Gynostemma pentaphyllum (Thunb.) Makino (Cucurbitaceae family) is a perennial creeping plant with a common Chinese name of “south ginseng”. To date, more than 250 individual saponins with dammarane-type skeleton have been isolated from G. pentaphyllum. The purpose of this study was the isolation and structural characterization of novel, minor gypenosides from G. pentaphyllum and evaluation of their Sirt1 agonist activity. Individual saponins from G. pentaphyllum were isolated and purified by a variety of chromatography techniques, and their structures were elucidated by means of various spectroscopic analysis and comparision with the reported data. Sirt1 enzyme activity detection kit was used to preliminarily evaluate the Sirt1 agonist activity of thirty three individual saponins purified from G. pentaphyllum. Fourteen new triterpenoid saponins named gypenoside CII-CXV (1–14) along with twenty six known compounds (15–40) were isolated from G. pentaphyllum. Thirty three of all the isolates were screened for Sirt1 agonist activity, and the results showed that three dammarane-type saponins (2, 18, 37) and one cucurbitane-type saponin 33 exhibited satisfactory Sirt1 agonist activity. These findings suggested that G. pentaphyllum was worthy of further investigation to find small molecule Sirt1 agonist and facilitate their utilization as “south ginseng”.

绞股蓝（Thunb.）牧野（葫芦科）为多年生匍匐植物，中文俗名“南参”。迄今为止，已从G. pentaphyllum 中分离出 250 多种具有达玛烷型骨架的个体皂苷。本研究的目的是从G. pentaphyllum 中分离出新型次要绞股蓝皂苷并对其进行结构表征，并评估它们的 Sirt1 激动剂活性。来自G. pentaphyllum 的单个皂苷通过各种色谱技术分离纯化，并通过各种光谱分析和与报道数据的比较阐明了它们的结构。用Sirt1酶活性检测试剂盒初步评价了从五叶草中纯化的33种皂苷的Sirt1激动剂活性。命名绞股蓝皂苷CII-CXV（十四新三萜皂苷1 - 14与26种的已知化合物（沿）15 - 40）从分离绞股蓝。对所有分离株中的 33 株进行了 Sirt1 激动剂活性筛选，结果显示三种达玛烷型皂苷 ( 2 , 18, 37 ) 和一种葫芦素型皂苷33表现出令人满意的 Sirt1 激动剂活性。这些发现表明G. pentaphyllum值得进一步研究以寻找小分子Sirt1 激动剂并促进其作为“南参”的利用。