• The Journal of Traditional Korean Medicine
• /
• v.15 no.1
• /
• pp.97-105
• /
• 2006

To study on antioxidant effects in the liver of 40-week-old mouse, the sample were orally pretreated 5mg/kg/day for 5 days with red ginseng saponin components(total saponin, protopanaxadiol saponin, protopanaxatriol saponin, ginsenoside-Rd, ginsenoside-Re, compound-K) for 5 days. The ability of saponin to protect the mouse liver from oxidative damage was examined by determining the activity of superoxide dismutase(SOD), glutathione peroxidase(GPx) and the contents of glutathione, the level of malondialdehyde, The only protopanaxadiol among the ginseng saponin fractions was significantly increased the hepatic SOD activity(p<0.01). The red ginseng saponin induced a slight increase of GPx activity, especially ginsenoside Rd, compound K and protopanaxatriol treatments significantly increased its activity. The content of glutathione was significantly increased by total saponin, protopanaxadiol and ginsenoside Rd(p<0.01), but the oxidized glutathione level was lowered in all the red ginseng saponin. Finally, the level of malondialdehyde was significantly decreased by ginsenoside Rd and protopanaxadiol. In conclusion, protopanaxadiol and ginsenoside Rd among the saponin fraction were especially increased in the activity of hepatic antioxidative enzyme and decreased the lipid peroxidation that was expressed in term of MDA formation. This comprehensive antioxidant effects of red ginseng saponin seems to be by a certain action of saponin other than a direct antioxidant action.

• Journal of Ginseng Research
• /
• v.46 no.4
• /
• pp.505-514
• /
• 2022

Background: The roots of Panax ginseng contain two types of tetracyclic triterpenoid saponins, namely, protopanaxadiol (PPD)-type saponins and protopanaxatiol (PPT)-type saponins. In P. ginseng, the protopanaxadiol 6-hydroxylase (PPT synthase) enzyme catalyses protopanaxatriol (PPT) production from protopanaxadiol (PPD). In this study, we constructed homozygous mutant lines of ginseng by CRISPR/Cas9-mediated mutagenesis of the PPT synthase gene and obtained the mutant ginseng root lines having complete depletion of the PPT-type ginsenosides. Methods: Two sgRNAs (single guide RNAs) were designed for target mutations in the exon sequences of the two PPT synthase genes (both PPTa and PPTg sequences) with the CRISPR/Cas9 system. Transgenic ginseng roots were generated through Agrobacterium-mediated transformation. The mutant lines were screened by ginsenoside analysis and DNA sequencing. Result: Ginsenoside analysis revealed the complete depletion of PPT-type ginsenosides in three putative mutant lines (Cr4, Cr7, and Cr14). The reduction of PPT-type ginsenosides in mutant lines led to increased accumulation of PPD-type ginsenosides. The gene editing in the selected mutant lines was confirmed by targeted deep sequencing. Conclusion: We have established the genome editing protocol by CRISPR/Cas9 system in P. ginseng and demonstrated the mutated roots producing only PPD-type ginsenosides by depleting PPT-type ginsenosides. Because the pharmacological activity of PPD-group ginsenosides is significantly different from that of PPT-group ginsenosides, the new type of ginseng mutant producing only PPD-group ginsenosides may have new pharmacological characteristics compared to wild-type ginseng. This is the first report to generate target-induced mutations for the modification of saponin biosynthesis in Panax species using CRISPR-Cas9 system.

• YAKHAK HOEJI
• /
• v.38 no.4
• /
• pp.425-429
• /
• 1994

The genuine aglycone, 20(S)-protopanaxadiol, obtained from the leaves of Panax ginseng as a result of direct alkaline treatment was isolated and characterized by spectroscopic evidences. The study on the yield of genuine aglycone which is produced from the treatment of some kinds of alkali was carried out. $Ginsenoside-Rh_2$ was synthesized by conjugation of 2,3,4,6-tetra-O-acetyl-${\alpha}$-D-glucopyranosyl bromide to 20(S)-protopanaxadiol in the presence of silver carbonate and cadmium cabonate. The preparation of $ginsenoside-Rh_2$ by this method is a new one which the yield of this saponin can be improved in the mild condition.

• YAKHAK HOEJI
• /
• v.35 no.5
• /
• pp.432-437
• /
• 1991

A mixture of 20(R)- and 20(S)-ginsenoside Rg$_{3}$ was obtained under mild acidic hydrolysis from protopanaxadiol saponins, ginsenosides Rb$_{1}$, Rb$_{2}$, Rc and Rd. The product was acetylated to give the peracetates, which were further converted into 20(R)-ginsenoside Rg$_{3}$, 20(S)-ginsenoside Rg$_{3}$, 20(R)-ginsenoside Rh$_{2}$ and 20(S)-ginsenoside Rh$_{2}$ by the direct alkaline treatment depending upon two kinds of temperature conditions respectively. The structure and physicochemical properties of a prosapogenin, 20(R)-ginsenoside Rh$_{2}$, were investigated.

• Journal of Pharmaceutical Investigation
• /
• v.16 no.4
• /
• pp.135-138
• /
• 1986

Ginseng total saponins(GS), protopanaxadiol saponins(PD) and protopanaxadiol saponins(PT) antagonized the analgesia in mice induced by morphine. The administrations of 2,4-dihydroxyphenylalanine, and 5-hydroxytryptophan reduced the GS, PD and PT antagonisms of morphine analgesia. Possible mechanisms involved in the antagonistic actions of GS, PD and PT on morphine analgesia were described.

• Proceedings of the Korean Society of Toxicology Conference
• /
• 2001.10a
• /
• pp.139-140
• /
• 2001

Ginseng saponins (ginsenosides) have been regarded as principal components responsible for the majority of pharmacological activities exerted by ginseng. IH-901, an intestinal bacterial metabolite derived from the protopanaxadiol saponin of Panax ginseng C.A. Meyer, has been reported to have anti-tumor effects including inhibition of angiogenesis, invasion and metastasis, as well as induction of tumor cell apoptosis. (omitted)

• Food Science and Biotechnology
• /
• v.18 no.1
• /
• pp.253-256
• /
• 2009

The purpose of the study was to develop a new process to manufacture ginseng extract containing saponin aglycon of high concentration. The process to transform saponin glycosides to saponin aglycon was analyzed by high performance liquid chromatography (HPLC). GCK-1 (open cultured mixture for 1 day at $42^{\circ}C$) had the highest content of protopanaxadiol (0.662%). However, other mixtures (GCK-2, 3, 4, 5, and 6) had less than 0.152% in the content of protopanaxadiol. In case of fermentation by inoculation of Bacillus natto, BNG-5 (B. natto inoculated mixture for 5 days at $42^{\circ}C$) showed the highest content of protopanaxadiol (0.364%). Other mixtures (BNG-1, 2, 3, 4, and 6) also showed the high content of more than 0.2% in protopanaxadiol. B. natto inoculation or open culture fermentation with soybean transformed ginseng saponin glycosides into saponin aglycon.

• Journal of Ginseng Research
• /
• v.40 no.1
• /
• pp.47-54
• /
• 2016

Background: The roots of Panax ginseng contain noble tetracyclic triterpenoid saponins derived from dammarenediol-II. Dammarene-type ginsenosides are classified into the protopanaxadiol (PPD) and protopanaxatriol (PPT) groups based on their triterpene aglycone structures. Two cytochrome P450 (CYP) genes (CYP716A47 and CYP716A53v2) are critical for the production of PPD and PPT aglycones, respectively. CYP716A53v2 is a protopanaxadiol 6-hydroxylase that catalyzes PPT production from PPD in P. ginseng. Methods: We constructed transgenic P. ginseng lines overexpressing or silencing (via RNA interference) the CYP716A53v2 gene and analyzed changes in their ginsenoside profiles. Result: Overexpression of CYP716A53v2 led to increased accumulation of CYP716A53v2 mRNA in all transgenic roots compared to nontransgenic roots. Conversely, silencing of CYP716A53v2 mRNA in RNAi transgenic roots resulted in reduced CYP716A53v2 transcription. HPLC analysis revealed that transgenic roots overexpressing CYP716A53v2 contained higher levels of PPT-group ginsenosides ($Rg_1$, Re, and Rf) but lower levels of PPD-group ginsenosides (Rb1, Rc, $Rb_2$, and Rd). By contrast, RNAi transgenic roots contained lower levels of PPT-group compounds and higher levels of PPD-group compounds. Conclusion: The production of PPD- and PPT-group ginsenosides can be altered by changing the expression of CYP716A53v2 in transgenic P. ginseng. The biological activities of PPD-group ginsenosides are known to differ from those of the PPT group. Thus, increasing or decreasing the levels of PPT-group ginsenosides in transgenic P. ginseng may yield new medicinal uses for transgenic P. ginseng.

• Journal of Ginseng Research
• /
• v.30 no.4
• /
• pp.181-187
• /
• 2006

Protopanaxadiol (PPD) is a mixture of protopanaxadiol type saponins with a dammarane skeleton, from Korean red ginseng (Panax ginseng C.A. Meyer; Araliaceae). Korean ginseng is well-known herb to treat almost all kinds of diseases in Oriental medicine. This herb was particularly prescribed for treatment various inflammatory diseases, including rheumatoid arthritis, atherosclerosis, and diabetes mellitus, for centuries. To understand the efficacy of ginseng against inflammatory diseases, we aimed to show anti-inflammatory activities of the PPD in murine macrophage cell line, RAW264.7 cells using nitric oxide (NO) production assay and the expressions of pro-inflammatory cytokines, such as tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$), interleukin-$1{\beta}$ (IL-$1{\beta}$), and IL-6, and monocyte chemotactic protein-1 (MCP-1). We found that PPD saponin significantly blocked LPS ($1{\mu}g/ml$)-induced NO production in a dose-dependent manner. In addition, PPD abrogated the expressions of LPS-induced pro-inflammatory cytokines, such as IL-$1{\beta}$ and MCP-1. Moreover, cyclooxygenase (COX)-2, a critical enzyme to produce prostaglandin E2 (PGE2), was significantly inhibited by PPD in LPS-activated RAW264.7 cells. Taken together, these results suggested that anti-inflammatory efficacy of Korean red ginseng on inflammatory diseases is, at least, due to the NO inhibitory activity and the inhibition of the expressional level of inflammatory cytokines and/or mediators.

• Archives of Pharmacal Research
• /
• v.27 no.1
• /
• pp.61-67
• /
• 2004

When ginseng water extract was incubated at $60^{\circ}C$ 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 $60^{\circ}C$ 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., and 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 Helicobacter pylori.