• Biomolecules & Therapeutics
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• v.7 no.2
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• pp.145-152
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• 1999

In an attempt to elucidate the anti-inflammatory action of ginseng total saponin, protopanaxadiol and protopanaxatriol, the anti-inflammatory activity of three compounds was investigated under various acute and chronic inflammatory models. The blood vessel permeability was slightly inhibited by total saponin and protopanaxatriol treatments. Granuloma formation induced by 2% carrageenan was inhibited by total saponin and protopanaxatriol. The cotton-pellet granuloma formation was significantly inhibited by intraperitoneal injection of total saponin. Total saponin and protopanaxadiol inhibited leukocyte emigration and protein exudation in CMC-induced pouch but protopanaxauiol increased leukocyte emigration. The swelling of rat hind paw induced by 1% carrageenan was significantly inhibited by total saponin, protopanaxadiol and protopanaxatriol both single and 2 weeks treatments. Total saponin, protopanaxadiol and protopanaxatriol decreased the anti-inflammatory activity in adrenalectomized rat. Our results suggest that total saponin, protopanaxadiol and protopanaxatriol have potent anti-inflammatory activity, this may be mediated in part through stimulation of adrenal glands.

• Journal of Ginseng Research
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• v.5 no.1
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• pp.41-48
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• 1981

Total saponin, protopanaxadiol-saponin and protopanaxatriol-saponin were isolated and purified from the side roots of red ginseng. After we administered them orally into rats during 5 weeks, we observed their effects on lipid and glucose content in rat serum. The change in body weight of protopanaxatriol- saponin treated group was slightly larger than those of other groups. Total lipid content in total saponin treated group showed an increase of about 20 % over that in control group. However, protopanaxadiol-saponin and protopanaxatriol- saponin treated groups showed no change. While triglyceride content in total saponin treated group decreased 29oyo compared to it s content in control group, its content in protopanaxatriol-saponin treated group increased 45%. Three saponin treated groups showed lower value than control group in total ant free cholesterol levels. While glucose content in total saponin treated group decreased slightly, that in Protopanaxadiol-saponin treated group decreased slightly compared to that in control group. And protopanaxatriol- saponin trented group showed the significant decrease of 25%. From these results, it is supposed that total saponin accelerates the conversion of lipid into glucose and that protopanaxatriol- saponin accelerates the conversion of glucose into lipid.

• Journal of Ginseng Research
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• v.5 no.1
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• pp.49-55
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• 1981

The effects of total, protopanaxadiol-and protopanaxatriol-saponins on the in vitro activities of several enzymes in rat serum were observed Alkaline phosphatase activity was increased 61 % by total saponin and 46% by protopanaxatriol-saponin, compared to control group. While SCOT activity was slightly decreased by total saponin and protopanaxatriol- saponin, it was slightly increased by Protopanaxadiol-saponin And while SCPT activity was slightly decreased by total saponin, it was increased by protopanaxadiol-saponin and protopanaxatriol-saponin. Creatine phosphokinase activity had a tendency to be increased by protopanaxatriol-saponin. Lactate dehydrogenase activities were increased in three saponin treated groups, but those were nonignificant. Compared to the control group, lipase activity was increased by all saponin samples. It was increased 157% by total saponin The increase in lipase activity by total saponin corresponded with the decrease in serum t total lipid by total saponin .

• Journal of Ginseng Research
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• v.21 no.1
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• pp.35-38
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• 1997

We investigated the effects of ginseng protopanaxadiol (PD) and protopanaxatriol (PT) saponins on the spontaneous contractility of intestine. Treatment with PD saponins showed a slight inhibition of spontaneous contraction of rabbit jejunum. In contrast, PT saponins showed much larger inhibition with dose-dependent manner in a range of 25~250 $\mu\textrm{g}$/ml. The inhibitory effect by PT saponins was not desensitized with continuous presence of PT saponins for several minutes. In addition, leu-enkephalin (1 PM) also inhibited the spontaneous contraction of rabbit jejunum but the in- hibition by leu-enkephalin was desensitized rapidly. The presence of PT saponins prevented the desenstization induced by leu-enkephalin. In conclusion, we found that PT saponins exert inhibition of spontaneous contractility of rabbit jejunum and the pattern of inhibition is different from that of opioid.

• Archives of Pharmacal Research
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• v.24 no.4
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• pp.297-299
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• 2001

This study investigated the effect that some polyacetylenes and protopanaxatriol, which were isolated from heated ginseng (family Araliaceae), have on inhibiting Helicobacter pylori (HP) growth. Among the compounds tested, panaxytriol was quite effective in inhibiting HP growth with an MIC of 50 ${\mu}g/ml$. Cinsenoside Rhl and protopanaxatriol weakly inhibited $H^{+}/K^{+}$-ATPase from a rat stomach.

• Journal of Microbiology and Biotechnology
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• v.28 no.2
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• pp.255-261
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• 2018

Aglycon protopanaxatriol (APPT) has valuable pharmacological effects such as memory enhancement and tumor inhibition. ${\beta}$-Glycosidase from the hyperthermophilic bacterium Dictyoglomus turgidum (DT-bgl) hydrolyzes the glucose residues linked to APPT, but not other glycoside residues. ${\beta}$-Glycosidase from the hyperthermophilic bacterium Pyrococcus furiosus (PF-bgl) hydrolyzes the outer sugar at C-6 but not the inner glucose at C-6 or the glucose at C-20. Thus, the combined use of DT-bgl and PF-bgl is expected to increase the biotransformation of PPT-type ginsenosides to APPT. We optimized the ratio of PF-bgl to DT-bgl, the concentrations of substrate and enzyme, and the reaction time to increase the biotransformation of ginsenoside Re and PPT-type ginsenosides in Panax ginseng leaf extract to APPT. DT-bgl combined with PF-bgl converted 1.0 mg/ml PPT-type ginsenosides in ginseng leaf extract to 0.58 mg/ml APPT without other ginsenosides, with a molar conversion of 100%. We achieved the complete biotransformation of ginsenoside Re and PPT-type ginsenosides in ginseng leaf extract to APPT by the combined use of two ${\beta}$-glycosidases, suggesting that discarded ginseng leaves can be used as a source of the valuable ginsenoside APPT. To the best of our knowledge, this is the first quantitative production of APPT using ginsenoside Re, and we report the highest concentration and productivity of APPT from ginseng extract to date.

• Journal of Microbiology and Biotechnology
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• v.27 no.9
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• pp.1559-1565
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• 2017

Naturally occurring ginsenoside F1 (20-O-${\beta}$-$\text\tiny{D}$-glucopyranosyl-20(S)-protopanaxatriol) is rare. Here, we produced gram-scale quantities of ginsenoside F1 from a crude protopanaxatriol saponin mixture comprised mainly of Re and Rg1 through enzyme-mediated biotransformation using recombinant ${\beta}$-glucosidase (BgpA) cloned from a soil bacterium, Terrabacter ginsenosidimutans Gsoil $3082^T$. In a systematic step-by-step process, the concentrations of substrate, enzyme, and NaCl were determined for maximal production of F1. At an optimized NaCl concentration of 200 mM, the protopanaxatriol saponin mixture (25 mg/ml) was incubated with recombinant BgpA (20 mg/ml) for 3 days in a 2.4 L reaction. Following octadecylsilyl silica gel column chromatography, 9.6 g of F1 was obtained from 60 g of substrate mixture at 95% purity, as assessed by chromatography. These results represent the first report of gram-scale F1 production via recombinant enzyme-mediated biotransformation.

• Journal of Ginseng Research
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• v.39 no.3
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• pp.189-198
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• 2015

Background: Antiallergic effect of 20(S)-protopanaxatriol (PPT), an intestinal metabolite of ginseng saponins, was investigated in guinea pig lung mast cells and mouse bone marrow-derived mast cells activated by a specific antigen/antibody reaction. Methods: Increasing concentrations of PPT were pretreated 5 min prior to antigen stimulation, and various inflammatory mediator releases and their relevant cellular signaling events were measured in those cells. Results: PPT dose-dependently reduced the release of histamine and leukotrienes in both types of mast cells. Especially, in activated bone marrow-derived mast cells, PPT inhibited the expression of Syk protein, cytokine mRNA, cyclooxygenase-1/2, and phospholipase $A_2$ ($PLA_2$), as well as the activities of various protein kinase C isoforms, mitogen-activated protein kinases, $PLA_2$, and transcription factors (nuclear factor-${\kappa}B$ and activator protein-1). Conclusion: PPT reduces the release of inflammatory mediators via inhibiting multiple cellular signaling pathways comprising the $Ca^{2+}$ influx, protein kinase C, and $PLA_2$, which are propagated by Syk activation upon allergic stimulation of mast cells.

• Korean Journal of Pharmacognosy
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• v.26 no.4
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• pp.360-367
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• 1995

The metabolism of ginseng saponins by human intestinal bacteria was studied using human feces under anaerobic culture conditions. $Ginsenoside-Rb_1$, $-Rb_2$ and -Rc(protopanaxadiol type) were mainly metabolized to compound-K(C-K), $20-O-[{\alpha}-L-arabinopyranosyl(1{\rightarrow}6)-{\beta}-{_D}-glucopyranosyl]-20(S)-protopanaxadiol(compound-Y,\;C-Y)$, $20-O-[{\alpha}-L-arabinopyranosyl(1{\rightarrow}6)-{\beta}-{_D}-glucopyranosyll-20(S)-protopanaxadiol(ginsenosied-MC,{\;}MC)$, respectively, and $ginsenoside-Rg_1$ and -Re(protopanaxatriol type) to their aglycon, 20(S)-protopanaxatriol, though the pathway and rate of the metabolism were affected by fermentation medium. C-K was not decomposed any more, while C-Y and Mc were both gradually hydrolyzed to C-K.

• YAKHAK HOEJI
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• v.29 no.4
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• pp.188-192
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• 1985

Protopanaxadiol (PD) fraction and protopanaxatriol (PT) fraction were separated from thebutanol fraction of panax ginseng roots. Each group of mice was injected with morphine hydrochloride (40 mg/kg s.c.) three times at 8 hr intervals for a period of 6 days. PD fraction and PT fraction were injected (25, 100 mg/kg i.p.) to mice 1 hr prior to the third morphine injection daily. Inhibition of morphine tolerance was evidenced by the increase in analgesic response to morphine hydrochloride (10mg/ kg i.p.) as estimated by the tail flick method. Inhibition of morphine tolerance by PT fraction was effective but there was no remarkable difference in inhibition of tolerance development between control group andPD fraction group.