Bioactivity and bioavailability of ginsenosides are dependent on the glycosidase activities of the A/J mouse intestinal microbiome defined by pyrosequencing

Tao Niu, Diane L. Smith, Zhen Yang, Song Gao, Taijun Yin, Zhi Hong JIANG, Ming You, Richard A. Gibbs, Joseph F. Petrosino*, Ming Hu

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

34 Citations (Scopus)

Abstract

Purpose: To investigate the ability of bacteria in the intestinal microbiome to convert naturally occurring primary ginsenosides in red ginseng extract to active secondary ginsenosides. Methods: Anti-proliferative ginsenoside activity was tested using mouse lung cancer LM1 cells. Permeabilities were evaluated in Caco-2 cell monolayers. Systemic exposure of secondary ginsenosides was determined in A/J mice. 16S rRNA gene pyrosequencing was used to determine membership and abundance of bacteria in intestinal microbiome. Results: Secondary ginsenoside C-K exhibited higher anti-proliferative activity and permeability than primary ginsenosides. Significant amounts of secondary ginsenosides (F2 and C-K) were found in blood of A/J mice following oral administration of primary ginsenoside Rb1. Because mammalian cells did not hydrolyze ginsenoside, we determined the ability of bacteria to hydrolyze ginsenosides and found that Rb1 underwent stepwise hydrolysis to Rd, F2, and then C-K. Formation of F2 from Rd was the rate-limiting step in the biotransformation of Rb1 to C-K. Conclusion: Conversion to F2 is the rate-limiting step in bioactivation of primary ginsenosides by A/J mouse intestinal microbiome, whose characterization reveals the presence of certain bacterial families capable of enabling the formation of F2 and C-K in vivo.

Original languageEnglish
Pages (from-to)836-846
Number of pages11
JournalPharmaceutical Research
Volume30
Issue number3
DOIs
Publication statusPublished - Mar 2013

Scopus Subject Areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

User-Defined Keywords

  • 16S rRNA gene sequencing
  • F2 and C-K
  • ginseng
  • ginsenosides Rb1
  • microbiome
  • permeability
  • pharmacokinetic profile
  • rate-limiting step
  • Rd
  • stepwise metabolism

Fingerprint

Dive into the research topics of 'Bioactivity and bioavailability of ginsenosides are dependent on the glycosidase activities of the A/J mouse intestinal microbiome defined by pyrosequencing'. Together they form a unique fingerprint.

Cite this