Inhibitory activities of Lignum Sappan extractives on growth and growth-related signaling of tumor cells / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 607-612, 2014.
Article
in English
| WPRIM
| ID: wpr-812227
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Sarcoma
/
Benzopyrans
/
Plant Extracts
/
Signal Transduction
/
NF-kappa B
/
Interleukin-6
/
Tumor Necrosis Factor-alpha
/
Caesalpinia
/
Therapeutic Uses
Type of study:
Prognostic study
Limits:
Animals
/
Humans
/
Male
Language:
English
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2014
Type:
Article
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