Abstract

Enriched-baicalein (baicalein) from baicalin was prepared by fermentation of an SB extract with mycelium of Laetiporus sulphureus. To investigate the pharmacologic effects of baicalein, its antiallergic effect was measured in vitro and in vivo. Allergy was induced by intraperitoneal injection of ovalbumin (OVA) into Balb/c mice. As a result, baicalein showed antiallergic effects by inhibiting the release of β-hexosaminidase from immunoglobulin E- (IgE-) stimulated rat basophilic leukemia (RBL-2H3) mast cells without cytotoxicity after the methodology. After four weeks, the decrease of OVA-specific IgE level, decrease of histamine and tryptase level in serum, and then the decrease of the levels of T helper type 2 (Th2) cell-derived cytokines interleukin- (IL-) 4 and IL-13 in the splenocyte were observed. In a histological analysis for lung, baicalein excellently reduced eosinophil infiltration with the inhibition of characteristic lesions and inflammation including OVA-induced necrosis, numbers of inflammatory cells, and pulmonary edema. Therefore, these results showed that baicalein had excellent efficacy in the antiallergic activity.

Highlights

  • Scutellaria baicalensis Georgi (SB), Chinese name, “Huangqin,” has been routinely used in the treatment of bronchitis, hepatitis, allergy, atopy, inflammation, and arteriosclerosis and has been listed in the Pharmacopoeia of China [1]

  • It is reported that aglycon forms of baicalein in SB, monoglycoside of geniposide in Gardenia jasminoides, and glycyrrhizin in Glycyrrhiza uralensis are derived from the deglycosylation of baicalin, geniposide, and glycyrrhetinic acid, respectively [9]. ose aglycons are absorbed in the body more effectively and show a stronger pharmacologic effect [10]

  • To search the noncytotoxicity concentration of the SB extracts and baicalein, we evaluated the effect of the SB extracts and baicalein on the viability of RBL-2H3 mast cells

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Summary

Introduction

Scutellaria baicalensis Georgi (SB), Chinese name, “Huangqin,” has been routinely used in the treatment of bronchitis, hepatitis, allergy, atopy, inflammation, and arteriosclerosis and has been listed in the Pharmacopoeia of China [1]. In radix S. baicalensis Georgi, flavonoids with O-di-hydroxyl group or O-three-hydroxyl group or in ring A, such as baicalin and baicalein, could be good free-radical scavengers [4]. Baicalin which is a glycoside and active component of SB has low bioavailability and rate of low absorption in the body [5]. Conversion of baicalin into baicalein as an aglycon form can increase efficacy and rate of absorption by fermentation [6]. Is process boosts the pharmacological effect and rate of absorption in the body by converting glycoside present in natural material to aglycon, which is the active form [8]. It is reported that aglycon forms of baicalein in SB, monoglycoside of geniposide in Gardenia jasminoides, and glycyrrhizin in Glycyrrhiza uralensis are derived from the deglycosylation of baicalin, geniposide, and glycyrrhetinic acid, respectively [9]. It is reported that aglycon forms of baicalein in SB, monoglycoside of geniposide in Gardenia jasminoides, and glycyrrhizin in Glycyrrhiza uralensis are derived from the deglycosylation of baicalin, geniposide, and glycyrrhetinic acid, respectively [9]. ose aglycons are absorbed in the body more effectively and show a stronger pharmacologic effect [10]

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