title: New SIRT1 activator from alkaline hydrolysate of total saponins in the stems-leaves of Panax ginseng.
abstract: Two new dammarane-type triterpenes, namely ginsenoslaloside-I [3β,12β,24S-trihydroxy-dammara-20(22)E,25-diene-3-O-β-D-glucopyranoside, 1] and 20(S)-ginsenoside-Rh1-6'-acetate (2), together with twelve known compounds (3-14) were isolated from the alkaline hydrolysate of total saponins of the stems-leaves of Panax ginseng C.A. Meyer. Their chemical structures were elucidated by extensive spectroscopic analyses and comparison with the reported data. All 14 compounds were evaluated for their anti-proliferative activities against two human cancer cell lines (HL-60 and Hep-G2) and promotion activities of SIRT1. Compound 6 exhibited significant inhibitory activity in a concentration-dependent manner against HL-60 and Hep-G2 with the IC50 values of 10.32 and 24.33μM, respectively, and had comparable IC50 values with those of vinorelbine, a positive control agent. Meanwhile, compounds 1 and 6 were found to be a potential activator of SIRT1. The preliminary structure-activity relationship was also discussed based on the experimental data obtained.
authors.affiliation: 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, No. 38, Xueyuan Road, Haidian District, Beijing 100191, PR China.
authors.forename: Li-Yuan
authors.initials: LY
authors.lastname: Ma
authors.affiliation: 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, No. 38, Xueyuan Road, Haidian District, Beijing 100191, PR China.
authors.forename: Qi-Le
authors.initials: QL
authors.lastname: Zhou
authors.affiliation: 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, No. 38, Xueyuan Road, Haidian District, Beijing 100191, PR China. Electronic address: xwyang@bjmu.edu.cn.
authors.forename: Xiu-Wei
authors.initials: XW
authors.lastname: Yang
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004789:Enzyme Activation / Q000187:drug effects; D036145:Ginsenosides / Q000737:chemistry* / Q000494:pharmacology; D018922:HL-60 Cells; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D005894:Panax / Q000737:chemistry*; D018515:Plant Leaves / Q000737:chemistry*; D018547:Plant Stems / Q000737:chemistry*; D011492:Protein Hydrolysates / Q000737:chemistry; D012503:Saponins / Q000737:chemistry*; D056564:Sirtuin 1 / Q000378:metabolism*
chemical_list: C000612922:20(S)-ginsenoside-Rh1-6'-acetate; D000972:Antineoplastic Agents, Phytogenic; D036145:Ginsenosides; D011492:Protein Hydrolysates; D012503:Saponins; C000612923:ginsenoslaloside-I; C447939:SIRT1 protein, human; D056564:Sirtuin 1
keywords: 20(S)-Ginsenoside-Rh(1)-6′-acetate; Alkaline hydrolysate; Anti-proliferativity; Ginsenoslaloside-I; SIRT1 activator; Stems-leaves of Panax ginseng