Inhibitory activities of Lignum Sappan extractives on growth and growth-related signaling of tumor cells.
10.1016/S1875-5364(14)60092-3
- Author:
Qing ZHANG
1
;
Jing-Li LIU
1
;
Xiao-Man QI
1
;
Chun-Ting QI
1
;
Qiang YU
2
Author Information
1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address: qyu@sibs.ac.cn.
- Publication Type:Journal Article
- Keywords:
Anti-tumor activity;
Caesalpinia sappan L.;
Cell cycle blocker;
Lignum Sappan;
Signaling pathway inhibitor;
Synergy
- MeSH:
Animals;
Antineoplastic Agents, Phytogenic;
pharmacology;
therapeutic use;
Benzopyrans;
pharmacology;
therapeutic use;
Caesalpinia;
Cell Cycle Checkpoints;
drug effects;
Chalcones;
pharmacology;
therapeutic use;
Hep G2 Cells;
Humans;
Interleukin-6;
metabolism;
Male;
Mice, Inbred BALB C;
Mitosis;
drug effects;
NF-kappa B;
metabolism;
Phytotherapy;
Plant Extracts;
pharmacology;
therapeutic use;
STAT3 Transcription Factor;
metabolism;
Sarcoma;
drug therapy;
metabolism;
Signal Transduction;
Tumor Necrosis Factor-alpha;
metabolism
- From:
Chinese Journal of Natural Medicines (English Ed.)
2014;12(8):607-612
- CountryChina
- Language:English
-
Abstract:
AIM:To investigate the active constituents of Lignum Sappan (Caesalpinia sappan L.) on growth-related signaling and cell mitosis.
METHOD:The influence of the ethyl acetate (EtOAc) extract of Lignum Sappan and its constituents on growth-related signaling were evaluated by a luciferase assay in cells stably-transfected with NF-κB, STAT1, or STAT3 responsive luciferase reporter plasmid. The inhibitory effect on the cell cycle was determined by flow cytometric analysis. The anti-tumor activities were assessed in vitro and in vivo.
RESULTS:The EtOAc extract of Lignum Sappan had inhibitory activities on growth-related signaling and cell mitosis. Three major active compounds were sappanchalcone, brazilin, and butein. Sappanchalcone blocked cell cycle progression in the G2/M phase, brazilin inhibited TNFα/NF-κB signaling, while butein inhibited IL-6/STAT3 signaling, as well as TNFα/NF-κB signaling. The three compounds all demonstrated cytotoxic activities against human tumor cells in vitro. In a S180 tumor cell-bearing mice model, the anti-tumor efficacy of the EtOAc extract was better than the individual compounds acting alone.
CONCLUSION:These results indicate that Lignum Sappan contains multiple active compounds with different antitumor activities, which act synergistically to enhance their anti-tumor effects. The EtOAc extract of Lignum Sappan may be better than individual active constituent as a novel medicine for the treatment of cancer.
