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SIRT1 activator isolated from artificial gastric juice incubate of total saponins in stems and leaves of Panax ginseng
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-12-30 , DOI: 10.1016/j.bmcl.2017.12.067
Xiu-Wei Yang , Li-Yuan Ma , Qi-Le Zhou , Wei Xu , You-Bo Zhang

Panax ginseng as a traditional Chinese medicine has been extensively used for the treatment of many diseases, especially in prolonging life and anti-tumor. Dammarane-type triterpenoids from P. ginseng have diverse beneficial effects and their chemical structures can be modified in the gastrointestinal tract after oral administration. In this paper, the dammarane-type triterpenoids were isolated from artificial gastric juice incubate of total saponins in the stems and leaves of P. ginseng through column chromatographic methods and their chemical structures were determined based on spectral data. Two new dammarane-type triterpenoids named ginsenotransmetins B (1) and C (2), along with twenty-nine known compounds (331), were obtained. All 31 compounds isolated were investigated for their activities of SIRT1 using SIRT1 fluorometric drug discovery assay kit. Among them, compounds 11, 17, 18, 20, 23, 24, 28, and 29, which were found to be potential as SIRT1 activators, exhibited significant stimulation of SIRT1 activity. The results showed that these compounds may be considered to be a useful medicinal resource for prolonging life and anti-tumor. In addition, the results were helpful to explain the longevity effect of ginseng from the new field of view.



中文翻译:

人参胃液中分离出SIRT1激活剂孵育人参茎和叶中总皂苷

人参作为一种传统中药已被广泛用于治疗许多疾病,特别是在延长寿命和抗肿瘤方面。人参的达玛烷型三萜类化合物具有多种有益作用,口服后可在胃肠道中修饰其化学结构。本文通过人工色谱法从人参茎叶中总皂苷的人工胃液中分离得到了达玛烷型三萜类化合物,并利用光谱数据确定了其化学结构。两个新的金刚烷型三萜类化合物,称为人参转铁蛋白B(1)和C(2),以及二十九种已知化合物(331),已获得。使用SIRT1荧光药物发现测定试剂盒对所有分离出的31种化合物的SIRT1活性进行了研究。其中,化合物11171820232428,和29,其被发现是作为活化剂SIRT1潜力,表现出SIRT1活性的显著刺激。结果表明,这些化合物可被认为是延长寿命和抗肿瘤的有用医学资源。此外,这些结果有助于从新的角度解释人参的延寿作用。

更新日期:2017-12-30
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