When ginseng water extract was incubated at 60degreesC in acidic conditions, its protopanaxadiol ginsenosides were transformed to ginsenoside Rg(3) and Delta(20)-ginsenoside Rg(3). However, protopanaxadiol glycoside ginsenosides Rb-1, Rb-2 and Rc isolated from ginseng were mostly not transformed to ginsenoside Rg(3) by the incubation in neutral condition. The transformation of these ginsenosides to ginsenoside Rg(3) and Delta(20)-ginsenoside Rg(3) was increased by increasing incubation temperature and time in acidic condition: the optimal incubation time and temperature for this transformation was 5 h and 60degreesC resepectively. The transformed ginsenoside Rg(3) and Delta(20)-ginsenoside Rg(3) were metabolized to ginsenoside Rh-2 and Delta(20)-ginsenoside Rh-2, respectively, by human fecal microflora. Among the bacteria isolated from human fecal microflora, Bacteroides sp., Bifidobacterium sp. and Fusobacterium sp. potently transformed ginsenoside Rg(3) to ginsenoside Rh-2. Acid-treated ginseng (AG) extract, fermented AG extract, ginsenoside Rh-2 and protopanaxadiol showed potent cytotoxicity against tumor cell lines. AG extract, fermented AG extract and protopanaxadiol potently inhibited the growth of Helicobacterpylori.