Constituents isolated from Cordyceps militaris suppress enhanced inflammatory mediator's production and human cancer cell proliferation

• Published in: Journal of ethnopharmacology 2010-09, Vol.131 (2), p.363-367
• Main Authors: Rao, Yerra Koteswara, Fang, Shih-Hua, Wu, Wen-Shi, Tzeng, Yew-Min
• Format: Article
• Language: English
• Subjects: anti-inflammatory activity; Anti-Inflammatory Agents - isolation & purification; Anti-Inflammatory Agents - pharmacology; Antineoplastic Agents - isolation & purification; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Biological and medical sciences; Biological Products - isolation & purification; Biological Products - pharmacology; Biological Products - therapeutic use; Cell Line, Tumor; cell proliferation; Cell Proliferation - drug effects; chemical composition; Cordyceps; Cordyceps - chemistry; Cordyceps militaris; extracts; General pharmacology; Human cancer cells proliferation; human cell lines; Humans; inflammation; Inflammation Mediators - antagonists & inhibitors; Inflammatory mediators; Inhibitory Concentration 50; Interferon-gamma; interferons; interleukin-12; Interleukin-12 - antagonists & inhibitors; Lipopolysaccharides; macrophages; Macrophages - drug effects; Macrophages - metabolism; Medical sciences; medicinal properties; neoplasms; Neoplasms - drug therapy; Neoplasms - metabolism; nitric oxide; Nitric Oxide - antagonists & inhibitors; pharmacognosy; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Phytoconstituents; Phytotherapy; tumor necrosis factor-alpha; Tumor Necrosis Factor-alpha - antagonists & inhibitors
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2010.07.020

In traditional Chinese medicine, Cordyceps militaris is widely used for various ethnomedical conditions including inflammation and cancer complications. In this report, silica gel column chromatographic purification of Cordyceps militaris extracts resulted in the isolation of 10 pure compounds. These compounds displayed potent growth inhibition on nitric oxide, tumor necrosis factor-α and interleukin-12 production from LPS/IFN-γ-stimulated macrophages, in addition to their anti-proliferation effect against human cancer cells. 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. 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)-α and interleukin (IL)-12 enhanced production from LPS/IFN-γ-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. Compound 8 displayed potent growth inhibition on NO, TNF-α and IL-12 production with an IC 50 value of 7.5, 6.3, and 7.6 μg/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 μg/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 μg/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. The present study provides scientific supporting information for the ethnopharmacological use of Cordyceps militaris as an anti-inflammatory and anticancer agent.