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)

A simple, rapid and reproducible method was developed to isolate high-purity baicalin from Scutellariae Radix, the dried roots of Scutellaria baicalensis Georgi. The method involves partition/recrystallization steps without repeated column chromatography or special instruments. Isolated baicalin was characterized by comparisons of TLC, HPLC, IR, MS, and NMR data with an authentic sample. Moreover, beta-glucuronidase hydrolysis of baicalin sequentially yielded glucuronic acid and baicalein as confirmed by co-TLC with authentic samples. The purity of baicalin was more than 97% with yield ca. 8.7% (w/w). The method presented here appears suitable for commercial application.
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PMID:Simple preparation of baicalin from Scutellariae Radix. 1840 79

A series of aromatic aminoketones were synthesized by Mannich reaction. Structures of these compounds were confirmed by 1H NMR, MS and HRMS or element analysis. Pharmacological screening showed that most target compounds inhibited the release of beta-glucuronidase in polymorphonuclear leucocytes by PAF (platelet activating factor) and compounds MA12, MA13, MA18, MA21 and MA33 were more active. The study suggests that target compounds are potential PAF receptor antagonists and their anti-inflammatory activities are due to the inhibition of release of lysosomal enzyme.
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PMID:[Synthesis and antiinflammation activity of aromatic aminoketone compounds, a new type of PAF-receptor antagonist]. 1904 82

Chloramphenicol (CP), a broad spectrum antibiotic, is eliminated in humans by glucuronidation. The primary UGT enzymes responsible for CP O-glucuronidation remain unidentified. We have previously identified the 3-O-CP (major) and 1-O-CP (minor) glucuronides by beta-glucuronidase hydrolysis, liquid chromatography-tandem mass spectrometry, and 1D/2D H NMR. Reaction phenotyping for the glucuronidation of CP with 12 expressed human liver UGT isoforms has identified UGT2B7 as having the highest activity for 3-O- and 1-O-CP glucuronidation with minor contributions from UGT1A6 and UGT1A9. The kinetics of CP 3-O-glucuronidation by pooled human liver microsomes (HLMs) exhibited biphasic Michaelis-Menten kinetics with the apparent high-affinity K(m1) and low-affinity K(m2) values of 46.0 and 1027 microM, whereas expressed UGT2B7 exhibited Michaelis-Menten kinetics with the apparent K(m) value of 109.1 microM. The formation of 1-O-CP glucuronide by pooled HLM and expressed UGT2B7 exhibited substrate inhibition kinetics with apparent K(m) values of 408.2 and 115.0 microM, respectively. Azidothymidine (AZT) and hyodeoxycholic acid (substrates of UGT2B7) inhibited 3-O- and 1-O-CP glucuronidation in pooled HLMs. In 10 donor HLM preparations, both CP 3-O- and CP 1-O-glucuronidation showed a significant correlation with AZT glucuronidation (UGT2B7) (r(s) = 0.85 and r(s) = 0.83, respectively) at 30 microM CP, whereas no significant correlation was observed between CP 3-O-glucuronidation and serotonin glucuronidation (UGT1A6) or propofol glucuronidation (UGT1A9) at this CP concentration. These results suggest that UGT2B7 is the primary human hepatic UDP-glucuronosyltransferase isoform catalyzing 3-O- and 1-O-CP glucuronidation with minor contributions from UGT1A6 and UGT1A9.
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PMID:Identification of human UGT2B7 as the major isoform involved in the O-glucuronidation of chloramphenicol. 2000 37

To search for the chemical constituents possessing anti-inflammatory or cytotoxic activities from plants, Morus wittiorum was investigated for the first time. The stem bark of M. wittiorum was extracted with 95% EtOH. The EtOH extract was fractionationed on silica gel by eluting with petroleum ehter, CHCl3 and EtOAc successively. The further isolation and purification of the EtOAc fraction of 95% EtOH extract was performed by various column chromatography such as silica gel, Sephadex LH-20, RP-C18 column chromatography and so on. The structures of compounds were determined on the basis of spectral analysis such as NMR, MS etc. As a result, nine compounds were isolated including six flavonoids and three stilbenoids and elucidated as quercetin (1), 5, 7, 3', 4'-tetrahydroxy-3-methoxyflavone (2), norartocarpanone (3), dihydrokaempferol (4), euchrenone a7 (5), morachalcone A (6), resveratrol (7), oxyresveratrol (8), 4'-prenyloxyresveratrol (9). Compounds 1-9 were isolated from this plant for the first time, among which compounds 1-8 were evaluated for their anti-inflammatory and cytotoxic activities, respectively. Wherein compounds 6 and 8 showed inhibition to the release of beta-glucuronidase from rat polymorphonuclear leukocyte (PMNs) induced by platelet activating factor (PAF) at a concentration of 10(-5) mol x L(-1). The inhibitory ratios were 76.8%, 94.2% individually. Compounds 2 and 8 exhibited selective cytotoxicity agaist human ovarian cancer (A2780) and human gastric cancer (BGC-823) with IC50 values as 0.66, 1.31 micromol x L(-1) individually.
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PMID:[Phenolic constituents from stem bark of Morus wittiorum and their anti-inflammation and cytotoxicity]. 2124 22

Twenty-one compounds were isolated from an ethanol extract of Machilus wangchiana by a combination of various chromatographic techniques including column chromatography over silica gel and Sephadex LH-20 and reversed-phase HPLC. Their structures were identified by spectroscopic data analysis including optical rotation, UV, IR, MS, and NMR data. The compounds are categorized as eight butanolides (1-8), eight lignans (9-16), and five terpenoids (17-21). Compound 16 is a new natural product with an uncommon heptanorlignan skeleton. Meanwhile, the unique Ginkgo biloba (maidenhair) metabolites ginkgolides A (19) and ginkgolides B (20) were obtained from this material. In the preliminary assays, compound 5 showed selective inhibitory activities against human stomach cancer cells (BGC-823) and ovary cancer cells (A2780) with IC50 values of 0.13 x 10(-6) and 2.66 x 10(-6) mol x L(-1), respectively. Compounds 8 and 9, at 1 x 10(-5) mol x L(-1), showed inhibitory activities against the release of beta-glucuronidase of the polymorphous nuclear leukocytes induced by platelet activating factor (PAF), with inhibition rates of 60.0% and 54.2%.
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PMID:[Chemical constituents from Machilus wangchiana]. 2318 36


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