Urinary Pharmacokinetics of Baicalein, Wogonin and Their Glycosides after Oral Administration of Scutellariae Radix in Humans.

Lai, M.-Y.; Hsiu, Su-Lan; Chen, Chung-Chuan; Hou, Yu‐Chi; Chao, Pei‐Dawn Lee

doi:10.1248/bpb.26.79

Cited by 110 publications

(91 citation statements)

References 19 publications

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“…For example, Akao et al (24) and our previous study using a rat intestinal perfusion model demonstrated the secretion of BG in the intestine. Kidney disposition of conjugates of Ba was also reported (25). Therefore, it is probable that different organs may show their preference to the uptake of conjugates, and the preference may also vary with different plasma concentrations of the conjugates.…”

Section: −1mentioning

confidence: 89%

Hepatic Metabolism and Disposition of Baicalein via the Coupling of Conjugation Enzymes and Transporters—In Vitro and In Vivo Evidences

Zhang

Lin

et al. 2011

AAPS J

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Abstract. Baicalein (Ba) was found to be subject to serious first-pass metabolism after oral administration. We previously revealed the important role of intestine in the low oral bioavailability of Ba. The present study aims to evaluate the hepatic metabolism and disposition of Ba. Ba was given to Sprague-Dawley rats through bolus or infusion via intravenous or intra-portal route of administrations. Both plasma and bile samples at different time intervals were obtained. Concentrations of Ba and potential metabolites in the collected samples were analyzed with HPLC/UV and identified by LC/MS/ MS, respectively. Plasma concentration versus time profiles of Ba obtained from intravenous and intraportal administrations were compared to estimate the extent of hepatic metabolism. In addition, transport studies of baicalein-7-glucuronide (BG), one of the major metabolites of Ba, were carried out using transfected cell systems overexpressing various human organic anion-transporting polypeptide (OATP) isoforms to estimate the specific transporters involved in the hepatic disposition of Ba metabolites. The results showed that liver, in addition to intestine, also conferred extensive metabolism to Ba. Several mono-and di-conjugates of Ba, which were mainly glucuronides, sulfates, and methylates, were found in bile. The transport study demonstrated that besides MRPs and BCRP, human OATP2B1 and OATP1B3 in liver might also mediate the secretion of BG to bile. In summary, liver plays an important role in the metabolism of Ba and transport of its conjugated metabolites.

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Section: −1mentioning

confidence: 89%

Hepatic Metabolism and Disposition of Baicalein via the Coupling of Conjugation Enzymes and Transporters—In Vitro and In Vivo Evidences

Zhang

Lin

et al. 2011

AAPS J

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“…A recent study reported the urinary pharmacokinetics of wogonin after oral administration of a commercial powder of Scutellariae radix to humans (31). No free form of wogonin was found in the urine and the total excreted wogonin conjugates amounted to 11.6% of the administered dose.…”

Section: Pharmacokinetic Studiesmentioning

confidence: 99%

Therapeutic Potential of Wogonin: A Naturally Occurring Flavonoid

et al. 2005

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The search for flavonoids with novel therapeutic effects has been intense. Wogonin, as a naturally existing monoflavonoid, has been shown to have therapeutic potential in vitro and in vivo. Methods for its extraction from herbs and its chemical synthesis have been developed. Pharmacokinetic studies have shown a rapid tissue distribution and prolonged plasma elimination phase of wogonin. It has been shown experimentally that wogonin exerts anti-oxidant activity, which may, in part, underlie its antiinflammatory, anti-cancer, antiviral and neuroprotective actions. The recent discovery of its anxiolytic activity suggests a new mechanism of action, involving interaction with the benzodiazepine (BZD) binding site of the GABA A receptor and modulation of this receptor activity. Although the safety record of wogonin is remarkable and voluminous literature about its pharmacological effects is available, it has not been used in Western medicine in the form of a pure chemical. In this article we review its therapeutic effects, its sources and pharmacokinetic profile to highlight its therapeutic potential.

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“…[7][8][9][10][11][12][13] To our knowledge, two studies have reported the simultaneous determination of the bioactive flavonoids of Scutellariae Radix including all of baicalein, baicalin, wogonin, and wogonoside in biological samples with full validation data by using LC-MS/MS. 14,15 However, in those studies, the analytical method was validated in the restricted concentration ranges.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous Determination of Baicalein, Baicalin, Wogonin, and Wogonoside in Rat Plasma by LC-MS/MS for Studying the Pharmacokinetics of the Standardized Extract of Scutellariae Radix

Chung¹,

Lim²,

Kim³

et al. 2012

Bulletin of the Korean Chemical Society

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A new composition of standardized Scutellariae Radix extract (HPO12) was developed for treatment of Alzheimer's disease. For the preclinical pharmacokinetic study of HPO12, a rapid, sensitive, and selective LC-MS/MS method was developed and validated for the simultaneous determination of 4 bioactive compounds, baicalein, baicalin, wogonin, and wogonoside. After extraction with ethylacetate, chromatographic analysis was performed on a Thermo C 18 column (150 mm × 2.1 mm, 3 μm) with a mobile phase consisting of 0.1% formic acid (A) and 0.1% formic acid in 95% acetonitrile (B) by using gradient elution at a flow rate of 250 μL/min. Analytes introduced to a mass spectrometer were monitored by multiple reaction monitoring (MRM) in positive ion mode. Using 25 μL of plasma sample, the method was validated over the following concentration ranges: 25-5000 ng/mL for baicalein, 20-40000 ng/mL for baicalin, 1-1000 ng/mL for wogonin, and 5-10000 ng/mL for wogonoside. The intra-and inter-day precision and accuracy of the quality control samples at the 4 concentrations showed ≤ 13.7% relative standard deviation (RSD) and 86.6-105.5% accuracy. The method was successfully applied to determine the concentrations of baicalein, baicalin, wogonin, and wogonoside in rat plasma after intraperitoneal and oral administrations of HPO12.

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Urinary Pharmacokinetics of Baicalein, Wogonin and Their Glycosides after Oral Administration of Scutellariae Radix in Humans.

Cited by 110 publications

References 19 publications

Hepatic Metabolism and Disposition of Baicalein via the Coupling of Conjugation Enzymes and Transporters—In Vitro and In Vivo Evidences

Hepatic Metabolism and Disposition of Baicalein via the Coupling of Conjugation Enzymes and Transporters—In Vitro and In Vivo Evidences

Therapeutic Potential of Wogonin: A Naturally Occurring Flavonoid

Simultaneous Determination of Baicalein, Baicalin, Wogonin, and Wogonoside in Rat Plasma by LC-MS/MS for Studying the Pharmacokinetics of the Standardized Extract of Scutellariae Radix

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