HPLC with electrochemical detection to examine the pharmacokinetics of baicalin and baicalein in rat plasma after oral administration of a Kampo medicine

Kotani, Akio; Kojima, Satoshi; Hakamata, Hideki; Kusu, Fumiyo

doi:10.1016/j.ab.2005.11.007

Cited by 53 publications

(30 citation statements)

References 16 publications

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“…A bimodal phenomenon of 10 flavonoids was presented in Fig. 4, which was in agreement with the literature and was probably due to distribution, re-absorption and enterohepatic circulation (Kowalczyk et al, 2006;Kotani et al, 2006;Zhu et al, 2010;Tong et al, 2012;Kim et al, 2006;Walle et al, 2001;Lu et al, 2007). This is the first study on the pharmacokinetics of flavonoids, including scutellarin, scutellarein and apigenin from RS.…”

Section: Analytessupporting

confidence: 86%

“…To study the pharmacokinetics of these flavonoids in vivo, HPLC-UV (Lu et al, 2007), HPLC-ECD (Kotani et al, 2006) and LC-MS (Zhu et al, 2010) analytical methods have been established. In the last 10 years, large numbers of studies have focused mainly on the pharmacokinetics of baicalin, wogonoside, oroxylin A-7-glucuronide, baicalein, wogonin and oroxylin A in crude RS, single compenents or multiple compenents, five or six at most (Ye et al, 2010;Shi et al, 2011;Tong et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

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Simultaneous determination of ten flavonoids of crude and wine‐processed Radix Scutellariae aqueous extracts in rat plasma by UPLC‐ESI‐MS/MS and its application to a comparative pharmacokinetic study

Cui

Qian

Huang

et al. 2014

Biomedical Chromatography

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Radix Scutellariae (RS) is a herbal medicine with various pharmacological activities to treat inflammation, respiratory and gastrointestinal infections, etc. In this study, a rapid, sensitive and selective UPLC-ESI-MS/MS method was developed for simultaneous determination of 10 flavonoids - scutellarin, scutellarein, chrysin, wogonin, baicalein, apigenin, wogonoside, oroxylin A-7-O-glucuronide, oroxylin A and baicalin - from RS aqueous extracts in rat plasma with propyl paraben as internal standard (IS). Chromatographic separation was achieved on a C18 column using gradient elution with the mobile phase consisting of methanol and water (containing 0.1% formic acid) at a flow rate of 0.2 mL/min. The detection was performed in multiple reaction monitoring mode using electrospray ionization in negative mode. The validated method showed good linearity over a wide concentration range (r >0.9935). The intra- and interday assay variabilities were <9.5% and <12.4% for all analytes, respectively. The extraction recovery ranged from 71.2 to 89.7% for each analyte and IS. This method was successfully applied to pharmacokinetic comparision after oral administration of crude and wine-processed RS aqueous extracts. There were significant differences in some pharmacokinetic parameters of most analytes between crude and wine-processed RS. This suggested that wine-processing exerted effects absorption of most flavonoids.

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Section: Analytessupporting

confidence: 86%

Section: Introductionmentioning

confidence: 99%

Simultaneous determination of ten flavonoids of crude and wine‐processed Radix Scutellariae aqueous extracts in rat plasma by UPLC‐ESI‐MS/MS and its application to a comparative pharmacokinetic study

Cui

Qian

Huang

et al. 2014

Biomedical Chromatography

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“…In fact, the existence of unidentified B-glucuronides, as well as BG, in the rat systemic circulation after oral administration of Kampo medicine containing Scutellariae Radix has been reported. 16) In the present study, we detected for the first time B6G at a higher level than BG in the rat systemic circulation after oral administration of BG or B, and investigated the pharmacokinetics of B6G and the contribution of the liver to the appearance of this metabolite.…”

Section: Discussionmentioning

confidence: 99%

“…15) In addition, unidentified metabolites besides BG in rat plasma have been found after oral administration of Kampo medicine including Scutellariae Radix, after being hydrolyzed enzymatically using β-glucuronidase and sulfatase. 16) However, types of metabolites besides BG that are present in plasma after oral administration of BG or B to rats are still unclear.…”

mentioning

confidence: 99%

Baicalein 6-<i>O</i>-β-d-Glucopyranuronoside Is a Main Metabolite in the Plasma after Oral Administration of Baicalin, a Flavone Glucuronide of Scutellariae Radix, to Rats

Akao¹,

Sato²,

He³

et al. 2013

Biological & Pharmaceutical Bulletin

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Baicalin (BG) and its aglycone, baicalein (B) are strong antioxidants that exert various pharmacological actions and show unique metabolic fates in the rat. The aim of the present study was to identify major metabolite(s) besides BG in rat plasma after oral administration of BG or B. The main metabolite was detected by HPLC equipped with an electrochemical detector at a potential of +500 mV and identified as baicalein 6-O-β-d-glucopyranuronoside (B6G) by HPLC/MS/MS. When BG at a dose of 20 mg/kg was administered orally to Wistar rats, the level of B6G in plasma was higher than that of BG. C max and the area under the concentration-curve from 0 to 24 h (AUC 0-24 h ) values of the plasma B6G were 1.66±0.34 µm and 19.8±3.9 µm·h, respectively, whereas those of BG were 0.853±0.065 µm and 10.0±3.1 µm·h, respectively. When B was administered, similar results were also obtained. B6G-producing activities from B were found in microsomes of both rat jejunum and liver, in spite of the low activity. Rat everted jejunal sacs formed B6G after application of B, but only in a small amount that was excreted into the mucosal side, and not the serosal side, indicating little contribution to the appearance of B6G in plasma. On the other hand, when B was injected into the rat portal vein, B6G was detected at a higher level than BG in the systemic circulation, demonstrating the hepatic contribution to the appearance of plasma B6G.Key words baicalin; baicalein 6-O-β-d-glucopyranuronoside; metabolite; rat Scutellariae Radix, the root of Scutellaria baicalensis GeorGi (Labiatae), is used in combination with other herbs in Chinese traditional (Kampo, in Japanese) medicines, and contains baicalin (BG, 5,6,7-trihydroxyflavone-7-β-d-glucuronide; Fig. 1) as its main active constituent. BG and its aglycone, baicalein (B), have wide-ranging pharmacological effects, such as antiallergic, 1) anti-inflammatory, 2) antiviral, 3,4) antiproliferative, 5) and antitumor 6) effects, and also show strong antioxidant activity. 7,8) In addition, they inhibit prostaglandin E2 production, and prevent the gene expression of inducible nitric oxide synthase and cyclooxygenase-2. 9) B also has an anxiolytic-like effect 10) and a protective effect against amnesia. 11)BG has been detected in rat plasma after its oral administration, 12) suggesting that it is absorbed directly from the gastrointestinal tract. However, in our previous study when BG was given to germ-free rats, only a small amount of BG was detected in their plasma. In addition, BG, and not B, has been detected even after oral administration of B to rats. 13) On the other hand, many kinds of metabolites such as B-glucuronides and B-sulfates besides BG have been found in bile after oral administration of either BG or B to rats.14) Many kinds of B-metabolites have also been detected in bile and urine after oral administration of Scutellariae Radix extract or Chinese traditional medicines that include Scutellariae Radix. 15) In addition, unidentified metabolites besides BG in rat plasma have been found ...

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“…Therefore, the accurate determination of baicalein is an important and significant work in practice. Some of the analytical methods including UV-vis spectrophotometry [8], flow-injection chemiluminescence [9], thin layer chromatography [10], high performance liquid chromatography [11,12], capillary electrophoresis [13,14] and voltammetry [15,16] have been applied to determine baicalein. Nevertheless, most of these methods required complicated sample preparation, or suffered from low sensitivities and strong acidic analysis system.…”

Section: Introductionmentioning

confidence: 99%

Sensitive Voltammetric Determination of Baicalein at Thermally Reduced Graphene Oxide Modified Glassy Carbon Electrode

Zhang

2013

Electroanalysis

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This work presents a sensitive voltammetric method for determination of the flavonoid baicalein by using a thermally reduced graphene oxide (TRGO) modified glassy carbon electrode (GCE) in 100 mM KCl-10 mM sodium phosphate buffer solution (pH 7.40). The surface morphology and structure of TRGO investigated by atomic force microscopy, FT-IR spectroscopy and Raman spectroscopy reveal that the TRGO prepared maintained as single or bilayer sheets and with significant edge-plane-like defect sites. The TRGO/GCE modified electrode shows more favorable electron transfer kinetics for potassium ferricyanide and potassium ferrocyanide probe molecules, which are important electroactive compounds, compared with bare GCE and GO/GCE electrodes. The electrochemical behaviors of baicalein at the TRGO/GCE were investigated by cyclic voltammetry, suggesting that the TRGO/GCE exhibits excellent electrocatalytic activity to baicalein. Under physiological conditions, the modified electrode showed linear voltammetric response from 10 nM to 10 mM for baicalein, with a detection limit of 6.0 nM. This work demonstrates that the graphene-modified electrode is a promising tool for electrochemical determination of flavonoid drugs.

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HPLC with electrochemical detection to examine the pharmacokinetics of baicalin and baicalein in rat plasma after oral administration of a Kampo medicine

Cited by 53 publications

References 16 publications

Simultaneous determination of ten flavonoids of crude and wine‐processed Radix Scutellariae aqueous extracts in rat plasma by UPLC‐ESI‐MS/MS and its application to a comparative pharmacokinetic study

Simultaneous determination of ten flavonoids of crude and wine‐processed Radix Scutellariae aqueous extracts in rat plasma by UPLC‐ESI‐MS/MS and its application to a comparative pharmacokinetic study

Baicalein 6-<i>O</i>-β-d-Glucopyranuronoside Is a Main Metabolite in the Plasma after Oral Administration of Baicalin, a Flavone Glucuronide of Scutellariae Radix, to Rats

Sensitive Voltammetric Determination of Baicalein at Thermally Reduced Graphene Oxide Modified Glassy Carbon Electrode

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