Constituents isolated from Cordyceps militaris suppress enhanced inflammatory mediator's production and human cancer cell proliferation.
OBJECTIVE
The purpose of this study is to isolate the pure compounds from the extracts of Cordyceps militaris obtained through solid-state cultivation process, and evaluate their anti-inflammatory and anticancer properties.


METHODS
Silica gel column chromatographic purification of Cordyceps militaris extracts resulted in the isolation of 10 pure compounds (1-10). The compounds 1-10 were examined for their growth inhibitory properties against nitric oxide (NO), tumor necrosis factor (TNF)-alpha and interleukin (IL)-12 enhanced production from LPS/IFN-gamma-stimulated macrophages. Additionally, the anti-proliferation effects of 1-10 on human cancer cell lines, colon (colon 205), prostate (PC-3), and hepatoma (HepG2) cells were also analyzed.


RESULTS
Compound 8 displayed potent growth inhibition on NO, TNF-alpha and IL-12 production with an IC(50) value of 7.5, 6.3, and 7.6 microg/ml, respectively. A similar inhibitory trend on these inflammatory mediators was observed for 3, 7, 9 and 10 with an IC(50) values ranging from 10.8 to 17.2 microg/ml. On the other hand, compounds 3 and 8 were potent anti-proliferative agents with an IC(50) value of 35.6 and 32.6 microg/ml toward PC-3 and colon 205 cell lines, respectively. The compounds 1 and 2 showed potent anti-proliferation in PC-3 and colon 205 cells, while only 3 displayed such effect in HepG2 cells.


CONCLUSIONS
The present study provides scientific supporting information for the ethnopharmacological use of Cordyceps militaris as an anti-inflammatory and anticancer agent.
Rao
Yerra Koteswara
YK
Institute of Biochemical Sciences and Technology, Chaoyang University of Technology, Taichung County, Wufeng, Taiwan, ROC.
Fang
Shih-Hua
SH
Wu
Wen-Shi
WS
Tzeng
Yew-Min
YM
D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D001688:Biological Products / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D032661:Cordyceps / Q000737:chemistry*; D006801:Humans; D018836:Inflammation Mediators / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D007371:Interferon-gamma; D018664:Interleukin-12 / Q000037:antagonists & inhibitors; D008070:Lipopolysaccharides; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D009569:Nitric Oxide / Q000037:antagonists & inhibitors; D008517:Phytotherapy; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors
D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D001688:Biological Products; D018836:Inflammation Mediators; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha; D018664:Interleukin-12; D009569:Nitric Oxide; D007371:Interferon-gamma