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New dammarane-type triterpenoid saponins from Gynostemma pentaphyllum and their Sirt1 agonist activity
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2021-09-15 , DOI: 10.1016/j.bioorg.2021.105357
Yun-Yun Lou 1 , Xian Zheng 1 , Ya-Ping Huang 2 , Long Mu 2 , Xiao-Gai Zhang 3 , Zhi-Wei Zhao 1 , Zhe Song 4 , Jian Zhang 5 , Zhi-Qi Yin 2 , Ke Pan 2
Affiliation  

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 (114) along with twenty six known compounds (1540) 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”.



中文翻译:


绞股蓝新达玛烷型三萜皂苷及其Sirt1激动剂活性



绞股蓝(Thunb.)Makino(葫芦科)是多年生匍匐植物,俗名“南参”。迄今为止,已从G. pentaphyllum中分离出超过 250 个具有达玛烷型骨架的皂苷。本研究的目的是从G. pentaphyllum中分离和结构表征新型次要绞股蓝皂苷,并评估其 Sirt1 激动剂活性。通过多种色谱技术分离和纯化了五叶紫葳中的各个皂苷,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。采用Sirt1酶活性检测试剂盒初步评价了五叶子草中纯化的33种皂苷的Sirt1激动剂活性。从G. pentaphyllum中分离出 14 种新的三萜皂苷,命名为绞股蓝皂苷 CII-CXV ( 114 ) 以及 26 种已知化合物 ( 1540 )。对33个分离株进行了Sirt1激动剂活性筛选,结果显示 3个达玛烷型皂苷(2,18,37 )和1个葫芦烷型皂苷33表现出了令人满意的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。

更新日期:2021-09-23
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