Ginseng was fermented by Aspergillus oryzae to search metabolites on the basis of increased biological activity and modified structure. From this research, two biotransformed compounds (WC2-2-1 and WC2-2-2) were detected and isolated through several chromatographic techniques. WC2-2-2 was confirmed to biologically active compound K by TLC, HPLC, and mass spectroscopy, while WC2-2-1 was going to be identified until now. In biological activity, both WG2-2-1 and WG2-2-2 exhibit the cytotoxicity on PC-3 cells, but WG2-2-2 was more active than WG2-2-1. It is supposed that WG2-2-1 is an intermediate metabolite transforming to final WG2-2-2, compound K.