Abstract: Objective: To extract and isolate bioactive components from the fruiting bodies of Codyceps militaris by systematic solvent method and determine the antitumor and antiviral activities of chloroform extract from the fruiting bodies of Codyceps militaris and its fractions soluble in ethyl acetate and ethanol. Methods: The antiviral activities of extracts on FLU-A, HSV-I and HSV-II viruses were assessed by cytopathic effect (CPE) method. The 50% toxic concentration (TC50), 50% inhibitory concentration (IC50) and selective index (SI) of the chloroform extract and its two fractions were determined by Reed-Muench method. Their antitumor activities were evaluated based on their inhibitory rates on tumor cell proliferation such as K562 and MCF-7 cells, determined by Alamar Blue method. Results: The antiviral activity assay showed that the chloroform extract had the best antiviral activity on HSV-I and HSV-II viruses with an IC50 of 194.01μg/mL and 173.34μg/mL, and an SI of higher than 1.29 and 1.44, respectively. The chloroform extract and its two fractions had no inhibitory effect on FLU-A virus but had obvious antitumor activity on K562 cells at the concentrations of 50 μg/mL and 200 μg/mL in and the ethanol-soluble fraction ranked first in decreasing order of anti-K562 cell activity, followed by the chloroform extract and its ethyl acetate-soluble fraction. Only the chloroform extract revealed an inhibitory effect on MCF-7 cells with inhibitory rates of (9.6 ± 3.0)%, (46.1 ± 8.9)%, and (68.5 ± 9.2)% at the concentrations of 10, 50μg/mL and 200 μg/mL, respectively, in a dose-dependent manner. Conclusion: The chloroform extract has higher antitumor and antiviral activities than its two fractions so that it will provide a potential resource for natural antitumor and antiviral agents.

Key words: Codyceps militaris, antitumor activity, antiviral activity, systematic solvent extraction