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 Rb₁, Rb₂, Rb₃, 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 °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 ¹H and ¹³C 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.