Yang Xiu-Wei, Ma Li-Yuan, Zhou Qi-Le, Xu Wei, Zhang You-Bo
State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing 100191, PR China.
State Key Laboratory of Natural and Biomimetic Drugs (Peking University), Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing 100191, PR China.
Bioorg Med Chem Lett. 2018 Feb 1;28(3):240-243. doi: 10.1016/j.bmcl.2017.12.067. Epub 2017 Dec 30.
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 (3-31), 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.
人参作为一种传统中药,已被广泛用于治疗多种疾病,尤其是在延年益寿和抗肿瘤方面。人参中的达玛烷型三萜类化合物具有多种有益作用,其化学结构在口服后可在胃肠道中发生修饰。本文通过柱色谱法从人参茎叶总皂苷的人工胃液孵育物中分离得到达玛烷型三萜类化合物,并根据光谱数据确定其化学结构。获得了两种新的达玛烷型三萜类化合物,命名为人参转素B(1)和C(2),以及29种已知化合物(3 - 31)。使用SIRT1荧光药物发现检测试剂盒对分离得到的所有31种化合物进行了SIRT1活性研究。其中,化合物11、17、18、20、23、24、28和29被发现具有作为SIRT1激活剂的潜力,对SIRT1活性表现出显著的刺激作用。结果表明,这些化合物可被认为是延年益寿和抗肿瘤的有用药物资源。此外,该结果有助于从新的视角解释人参的长寿效应。