Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.31 (beta-glucuronidase)
 7,680 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Baicalin, baicalein, wogonoside and wogonin are flavone constituents of Scutellariae Radix with various beneficial biological activities. The purpose of this study was to investigate the urinary pharmacokinetics of these flavones after oral administration of Scutellariae Radix commercial powder. Ten healthy male volunteers received a dose of 5.2 g commercial powder (comparable to 9 g crude drug), respectively. The concentrations of baicalin, baicalein and wogonin in the commercial powder as well as their metabolites in urine were assayed by HPLC method. The glucuronides and sulfates of baicalein and wogonin in urine were hydrolyzed with beta-glucuronidase and sulfatase, respectively. Our results showed that the mean cumulated renal excretion of baicalein glucuronides and sulfates were 43.1+/-4.5 micromol (2.9% of dose) and 64.8+/-6.3 micromol (4.3% of dose), respectively, whereas wogonin glucuronides and sulfates were 21.6+/-2.0 micromol (5.9% of dose) and 20.7+/-1.7 micromol (5.7% of dose), respectively. The result indicated that the renal excretion of conjugated metabolites of wogonin (11.6% of dose) were higher than that of baicalein (7.2% of dose). The baicalein sulfates was predominant than the corresponding glucuronides, whereas wogonin sulfates was comparable to the corresponding glucuronides.
 ...
PMID:Urinary pharmacokinetics of baicalein, wogonin and their glycosides after oral administration of Scutellariae Radix in humans. 1252 Jan 78

Baicalin and baicalein, a flavone glucuronide and its aglycone, are bioactive constituents of Scutellariae Radix with various beneficial activities. We have characterized and compared the metabolic pharmacokinetics of baicalin and baicalein in rats. Baicalein was administered intravenously and orally to rats, and baicalin was orally administered. An HPLC method was used to determine the concentration of baicalein before and after hydrolysis using beta-glucuronidase/sulfatase. The pharmacokinetic parameters were calculated by using WINNONLIN. Unpaired Student's t-test was used for statistical comparison. The result showed that after intravenous administration of baicalein, 75.7% of the dose was circulating as its conjugated metabolites. After oral administration of baicalein, absorption of baicalein itself was negligible, whereas the glucuronides/sulfates of baicalein were predominant in the plasma. When compared with intravenous bolus administration with dose correction, the absolute absorption was 40%. When baicalin was administered orally, glucuronides and sulfates of baicalein were exclusively circulating in the plasma. The relative absorption for baicalin was 65% when compared with baicalein. Profound differences of serum profile and pharmacokinetics were observed between oral baicalein and baicalin. Baicalin demonstrated significantly later time to peak concentration (t(max)) and lower peak serum concentration (C(max)) of baicalein conjugated metabolites than baicalein, indicating baicalin was absorbed more slowly and to a lesser extent than baicalein.
 ...
PMID:Comparison of metabolic pharmacokinetics of baicalin and baicalein in rats. 1263 13

Baicalin was extensively researched for utility in a number of therapeutic areas owing to its anti-inflammatory, anti-oxidant, anti-bacterial, and anti-cancer properties. A number of preclinical studies, in vitro work, and mechanistic studies were performed to understand the absorption, distribution, metabolism, and excretion profiles of baicalin. The absorption of baicalin involved several complexities: the restriction to two distant sites; the conversion of baicalin to baicalein; the possible role of transporter(s); and enhanced absorption due to breakdown of conjugates by beta-glucuronidase. Limited distribution data suggest that baicalin reached several sites such as the brain, eye lens, thymus, etc. Hepatobiliary recycling also served as a distribution phase for sustained delivery of baicalin. Metabolism data suggest the rapid conversion of baicalin to baicalein, which was extensively subjected to Phase 2 metabolism, conjugates baicalein glucuronide/sulfate have been identified. Limited excretion data suggest involvement of renal and faecal routes--glucuronide and sulfate conjugates were excreted in urine and faeces (via biliary excretion). The published data on baicalin suggest imminent challenges for developing baicalin and/or during co-administration with other agents. These challenges are absorption related (transporter or changes in the microenvironment), metabolism related (CYP2B6 induction and/or CYP2E1 inhibition), and excretion/efflux related (competitive biliary pathway and/or OATP1B1 transport).
 ...
PMID:Baicalin, an emerging multi-therapeutic agent: pharmacodynamics, pharmacokinetics, and considerations from drug development perspectives. 2023 Jan 89

The active compounds in the roots of Scutellaria baicalensis Georgi, a traditional Chinese medicinal plant, are mainly flavonoids which have anti-inflammatory, antitumour, and anti-HIV activity, respectively. The increasing annual average temperature has rendered the S. baicalensis plants grown in some ancient producing regions no longer suitable for their medicinal usage. Hydrogen peroxide plays an important role in root responses to abnormal temperature in S. baicalensis. Baicalin and baicalein and antioxidative enzymes were anticipated to detoxify H2O2 in S. baicalensis. Here, we show that abnormal temperatures (10 and 40 degrees C) decreased the content of flavonoids as compared with the normal temperature (30 degrees C), and the transcripts of UDP-glucuronate:baicalein 7-O-glucuronosyltransferase and beta-glucuronidase involved in the interconversion between baicalin and baicalein were affected by the 40-degrees C treatment. High temperature also increased the activities of catalase and peroxidase. Reverse transcription-polymerase chain reaction (RT-PCR) analysis revealed that the transcript levels of peroxidase 2, peroxidase 3, monodehydroascorbate reductase 2, and dehydroascorbate reductase were significantly increased under high-temperature conditions. The respective genes would be candidates for improvement of the adaptation of S. baicalensis plants to abnormal temperatures and for regulation of the contents of the active compounds.
 ...
PMID:Flavonoids and antioxidative enzymes in temperature-challenged roots of Scutellaria baicalensis Georgi. 2248 44