Metabolism of Wogonoside by Human Fecal Microflora and Its Anti-pruritic Effect

Abstract

-To understand the relationship between the metabolism of wogonoside from the rhizome of Scutellaria baicalensis, and its anti-pruritic effect, we anaerobically incubated it with human fecal microflora, identified its metabolite identified, and investigated its anti-pruritic effect in compound 48/80 or histamineinduced pruritic mice. Wogonoside was metabolized to wogonin, with metabolic activity of 6.9 ± 5.1 nmol/h/ mg wet weight of fecal microflora. Orally administered wogonoside had more potent anti-scratching behavioral effect in compound 48/80 or histamine-treated mice than intraperitoneally treated one, apart from orally administered its metabolite, wogonin, which was more potent than the orally administered one. Wogonoside showed more potent anti-pruritic effects when administered at 5 h prior to the pruritic agent treatment than when administered at 1 h before. However, wogonin orally administered 1 h before the treatment with pruritic agents showed a more potent anti-pruritic effect than when treated at 5 h before. Orally administered wogonoside may be metabolized to wogonin in the intestine and its anti-scratching behavioral effect may be dependent on its metabolism by intestinal microflora.

Simulated gastrointestinal tract metabolism and pharmacological activities of water extract of Scutellaria baicalensis roots

“…Although no change was observed in artificial gastric or intestinal juice, the main constituents, baicalin, wogonoside and oroxyloside, were found to be metabolized into their respective aglycons by intestinal bacteria. These findings are consistent with the reports that monomeric compounds baicalin, wogonoside and oroxyloside could be converted to metabolites baicalein, wogonin and oroxylin A by intestinal bacteria, respectively (Akao et al, 2000;Trinh et al, 2009;Zuo et al, 2002). The biotransformation of individual compound was the same as that in whole herb decoctions.…”

“…It was found that baicalin was initially hydrolyzed to baicalein prior to the absorption, while baicalein could be readily absorbed with a fast and extensive first pass metabolism (Akao et al, 2000;Lu et al, 2007). Wogonoside was found to be metabolized to wogonin by human fecal microflora (Trinh et al, 2009). In addition, pharmacokinetic study of Huangqin-Tang Decoction indicated that the constituents of wogonoside and oroxyloside had double-site absorption kinetics in rats which may due to the enteric circulation and enterohepatic circulation after oral dosing (Zuo et al, 2003).…”

UPLC-MS identification and anticomplement activity of the metabolites of Sophora tonkinensis flavonoids treated with human intestinal bacteria

“…Moreover, those components were metabolized by intestinal bacteria before absorbed from the digestive tract [9,10]. Research on herbal components of metabolism with intestinal flora is greatly significant to understand their potential biological characteristics [11].…”

The Relationship Between Endogenous β‐Glucuronidase Activity and Biologically Active Flavones‐Aglycone Contents in Hairy Roots of Baikal Skullcap

“…It has been used for the treatment of different diseases: hepatitis, leukemia, insomnia, hypertension, bleeding and inflammatory reactions of various origins. The aforelisted properties of skullcap roots are explained, first of all, by the presence of four main flavones: glycosylated forms, baicalin and wogonoside, and their free forms, aglycones, baicalein and wogonin ( Figure ), among which the most manifested medicinal activity is exhibited by aglycone flavones, baicalein and wogonin . Most of the attention is currently directed to wogonin because it has a selective efficiency on cancer cells .…”