摘要
研究在离体条件下各种单体柴胡皂甙和甘草甜素抑制Ｎａ＋，Ｋ＋ＡＴＰ酶活性的构效关系。实验结果表明，各种柴胡皂甙抑制Ｎａ＋，Ｋ＋ＡＴＰ酶活性的作用强度依次为：ｂ１＞ｄ＞ｂ２＞ｂ４＞ａ＞ｂ３＞ｅ＞ｃ。柴胡皂甙化学结构中的Ｃ２３ＯＨ，Ｃ１６ＯＨ及Ｃ１１和Ｃ１３的共轭双烯可能对其抑制活性起重要作用。甘草甜素（ＧＬ），甘草次酸（ＧＡ）和生胃酮（１８β甘草次酸半琥珀酸双钠盐，ＣＸ）抑制Ｎａ＋，Ｋ＋ＡＴＰ酶活性的作用强度依次为ＧＡ≥ＣＸ＞ＧＬ。研究还证明，柴胡皂甙ｄ对Ｎａ＋。
The study on structure activity relationship of saikosaponins and glycyrrhizin derivatives for Na +,K + ATPase inhibiting action has been made in vitro . The results showed that the order of potency of inhibitory effect of saikosaponins on Na +,K + ATPase is as follows: b 1>d>b 2>b 4>a>b 3>e>c. The chemical structure C 23 OH, C 16 OH and the C 11 , C 13 conjugated double diene of saikosaponins are important for its inhibitory activity. The inhibitory potency of glycyrrhizin(GL), glycyrrhetinic acid(GA) and carbenoxolone(CX) for Na +, K + ATPase activity is as follows: GA≥CX>GL. In addition, the inhibitory effect of saikosaponin d on Na +, K + ATPase was found to be non competitive.
出处
《药学学报》
CAS
CSCD
北大核心
1996年第7期496-501,共6页
Acta Pharmaceutica Sinica
关键词
柴胡皂甙
甘草甜素
钠离子
钾离子
ATP酶
Saikosaponin
Glycyrrhizin
Na +,K + ATPase
Non competitive inhibition
