Pharmacological bioactivity of enzymatically bio-transformed ginsenosides

Many ginsenosides have shown positive effects, including anti-cancer potential and anti-inflammatory effects. Of note, protopanaxadiol (PPD) and protopanaxatriol (PPT) are not easily absorbed by the body through the digestive tract due to their hydrophilicity. From this point of view, the cytotoxic potencies of the hydrolysates of PPD and PPT on CRC are much stronger than their source compounds. Moreover, several minor ginsenosides that are absent naturally but have high disease ameliorative efficacy can be obtained from major ginsenoside by enzymatic hydrolysis. Therefore, the first aim of this study was to determine the effectiveness of the biotransformation of ginsenosides via enzymatic hydrolysis to improve their bioactivity. Second, the anti-inflammatory and anti-cancer effects of the raw and bio-transformed ginseng metabolites were determined in vitro. The results suggest that enzymes can effectively biotransform major ginsenosides (i.e., PPD and PPT) into minor ginsenosides (i.e., compound K) by hydrolyzing the β-glucosidic linkage. Moreover, the bio-transformed ginsenosides were effective in inhibiting the proliferation of HCT-116 cells and suppressing lipopolysaccharide-induced nitric oxide production in RAW 264.7 murine macrophages. Therefore, the enzymatic hydrolysis of ginsenosides can be employed to functionally produce hydrolysates with increased bioactivity.