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Panax ginseng C. A. Meyer (PG), a well-known traditional Chinese medicine, has been widely used as a panacea in treatment of human diseases for a long time. In this study, we exerted systems biology and bioinformatics methods for the first time and analyzed the “giant components” of PG in the global component-target interaction network. Based upon this network, we further confirmed several key components and their related targets (e.g., NF-κB, COX-2, Bax, NOS, JNK, p21 and MMP3). Additionally, we demonstrated that ginsenosides and key targets were involved in several cancer-related pathways, which indicated that ginsenosides might play crucial roles in cancer treatments. Interestingly, we also found that the component-target network might provide new clues for further predicting new targets and elucidating the relationships amongst the network and side-effects. In conclusion, these inspiring findings demonstrate that the versatile effects of PG are mostly ascribed to the comprehensive interactions amongst ginsenosides and their pivotal targets.