Abstract: Ginsenosides,the main pharmacologically active natural compounds in ginseng (Panax ginseng),have multiple medical effects such as anti-oxidative,anticancer,antiaging and other health-improving activities.Rh2 and Rg3 are rare ginsenosides which represent promising candidates for cancer prevention and therapy and have low toxicity.Recent research showed that β-D-glucosidase from fungi can convert major ginsenosides into rare ginsenosides via the hydrolyses of glucoside.In this review,the pathway of biosynthesizing ginsenosides,anti-cancer activities of different classes of ginsenosides were summarized and recent works on functional characterization of β-D-glucosidase were highlighted.These breakthroughs provided an inexpensive and efficient industrial platform for the manufacture of ginsenosides for clinical applications.

Key words: ginsenoside, &beta, -D-glucosidase, fungi, glycosylation modification