New SIRT1 activator from alkaline hydrolysate of total saponins in the stems-leaves of Panax ginseng

[Display omitted] 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 sapon...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (22), p.5321-5325
Main Authors: Ma, Li-Yuan, Zhou, Qi-Le, Yang, Xiu-Wei
Format: Article
Language:English
Subjects:
20(S)-Ginsenoside-Rh1-6′-acetate
Alkaline hydrolysate
Anti-proliferativity
Antineoplastic Agents, Phytogenic - chemistry
Antineoplastic Agents, Phytogenic - pharmacology
Cell Proliferation - drug effects
Enzyme Activation - drug effects
Ginsenosides - chemistry
Ginsenosides - pharmacology
Ginsenoslaloside-I
Hep G2 Cells
HL-60 Cells
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Molecular Structure
Neoplasms - drug therapy
Panax - chemistry
Plant Leaves - chemistry
Plant Stems - chemistry
Protein Hydrolysates - chemistry
Saponins - chemistry
SIRT1 activator
Sirtuin 1 - metabolism
Stems-leaves of Panax ginseng
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.09.039