活性导向分离瓜蒌皮中具有抗血管紧张素转化酶作用的成分

Bioactivity-guided isolation of anti-angiotensin converting enzyme constituents from Trichosanthis Pericarpium

该试验基于活性导向分离瓜蒌皮中具有抗血管紧张素转化酶(ACE)作用的成分。瓜蒌皮经水提醇沉后取上清液,然后透析截留获1 000以上的部分得GLP,GLP经活性跟踪测定,DEAE Sepharose Fast Flow阴离子交换树脂分离和Superdex-75系列凝胶纯化后得GLP-1-1,并对GLP-1-1进行HPGPC分析、单糖组成测定和ACE抑制活性检测。结果显示,采用活性跟踪方法,从瓜蒌皮中得到一种具有ACE抑制作用的均一低聚糖GLP-1-1,相对分子质量为1 367,主要由阿拉伯糖、甘露糖和葡萄糖组成,3种单糖的摩尔比为0.2∶4.3∶10.0,GLP-1-1表现出较强的ACE抑制活性,其IC_(50)为(113.4±8.6)mg·L^(-1)。从瓜蒌皮中成功分离到具有ACE抑制作用的低聚糖,该发现为瓜蒌皮的化学物质基础提供依据。

To isolate the anti-angiotensin converting enzyme（ ACE） constituents from Trichosanthis Pericarpium based on bioactivity-guided separation. Trichosanthis Pericarpium was extracted with boiling water and precipitated by ethanol,then its supernatant was collected and dialyzed. The retentate of the fractions above 1 000 was lyophilized to obtain GLP,which was then successively separated by DEAE Sepharose fast flow anion-exchange and Superdex-75 gel permeation chromatographic steps to achieve GLP-1-1. A combination of HPGPC,monosaccharide compositions determination and ACE inhibitory activity studies was performed to investigate the structure and bioactivity. The results showed that an anti-angiotensin converting enzyme oligosaccharide,GLP-1-1,was obtained from Trichosanthis Pericarpium based on activity tracking,whose average molecular weight was estimated to 1 367; mainly composed of arabinose,mannose,and glucose at a ratio of 0. 2 ∶ 4. 3 ∶ 10. 0. GLP-1-1 showed potent anti-angiotensin converting enzyme effect with the IC_（50） of（ 113. 4 ± 8. 6） mg·L^（-1）. In this study,an oligosaccharide with anti-angiotensin converting enzyme effect was isolated from Trichosanthis Pericarpium,which could lay the foundation for the substance basis study of Trichosanthis Pericarpium.