Studies on the absorption, distribution, excretion and metabolism of ginseng saponins. II. The absorption, distribution and excretion of ginsenoside Rg1 in the rat.

Odani, Tsutomu; Tanizawa, Hisayuki; Takino, Yoshio

doi:10.1248/cpb.31.292

Cited by 105 publications

(53 citation statements)

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“…Ginsenosides has been reported to be only poorly absorbed from digestive tracts (16,17). The absorption amounts of ginsenoside-Rb 1 and -Rg 1 are 0.1% and 1.9% of the dosage to rats, respectively.…”

Section: M4 Did Not Alter the Specific Binding Of [mentioning

confidence: 99%

Proof of the Mysterious Efficacy of Ginseng: Basic and Clinical Trials: Suppression of Adrenal Medullary Function In Vitro by Ginseng

Tachikawa¹,

Kudo²

2004

J Pharmacol Sci

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Abstract. The root of Panax ginseng C.A. MEYER has been reported to have an anti-stress action. Therefore, the effects of ginseng components on functions of adrenal medulla, which is one of the most important organs responsive to stress, were investigated in vitro. First, the components of ginseng were mainly divided into two fractions, that is, the saponin-rich and non-saponin fractions. The saponin-rich fraction greatly reduced the secretion of catecholamines from bovine adrenal chromaffin cells stimulated by acetylcholine (ACh), whereas the nonsaponin fraction did not affect it at all. The protopanaxatriol-type saponins inhibited the AChevoked secretion much more strongly than the protopanaxadiol-type. On the other hand, the oleanane-type saponin, ginsenoside-Ro, had no such effect. Recent reports have demonstrated that the saponins in ginseng are metabolized and absorbed in digestive tracts following oral administration of ginseng. All of the saponin metabolites greatly reduced the ACh-evoked secretion. M4 was the most effective inhibitor among the metabolites. M4 blocked ACh-induced Na + influx and ion inward current into the chromaffin cells and into the Xenopus oocytes expressing human a 3b4 nicotinic ACh receptors, respectively, suggesting that the saponin metabolites modulate nicotinic ACh receptors followed by the reduction of catecholamine secretion. It is highly possible that these effects of ginsenosides and their metabolites are associated with the anti-stress action of ginseng.

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Section: M4 Did Not Alter the Specific Binding Of [mentioning

confidence: 99%

Proof of the Mysterious Efficacy of Ginseng: Basic and Clinical Trials: Suppression of Adrenal Medullary Function In Vitro by Ginseng

Tachikawa¹,

Kudo²

2004

J Pharmacol Sci

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“…Other researchers also found that the intestinal absorption of naturally occurring ginsenosides is very poor, 7,14) and that the intestinal bacterial metabolites of ginsenosides are really responsible for the main pharmacological activities of ginseng. [9][10][11][12][13] To the best of our knowledge, there are still no reports about the effects of intestinal bacterial metabolites of ginsenosides on metabolism enzymes.…”

Section: )mentioning

confidence: 99%

“…[9][10][11][12] For the 20(S)-protopanaxatriol ginsenosides, such as Re and Rg 1 , the intestinal bacterial metabolite is believed to be protopanaxatriol (Ppt, or M-4), which mediates the anticancer actions of ginsenosides. 13) In contrast to the very low absorption rate of Rg 1 , only 1.9% from intestines, 14) Ppt is easily absorbed. 13) As the major isozyme of CYPs, CYP3A, which constitutes 30% of the human hepatic P450 complement 15) and 70% of the human small intestine P450 complement 16) and metabolizes 40-50% drugs in clinical use, 17,18) has drawn great attention.…”

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confidence: 98%

The Inhibitory Effect of Intestinal Bacterial Metabolite of Ginsenosides on CYP3A Activity

Liu

Deng

et al. 2004

Biological & Pharmaceutical Bulletin

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“…Many experiments on the degradation of ginsenosides in the gastrointestinal tract were undertaken using acids, enzymes, intestinal bacteria, and animals (Odani et al, 1983;Strömbom et al, 1985;Karikura et al, 1990;Hasegawa et al, 1996;Akao et al, 1998). From these experiments it is known that protopanaxatriol ginsenosides are hydrolyzed to ginsenoside Rh 1 and its hydrated form under mild acidic conditions similar to gastric fluid (Han et al, 1982).…”

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confidence: 99%

Degradation of Ginsenosides in Humans After Oral Administration

Abdel‐Tawab

Bahr²,

Karas³

et al. 2003

Drug Metab Dispos

410

325

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This article is available online at http://dmd.aspetjournals.org ABSTRACT:Even though the degradation of ginsenosides has been thoroughly studied in animals and in vitro using acids, enzymes, and intestinal bacteria, knowledge concerning the systemic availability of ginsenosides and their degradation products in humans is generally lacking. Therefore, the attention in this article is focused on the identification of ginsenosides and their hydrolysis products reaching the systemic circulation in man. This is of great importance in understanding clinical effects, preventing herb-drug interactions, and optimizing the biopharmaceutical properties of ginseng preparations. Using a sensitive mass spectrometric method, which is specific for the identification of ginsenosides in complex biological matrices, the degradation pathway of ginsenosides in the gastrointestinal tract of humans could be elucidated following the oral administration of ginseng. Within the frame of a pilot study, human plasma and urine samples of two subjects were screened for ginsenosides and their possible degradation products. In general, the urine data coincided well with the plasma data. In both volunteers the same hydrolysis products, which are not originally present in the Ginsana extract (Pharmaton S.A., Lugano, Switzerland) ingested, were identified in plasma and urine. It was shown that two hydrolysis products of the protopanaxatriol ginsenosides, namely G-Rh 1 and G-F 1 may reach the systemic circulation. In addition, compound-K, the main intestinal bacterial metabolite of the protopanaxadiol ginsenosides, was detected in plasma and urine. These products are probably responsible for the action of ginseng in humans. In opposition to previous reports, G-Rb 1 was identified in plasma and urine of one subject.

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Studies on the absorption, distribution, excretion and metabolism of ginseng saponins. II. The absorption, distribution and excretion of ginsenoside Rg1 in the rat.

Cited by 105 publications

References 0 publications

Proof of the Mysterious Efficacy of Ginseng: Basic and Clinical Trials: Suppression of Adrenal Medullary Function In Vitro by Ginseng

Proof of the Mysterious Efficacy of Ginseng: Basic and Clinical Trials: Suppression of Adrenal Medullary Function In Vitro by Ginseng

The Inhibitory Effect of Intestinal Bacterial Metabolite of Ginsenosides on CYP3A Activity

Degradation of Ginsenosides in Humans After Oral Administration

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