Identification and evaluation of apoptotic compounds from Garcinia oligantha

Four new compounds, oliganthins A–D (1–4), and one known caged xanthone gaudichaudione H (5) were isolated from the leaves of Garcinia oligantha. All of the five compounds were evaluated for their apoptosis-inducing effects. All of them induced cell apoptosis at 10μM or lower concentrations. The apo...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (6), p.2350-2353
Main Authors: Gao, Xue-Mei, Yu, Ting, Cui, Ming-zhu, Pu, Jian-Xin, Du, Xue, Han, Quan-bin, Hu, Qiu-fen, Liu, Tian-Cheng, Luo, Kathy Qian, Xu, Hong-Xi
Format: Article
Language:English
Subjects:
Anticancer drug
antineoplastic agents
Antineoplastic Agents, Phytogenic - chemistry
Antineoplastic Agents, Phytogenic - isolation & purification
Antineoplastic Agents, Phytogenic - pharmacology
Apoptosis
Apoptosis - drug effects
Biological and medical sciences
biosensors
Blotting, Western
Caspase 3 - genetics
Caspase 3 - metabolism
Caspase-3
cell growth
Female
fluorescence
Garcinia
Garcinia - chemistry
Garcinia oligantha
Gene Expression
Genes, Reporter
HeLa Cells
Humans
inhibitory concentration 50
Magnetic Resonance Spectroscopy
Medical sciences
Pharmacology. Drug treatments
Plant Extracts - chemistry
Plant Stems - chemistry
Poly(ADP-ribose) Polymerases - genetics
Poly(ADP-ribose) Polymerases - metabolism
spectroscopy
stems
Uterine Cervical Neoplasms - drug therapy
Uterine Cervical Neoplasms - pathology
Western blotting
Xanthenes - chemistry
Xanthenes - isolation & purification
Xanthenes - pharmacology
Xanthone
Xanthones - chemistry
Xanthones - isolation & purification
Xanthones - pharmacology
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:Four new compounds, oliganthins A–D (1–4), and one known caged xanthone gaudichaudione H (5) were isolated from the leaves of Garcinia oligantha. All of the five compounds were evaluated for their apoptosis-inducing effects. All of them induced cell apoptosis at 10μM or lower concentrations. The apoptotic activity of oliganthins A, B and gaudichaudione H were further confirmed by detecting the cleavage of PARP using the method of Western blot. Moreover, the values of IC50 were measured for all four compounds on HeLa cells using the MTT assay. Four new compounds, oliganthins A–D (1–4), and one known caged xanthone gaudichaudione H (5) were isolated from the stems of Garcinia oligantha. The structures of the new compounds were elucidated by spectroscopic evidences. All of the five compounds were evaluated for their apoptosis-inducing effects using HeLa-C3 cells which have been genetically engineered to produce a fluorescent biosensor capable of detecting caspase-3 activation. All of them induced cell apoptosis at 10μM or lower concentrations. The apoptotic activity of oliganthins A, B and gaudichaudione H were further confirmed by detecting the cleavage of PARP, which is the substrate of activated caspase-3, in these compounds-treated cells using the method of Western blot. Moreover, the values of IC50 were measured for all five compounds on HeLa cells using the MTT assay. Among them, gaudichaudione H had the lowest IC50 value of 0.90μM, while the other four new compounds had IC50 values of 1.58, 1.52, 4.15, and 7.82μM, respectively. These results show that gaudichaudione H has the strongest apoptosis-inducing effect and cell growth inhibition effect among these xanthones and it may have the potential to be developed into a new anticancer agent.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.01.068