Pharmacokinetics and tissue distribution of ginsenoside Rh2 and Rg3 epimers after oral administration of BST204, a purified ginseng dry extract, in rats

Abstract

1. BST204, a purified ginseng dry extract containing a high concentration of racemic Rh2 and Rg3 mixtures, is being developed for supportive care use in cancer patients in Korea. This study investigates the pharmacokinetics and tissue distribution of BST204 in rats. 2. After oral administration of BST204, only the S epimers, S-Rh2 and S-Rg3, could be determined in rat plasma. The poor absorption of the R-epimers, R-Rh2 and R-Rg3, may be attributed to lower membrane permeability and extensive intestinal oxygenation and/or deglycosylation into metabolites. The AUC and Cmax values of both S-Rh2 and S-Rg3 after BST204 oral administration were proportional to the administered BST204 doses ranged from 400 mg/kg to 2000 mg/kg, which suggested linear pharmacokinetic properties. 3. There were no statistically significant differences in the pharmacokinetics of S-Rh2 and S-Rg3 after oral administration of pure S-Rh2 (31.5 mg/kg) and S-Rg3 (68 mg/kg) compared with oral administration of BST204, 1000 mg/kg. These indicated that the presence of other components of BST204 extract did not influence the pharmacokinetic behavior of S-Rh2 and S-Rg3. 4. After oral dosing of BST204, S-Rh2 and S-Rg3 were distributed mainly to the liver and gastrointestinal tract in rats. 5. Our finding may help to understand pharmacokinetic characteristics of S-Rh2, R-Rh2, S-Rg3, and R-Rg3, comprehensively, and provide useful information in clinical application of BST204.

Anti-adipogenic Effects and Mechanisms of Ginsenoside Rg3 in Pre-adipocytes and Obese Mice

“…et al, 2011), and anti-obesity. Currently, commercial use of Rh2 and Rg3 are produced by chemical (mild acidic conditions) (Han et al, 1982) or biological deglycosylation (microorganisms or glycoside hydrolases) (Bae S.H. et al, 2014) of the major protopanaxadiol-type ginsenosides.…”

Absorption and pharmacokinetic study of two sulphated triterpenoid saponins in rat after oral and intravenous administration of saponin extracts of Pearsonothuria graeffei by HPLC-MS

“…They contain various kinds of physiologically active substances, such as polysaccharides , bioactive phenolic compounds (Kaneko & Nakanishi, 2004), cerebroside (Yu et al, 2015;Zhang et al, 2012), chondroitin sulphate (Kawaguchi, Kuhlenschmidt, Roseman, & Lee, 1981;Sun et al, 2012), and fucoidan (Bae et al, 2014). Triterpene saponins, the most important secondary metabolites and bioactive components of sea cucumbers (Zou et al, 2003), have been proven to exhibit various biological activities including antifungal, cytotoxic, haemolytic, cytostatic, and immunomodulatory effects (Bordbar, Anwar, & Saari, 2011;Dong, Xue, Yu, Xu, & Chen, 2008).…”

Production of bioactive ginsenosides Rh2 and Rg3 by metabolically engineered yeasts

“…Rg3 is now used as the major active component in an anti-tumor and anticancer drug in China (Z20030043). BST204, a purified ginseng dry extract containing high concentrations of a Rh2 and Rg3 mixture, is being developed as a supportive-care agent for cancer patients in Korea (Bae et al, 2014).…”

“…In biological approaches, microorganisms or glycoside hydrolases were used to hydrolyze the glycosides of the major ginsenosides to produce Rh2 and Rg3 (Bae et al, 2004;Cheng et al, 2008;Su et al, 2006;Yan et al, 2008). For example, BST204, a ginsenoside extract containing a high concentration of Rh2 and Rg3 mixtures, was prepared from crude ginseng with a ginsenoside-β-glucosidase combined with acid hydrolysis to enrich Rh2 and Rg3 (Bae et al, 2014). Both of the chemical and biological deglycosylation approaches require a supply of PPD-type ginsenosides, which depends on plantations of Panax plants.…”