目的 基于活性导向分离瓜蒌皮Trichosanthis Pericarpium中具有抗肾素作用的成分。方法 瓜蒌皮经水提醇沉后取上清液，然后透析截留获相对分子质量1 000以上的部分（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-5-1，并对GLP-5-1进行HPGPC法分析、单糖组成测定和肾素抑制活性检测。结果 采用活性跟踪方法，从瓜蒌皮中得到一种具有肾素抑制作用的均一多糖GLP-5-1，相对分子质量为3 722，主要由阿拉伯糖、甘露糖、葡萄糖和半乳糖组成，4种单糖的物质的量比为5.5：4.4：6.9：10.0，GLP-5-1表现出较强的肾素抑制活性，其半数抑制浓度（IC₅₀）为（87.4±6.8）μg/mL。结论 从瓜蒌皮中成功分离到具有肾素抑制作用的低相对分子质量的多糖，为瓜蒌皮的化学物质基础研究提供依据。

Objective To isolate anti-renin constituents from Trichosanthis Pericarpium based on bioactivity tracking separation. Methods T. Pericarpium was extracted with boiling water and precipitated by ethanol, the supernate was collected and dialyzed, and the retentate was lyophilized giving GLP, then successively separated by DEAE Sepharose Fast Flow anion-exchange and Superdex-75 gel permeation chromatographic steps, to give GLP-5-1. A combination of HPGPC, monosaccharide composition, and anti-renin studies was performed to investigate the structure and bioactivity. Results An anti-renin polysaccharide, GLP-5-1, was obtained from T. Pericarpium based on activity tracking, the average molecular weight was estimated to 3722, monosaccharide composition analysis showed GLP-5-1 contained arabinose, mannose, glucose, and galactose with the ratio of 5.5:4.4:6.9:10.0. GLP-5-1 showed potent anti-renin effect with the IC₅₀ was (87.4 ±6.8) μg/mL. Conclusion In this study, a low molecular weight polysaccharide with anti-renin effect was isolated from T. Pericarpium, which could lay the foundation for the substance basis study of T. Pericarpium.

上海市科委科研计划项目（15DZ1900101）；中国博士后科学基金面上资助项目（2016M601637）