• Natural Product Sciences
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• v.10 no.4
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• pp.152-167
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• 2004

Traditional Chinese Medicines (TCM) have attracted great interest in recent researchers as alternative medicines for incurable diseases. This review focuses on qualitative and quantitative analytical approaches for bioactive metabolites of components flavonoids and saponins of traditional Chinese medicines by TLC system, although various methods have been introduced. Emphasis will be put on the processes of metabolite extraction from intestinal bacterial cultures or urines, separation (mobile phase) and detection. The identified metabolites by selection of extraction solvent and detection methods are also discussed. In addition, metabolite determinations of flavonoids (baicalin, apiin, rutin, quercetin, quercitrin, kaempferol, diosmin, hesperidin, poncirin, naringin, puerarin, daidzin, daidzein, tectoridin) and saponins (ginsenosides, kalopanaxsaponins, glycyrrhizin, chiisanoside, saikosaponins, soyasaponins) in culture fluid, in urine and in some herbal formula extracts are summarized. These bioactive metabolites of these components by intestinal microflora should be connected to pharmacological actions.

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

• Archives of Pharmacal Research
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• v.20 no.6
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• pp.539-544
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• 1997

Anti-metastatic activities of IH901, an intestinal bacterial metabolic derivative formed from Ginseng protopanaxadiol saponins, was determined in vitro and in vivo. Under in vitro conditions, IH901 inhibited the migration of bovine aortic endothelial cells 25 times stronger than suramin and suppressed the invasion of HT1080 human fibrosarcoma cells into reconstituted basement membrane components of Matrigel 1000 times stronger than RGDS peptide. IH901 also showed inhibitory effect on type-IV collagenase secretion from HT 1080 cells and platelet aggregation. When the anti-metastatic activity of IH901 was evaluated in comparison with that of 5-FU using a spontaneous lung metastatic model of Lewis lung carcinoma, the administration of IH901 (10 mg/kg p. o.) to tumor-bearing mice led to a significant decrease in lung metastasis (43% of untreated control), which was slightly more effective than that obtained with 5-FU (56% of control). Thus, IH901 seems to exhibit its anti-metastatic activity partly through the inhibition of tumor invasion which results from the blockade of type IV collagenase secretion and also through anti-platelet and anti-angiogenic activities.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.225.1-225.1
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• 2003

To evaluate the antiallergic activities of puerarin and daidzin from the rhizome of Pueraria lobata, in vitro and in vivo inhibitory activities of these compounds and their metabolite daidzein were measured. Daidzein exhibited potent inhibitory activity on the B-hexosaminidase release induced by DNP-HSA and potently inhibited the PCA reaction in mice. (omitted)

• Food Science and Biotechnology
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• v.14 no.4
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• pp.558-560
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• 2005

Hepatoprotective effects of white ginseng extract (WGE), and IH-901 (20-O-${\beta}$-D-glucopyranosyl-20(S)-protopanaxadiol) derived from intestinal metabolite of ginsenoside $Rb_1$ were studied using two experimental animal models with chemical-induced hepatic damage. Administration of WGE (200 and 500 mg/kg) and IH-901 (0.01, 0.05, and 0.1 mM/kg) significantly decreased aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels in acute hepatitic mice induced by $CCl_4$. Administration of WGE (l00 mg/kg) and IH-901 (0.02, 0.04, and 0.08 mM/kg) significantly decreased AST and ALT levels in acute hepatitic rats induced by D-galactosamine. AST and ALT levels of IH-901 groups decreased. These results suggested WGE and IH-901 may have protective effects against chemical-induced hepatic damage.

• Journal of Microbiology and Biotechnology
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• v.16 no.11
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• pp.1791-1798
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• 2006

When ginsenoside Rg5, a main component isolated from red ginseng, was incubated with three human fecal microflora for 24 h, all specimens showed hydrolyzing activity: all specimens produced ginsenoside Rh3 as a main metabolite, but a minor metabolite $3{\beta},12{\beta}$-dihydroxydammar-21(22),24-diene (DD) was observed in two specimens. To evaluate the antiallergic effect of ginsenoside Rg5 and its metabolites, the inhibitory effect of ginsenoside Rg5 and its metabolite ginsenoside Rh3 against RBL-2H3 cell degranulation, mouse passive cutaneous anaphylaxis (PCA) reaction induced by the IgE-antigen complex, and mouse ear skin dermatitis induced by 12-O-tetradecanoilphorbol-13-acetate (TPA) were measured. Ginsenosides Rg5 and Rh3 potently inhibited degranulation of RBL-2H3 cells. These ginsenosides also inhibited mRNA expression of proinflammatory cytokines IL-6 and $TNF-{\alpha}$ in RBL-2H3 cells stimulated by IgE-antigen. Orally and intraperitoneally administered ginsenoside Rg3 and orally administered ginsenoside Rg5 to mice potently inhibited the PCA reaction induced by IgE-antigen complex. However, intraperitoneally administered ginsenoside Rg5 nearly did not inhibit the PCA reaction. These ginsenosides not only suppressed the swelling of mouse ears induced by TPA, but also inhibited mRNA expression of cyclooxygenase-2, $TNF-{\alpha}$, and IL-4 and activation of transcription factor NF-kB. These inhibitions of ginsenoside Rh3 were more potent than those of ginsenoside Rg5. These findings suggest that ginsenoside Rg5 may be metabolized in vivo to ginsenoside Rh3 by human intestinal microflora, and ginsenoside Rh3 may improve antiallergic diseases, such as rhinitis and dermatitis.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.334.3-334.3
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• 2002

Ginseng(the root of Panax ginseng C.A. Meyer, Araliaceae) has been used for thousands of years as a traditional medicine in Asian countries. The main components of Ginseng are ginsenoside Rb1, Rb2 and Rc. These compounds are transformed by intestinal microflora. The main metabolite of ginsenosides was compoud K (IH-901). The transformed compound K shows an antimetastic or anticarcinogenic effect by blocking tumor invasion or preventing chromosomal aberration and tumorigenesis. Therefore. we isolated and characterzed ginseng saponin-metabolizing bacteria from human intestinal microffora. Among 200 tested intestinal bacteria. we found 78 bacteris to transform glnseng senseng saponins to compound K. These bacteria were seperated into three group: the first group highy produced ginsenside Rd (29) the second grop produced potently ginsenoside F2 (21) and the third produced compound K(28)

• Proceedings of the Korean Society of Toxicology Conference
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• 2003.10b
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• pp.146-146
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• 2003

20-O-(${\beta}$-D-Glucopyranosyl)-20(S)-protopanaxadiol (IH901), an intestinal bacterial metabolite of ginseng saponins formed from ginsenosides Rb1, Rb2 and Rc, is suggested to be a potential chemopreventive agent. Here we show that IH901 induces apoptosis in human hepatoblastoma HepG2 cells.(omitted)

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2001.10b
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• pp.139-140
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• 2001

• Proceedings of the Korean Nutrition Society Conference
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• 1995.05c
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• pp.21-21
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• 1995

Absorption of fat-soluble vi tamin, retinol occurs mainly in the proximal part of small intestine. But its intestinal transport mechanism isn't yet clear. The aim of the present study was to investigate on the mechanism of absorption of retinol by determining a concentration-dependent kinetic of retinol absorption in rats. The study was carried out by applying in vivo technique in which vitamin solution was infused to intestinal lumen and at the same time thoracic duct and choledochus duct were canulated to collect samples. The investigations showed that retinol is absorbed in the small intestine by a saturable, carrier-mediated transport system, i.e. wi thout signi ficant differences between the proximal and distal halves of the small intestine. The transport of retinol taken up by the enterocytes occured via different mechanisms: while the main vitamin A transport via the thoracic duct was saturated by limiting transport factors such as retinol-CRBP-II-complex formation and retinol esterification with increasing substrate concentrations, the transport of retinol metabolite product via the portal vein was proportional to the substrate concentration.ration.