Abstract
Minor ginsenosides, such as compound K, Rg3(S), which can be produced by deglycosylation of ginsenosides Rb1, showed strong anti-cancer effects. However, the anticancer effects of gypenoside LXXV, which is one of the deglycosylated shapes of ginsenoside Rb1, is still unknown due to the rarity of its content in plants. Here, we cloned and characterized a novel ginsenoside-transforming β-glucosidase (BglG167b) derived from Microbacterium sp. Gsoil 167 which can efficiently hydrolyze gypenoside XVII into gypenoside LXXV, and applied it to the production of gypenoside LXXV at the gram-scale with high specificity. In addition, the anti-cancer activity of gypenoside LXXV was investigated against three cancer cell lines (HeLa, B16, and MDA-MB231) in vitro. Gypenoside LXXV significantly reduced cell viability, displaying an enhanced anti-cancer effect compared to gypenoside XVII and Rb1. Taken together, this enzymatic method would be useful in the preparation of gypenoside LXXV for the functional food and pharmaceutical industries.
Highlights
One was homologous to glycoside hydrolase genes in glycoside hydrolase family 3 (GH3)
Showed similar anti-cancer effects with Rg3 (S) (Figure 6D), and higher than Rb1 and GypXVII, which have more attached glucose moieties (Figure 6A–C). It is the first report of the anti-cancer activity of gypenoside LXXV (GypLXXV), and the patent of the anti-cancer activity of GypLXXV against HeLa cells has been registered by this team [43]. These results demonstrate that deglycosylation contributes to improved anticancer activity, and the mechanism of increased anticancer effects requires further structure-related approaches
Ginsenoside standards that are over 98% purity, such as Rb1, Rb2, Rc, Rd, Rg3(S), Rh2(S), F2, Ginsenoside standards that are over 98% purity, such as Rb1, Rb2, Rc, Rd, Rg3 (S), Rh2 (S), F2, compound K (C-K), protopanaxadiol (PPD), Rg1, Re, Rg2(S), Rh1(S), and protopanaxatriol (PPT), were compound
Summary
Ginsenosides are considered as the main active ingredients responsible for pharmacological activities of the ginseng root, such as anti-cancer, anti-obesity, anti-inflammatory, antioxidant, and hepatoprotective activities [3,4,5,6,7]. The six major ginsenosides (Rb1 , Rb2 , Rc, Rd, Re, and Rg1 ) constitute more than 80% of the total ginsenosides in ginseng root, and various minor ginsenosides (Rg3 (S), Rh2 (S), F2 , compound K (C-K), Rg2 (S), Rh1 (S), F1 , protopanaxadiol (PPD) and protopanaxatriol (PPT), and gypenoside XVII (GypXVII)) that are deglycosylated from the major ginsenosides exist in smaller amounts in ginseng [8,9,10,11]. Major ginsenoside Rb1 is relatively abundant in ginseng, and it can be deglycosylated into rare minor ginsenosides (F2 , Rg3 (S), Rh2 (S), CK, PPD).
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