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)

Studies were made on the effects of baicalein (5,6,7-trihydroxyflavone) on leukotrienes B4 and C4 biosyntheses and degranulation induced by calcium ionophore A23187 (A23187) in human polymorphonuclear leukocytes. Baicalein inhibited A23187-induced biosynthesis of leukotrienes B4 and C4 in human polymorphonuclear leukocytes. The concentration of baicalein required for 50% inhibition (IC50) of leukotrienes B4 and C4 formations was 1.46.10(-6) and 6.00.10(-7) M, respectively, using 1.0 microgram/ml of A23187. In addition, baicalein dose-dependently inhibited beta-glucuronidase and lysozyme releases induced by A23187, leukotriene B4 plus cytochalasin B and platelet-activating factor plus cytochalasin B. Furthermore, baicalein was found to inhibit dose-dependently Ca2+ uptake into the cells and Ca2+ mobilization from the intracellular stores.
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PMID:Effects of baicalein on leukotriene biosynthesis and degranulation in human polymorphonuclear leukocytes. 282 95

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.
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PMID:Comparison of metabolic pharmacokinetics of baicalin and baicalein in rats. 1263 13