Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics

Since many glycoside compounds in natural products are hydrolyzed by intestinal microbiota when administered orally, it is of interest to know whether their pharmacological effects are derived from the glycoside itself or from the aglycone form in vivo. An interesting example is baicalin versus baic...

Full description

Saved in:
Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2016-03, Vol.21 (3), p.337-337
Main Authors: Noh, Keumhan, Kang, Youra, Nepal, Mahesh Raj, Jeong, Ki Sun, Oh, Do Gyeong, Kang, Mi Jeong, Lee, Sangkyu, Kang, Wonku, Jeong, Hye Gwang, Jeong, Tae Cheon
Format: Article
Language:English
Subjects:
Animals
baicalein
baicalin
Biomarkers
drug interaction
Drug Interactions
Flavanones - chemistry
Flavanones - pharmacokinetics
Flavanones - pharmacology
Flavonoids - chemistry
Flavonoids - pharmacokinetics
Flavonoids - pharmacology
Gastrointestinal Microbiome
Humans
Intestinal Absorption
intestinal microbiota
Intestinal Mucosa - metabolism
Intestinal Mucosa - microbiology
Molecular Structure
pharmacokinetics
Rats
Review
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Since many glycoside compounds in natural products are hydrolyzed by intestinal microbiota when administered orally, it is of interest to know whether their pharmacological effects are derived from the glycoside itself or from the aglycone form in vivo. An interesting example is baicalin versus baicalein, the aglycone of baicalin, which is contained in some herbs from Labiatae including Scutellaria baicalensis Georgi and Scutellaria lateriflora Linne. The herbs have been extensively used for treatment of inflammatory diseases in Asia. Although there have been numerous reports regarding the pharmacological effects of baicalin and baicalein in vivo and in vitro, some reports indicated that the glycoside form would hardly be absorbed in the intestine and that it should be hydrolyzed to baicalein in advance for absorption. Therefore, the role of metabolism by intestinal microbiota should also be considered in the metabolism of baicalin. In addition, baicalin contains a glucuronide moiety in its structure, by which baicalin and baicalein show complex pharmacokinetic behaviors, due to the interconversion between them by phase II enzymes in the body. Recently, concerns about drug interaction with baicalin and/or baicalein have been raised, because of the co-administration of Scutellaria species with certain drugs. Herein, we reviewed the role of intestinal microbiota in pharmacokinetic characteristics of baicalin and baicalein, with regards to their pharmacological and toxicological effects.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules21030337