分别为38.76%、97.83%。结论溶剂的电解质范围在20.7左右,低饱和度的溶剂以及低温有利于AD-1的分离。Objective To separate antitumor constituent AD-1 [20（R）-25-OCH3-protopanoxadiol （PPD）] from non-racemic enatiomeric mixture. Methods A crystallization method has been developed to separate AD-1 from 25-OCHa-PPD non-racemic enatiomeric mixture, the sorts and amount of solvent and crystallization temperature were optimized to obtain the best separative conditions, and the relationship between the S/R percentage of 25-OCH3-PPD non-racemic enantiomeric mixture and dielectric constant of the solventwas discussed. Results Under the optimized conditions （acetone 26 mL, 4 ~C）, the yield and purity ofAD-1 crystals are 38.76% and 97.83% from 25-OCHa-PPD non-racemic enatiomeric mixture （R： 59.34%; S： 38.35%）, respectively. Conclusion The e values of solvents are about 20.7, and an unsaturated solution and low temperature are beneficial to the separation of AD-1 from 25-OCHa-PPD non-racemic enatiomeric mixture.

关 键 词：结晶 非消旋体混合物 25-OCH3-原人参二醇 20(R)-25-OCH3-原人参二醇 介电常数 抗肿瘤 

分 类 号：R284.1[医药卫生—中药学]