Transformation of bioactive compounds by Fusarium sacchari fungus isolated from the soil-cultivated ginseng.

Ginsenoside bioactive compounds, namely, compound K (C-K), compound Mx (C-Mx), and ginsenoside Mc (G-Mc), were the metabolites of ginsenosides Rb 1, Rb 2, Rb 3, and Rc by intestinal microflora of humans or rats, microorganisms, and enzymes, and C-K showed beneficial effects in vitro and in vivo as an antitumoral agent. The objective of this work was to explore an efficient procedure for biotransformation of these bioactive compounds. Thus, a filamentous fungus, Fusarium sacchari, was first obtained from the soil-cultivated ginseng, which was verified to possess a potent capacity of transformation of C-K, C-Mx, and G-Mc. The optimal biotransformation conditions of F. sacchari with C-K, C-Mx, and G-Mc were obtained as follows: transforming temperature, 30 degrees C; transforming time, 6 days; rotary speed, 160 rpm; pH of the medium, 5.5. HPLC analysis indicated that these three bioactive compounds were key metabolites and their structures were confirmed by (1)H and (13)C NMR analysis. Moreover, the in vitro antitumor activities of C-K, C-Mx, and G-Mc and the in vivo antitumor activities of the transformed product mainly containing these compounds were also evaluated. Among C-K, C-Mx, and G-Mc, C-K exhibited the most potent antitumor activities. The in vivo study showed that the transformed products by F. sacchari had much more antitumor activity than those of commonly used ginsenoside Rg3 and Paclitaxel.