碱催化降解法制备抗癌活性化合物20(S)-原人参二醇

高等学校化学学报 ›› 2006, Vol. 27 ›› Issue (3): 478.

碱催化降解法制备抗癌活性化合物20(S)-原人参二醇

李绪文¹,金永日¹,桂明玉¹,张寒琦¹,张龙清²

1. 吉林大学化学学院,长春130012; 2. 海南亚洲制药有限公司药物研究所,海口 570102

收稿日期:2005-06-30 出版日期:2006-03-10 发布日期:2006-03-10
通讯作者: 张寒琦(1948年出生),男,教授,博士生导师,从事光谱化学分析研究.E-mail:analchem@jlu.edu.cn
基金资助:
"九五"国家重点科技攻关项目(批准号: 96-901-01-83)资助.

Preparation of Antitumor Compound 20(S)- Protopanaxidiol by the Method of Alkali Catalyzing Degradation

LI Xu-Wen¹,JIN Yong-Ri¹,GUI Ming-Yu¹,ZHANG Han-Qi^1*,ZHANG Long-Qing²

1. College of Chemistry,Jilin Uuniversity,Changchun 130012,China;
2. Asia Medicine Co.,Ltd.,Haikou 321017,China

Received:2005-06-30 Online:2006-03-10 Published:2006-03-10

摘要/Abstract

摘要：

通过碱催化降解制备了与植物体内结构一致且具有抗癌活性的人参皂苷元--20(S)-原人参二醇,并对其进行分离及结构表征. 将西洋参茎叶总皂苷和强碱溶于高沸点有机溶剂中,在常压和高温条件下进行降解. 通过正交试验确定了制备20(S)-原人参二醇的最佳降解条件,并将降解物经萃取、柱层析及重结晶等方法分离得到20(S)-原人参二醇. 按西洋参茎叶总皂苷计,20(S)-原人参二醇产率为5.01%,纯度为98.56% . 通过理化性质和光谱分析可确认该化合物为20(S)-原人参二醇. 所制备的20(S)-原人参二醇具有产率和纯度高及成本低等特点.

关键词: 20(S)-原人参二醇; 制备; 碱; 催化; 降解; 抗癌

Abstract:

To prepare 20(S)-protopanaxidiolone natural sapogenin in Panax Ginseng C.A.,the method of alkali catalyzing degradation was used. 20(S)-Protopanaxidiol was separated and it′s structure was characterized. The total saponins from leaves and stems of Panax qinquefolium L. and strong alkali were solved in an organic solvent with a high boiling point,then the degradation was performed at high temperature and common pressure. The optimal condition of degradation was confirmed through orthogonal experiment. 20(S)-Protopanaxidiol was separated and purified by extraction,column chromatography and recrystal from the degradation products. The obtained yield of 20(S)-protopanaxidiol was 5.01% accounting for the total saponins and the purity of 20(S)-protopanaxidiol was 98.56%. The structure of the compound was elucidated by characteristics and spectral analysis as 20(S)-protopanaxidiol. The characteristics of the method were proved to be high yield,high purity and low costing in 20(S)-protopanaxidiol preparation.

Key words: 20(S)-Protopanaxidiol; Preparation; Alkali; Catalysis; Degradation; Antitumor

中图分类号:

O623.413

TrendMD:

李绪文金永日桂明玉张寒琦张龙清. 碱催化降解法制备抗癌活性化合物20(S)-原人参二醇. 高等学校化学学报, 2006, 27(3): 478.

LI Xu-Wen, JIN Yong-Ri, GUI Ming-Yu, ZHANG Han-Qi, ZHANG Long-Qing. Preparation of Antitumor Compound 20(S)- Protopanaxidiol by the Method of Alkali Catalyzing Degradation. Chem. J. Chinese Universities, 2006, 27(3): 478.