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

Quercetin, rutin, alphaG-rutin (a water soluble flavonoid), and a mixture of rutin and alphaG-rutin were administered to rats by a single gastric intubation, and their absorption and urinary excretion were examined. The plasma and 24 h urinary levels of aglycons (quercetin and tamarixetin/isorhamnetin) were measured by HPLC after deconjugation with beta-glucuronidase/sulfatase treatment. alphaG-rutin was absorbed more rapidly than quercetin or rutin, and the plasma concentrations of quercetin and tamarixetin/isorhamnetin reached the highest peak level 30 min after dosing. Quercetin, rutin, and the mixture of rutin and alphaG-rutin showed the first peak level 8 h, 8 h, and 30 min after dosing, respectively. The area under the concentration-time curve (AUC) for quercetin in rats administered alphaG-rutin was approximately 4.5- and 2-fold higher than those in rats administered quercetin and rutin, respectively, and was almost the same as that in rats administered a mixture of rutin and alphaG-rutin. The highest 24 h urinary excretion was observed in alphaG-rutin-administered rats. These results suggest that alphaG-rutin is absorbed more efficiently than either quercetin or rutin and that a high plasma concentration can be maintained by supplying rutin and alphaG-rutin in combination.
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PMID:Absorption and urinary excretion of quercetin, rutin, and alphaG-rutin, a water soluble flavonoid, in rats. 1269 73

Determination of quercetin in human plasma was carried out by semi-micro high-performance liquid chromatography with electrochemical detection. Peak heights for quercetin were found to be linearly related to the amount of each quercetin injected from 1.5 to 750 pg. The detection limit (signal-noise ratio, S/N = 3) of the present method for quercetin was 0.3 pg. Glucuronic and sulfate forms of quercetin in plasma were hydrolyzed enzymatically using beta-glucuronidase and sulfatase, respectively. Quercetin in plasma and the hydrolyzed solution were extracted with ethyl acetate and determined by the present method. The time courses of concentrations of quercetin in human plasma showed maxima at 1-1.5 h after ingestion of 340 mL of commercial canned green tea.
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PMID:Determination of quercetin in human plasma after ingestion of commercial canned green tea by semi-micro HPLC with electrochemical detection. 1538 1

Quercetin exhibits a potent anticarcinogenic activity. However, ingested quercetin circulates as the glucuronide/sulfate conjugates, which are less active compared to the aglycone in healthy individuals. This study aimed to develop further understandings of the cancer-preventing mechanism with dietary quercetin. According to a two-stage hepatocarcinogenesis model with N-diethylnitrosamine (DEN) and phenobarbital (PB), preneoplasms were induced specifically in the liver of Fisher 344 rats. In the liver, glutathione S-transferase placental form (GST-P) positive foci were produced 14 weeks later. beta-Glucuronidase activity increased significantly in the liver by 1.2-fold in the DEN/PB group compared to the activity in a saline group. In the kidney, thymus, lung, heart, and plasma, the activities were similar between both groups. When quercetin was dosed intragastrically 15 min before sacrifice, the aglycone level of quercetin in liver was significantly 1.9-fold higher in the DEN/PB group than in the saline group. On the other hand, quercetin was dosed to rats 3 times a week for 14 weeks. The treatment kept the aglycone level of quercetin at a significantly higher level and tended to suppress the formation of GST-P positive foci. The increase in beta-glucuronidase activity with carcinogenesis induction became insignificant following the frequent doses of quercetin. It was considered that quercetin aglycone played a preventative role and, thus, the conjugates were converted to the active aglycone by beta-glucuronidase that was induced by the generation of preneoplasms.
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PMID:Metabolic conversion of dietary quercetin from its conjugate to active aglycone following the induction of hepatocarcinogenesis in fisher 344 rats. 1809 47

Quercetin is an anti-oxidative flavonoid widely distributed in the plant kingdom. Phenolic hydroxyl groups at the B-ring and the 3-position are responsible for its free radical-scavenging activity. Quercetin is commonly present as a glycoside and is converted to glucuronide/sulfate conjugates during intestinal absorption and only conjugated metabolites are therefore found in circulating blood. Although metabolic conversion attenuates its biological effects, active aglycone may be generated from the glucuronide conjugates by enhanced beta-glucuronidase activity during inflammation. With respect to its relationship with molecular targets relevant to cancer prevention, quercetin aglycone has been shown to interact with some receptors, particularly an aryl hydrocarbon receptor, which is involved in the development of cancers induced by certain chemicals. Quercetin aglycone has also been shown to modulate several signal transduction pathways involving MEK/ERK and Nrf2/keap1, which are associated with the processes of inflammation and carcinogenesis. Rodent studies have demonstrated that dietary administration of this flavonol prevents chemically induced carcinogenesis, especially in the colon, whilst epidemiological studies have indicated that an intake of quercetin may be associated with the prevention of lung cancer. Dietary quercetin is, therefore, a promising agent for cancer prevention and further research is warranted.
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PMID:Multitargeted cancer prevention by quercetin. 1846 24


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