Abstract
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.
Highlights
More than 400 bacterial species have been identified in the human feces, and most of them are anaerobic bacteria [1]
The results clearly indicated that antibiotics would decrease in the absorption of baicalin by reducing the hydrolysis process in the GI tract without affecting the absorption process of baicalein, and that metabolism of baicalin to baicalein by the intestinal microbiota would be a very critical step for the absorption of baicalein [23]
The results indicated that, to generate the anti-scratching behavioral effect of baicalin, it might require a time of at least 6 h for baicalin to be metabolized to baicalein and/or oroxylin A, and that these metabolites produced by intestinal microbiota are responsible for the anti-scratching behavioral effect of baicalin [16]
Summary
More than 400 bacterial species have been identified in the human feces, and most of them are anaerobic bacteria [1]. Glycosidic compounds are strongly affected by enzymes produced variation in metabolism efficacy and toxicity resulting the routes by intestinal microbiota,and so toxicity, that thedifferences change ofinintestinal microbiota can lead from to changes in of administration, and production of metabolites not formed in tissues, which were summarized in pharmacokinetics, pharmacodynamics and toxicity of glycosidic compounds [6,9,10,11,12]. In this regard, the literature elsewhere [6,8].
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