In vitro glucuronidation of kaempferol and quercetin by human UGT-1A9 microsomes

AbstractFlavonoids are important polyphenolic substances with widespread occurrence in plants and therefore in the human diet. Although considerable work has been done on the pharmacology of flavonoids, the understanding of their metabolism is still incomplete. In this work, the in vitro glucuronidation of the common dietary flavonoids quercetin and kaempferol by human UDP-glucuronosyltransferase microsomes (UGT-1A9) was investigated using HPLC and LC–MS. The two flavonoids were extensively metabolised by this enzyme with four monoglucuronides of quercetin and two of kaempferol being detected after incubation. The presence of a quercetin monoglucuronide in the urine of a volunteer after consumption of Ginkgo biloba tablets was demonstrated

Analysis of imatinib in bone marrow and plasma samples of chronic myeloid leukaemia patients using solid phase extraction LC-ESI-MS

The LC-ESI-MS was developed and validated for the analysis of imatinib in plasma and bone marrow samples using deuterated imatinib (D(8)-IM) as an internal standard. The biological samples were extracted using Strata-X-C SPE cartridges and separated on C<sub>8</sub> column (50 x 3 mm, 3 µm), and methanol: 0.1% formic acid (70:30) was delivered at the rate of 0.7 ml/min as a mobile phase. Imatinib was quantified in samples by monitoring the ions m/z 494.3 for imatinib and 502.3 for D<sub>8</sub>-imatinib on mass spectrometer. The method was linear in the concentration range of 1-1500 ng/250 µl in spiked human plasma samples and limit of quantification was 5 ng/mL. Inter-day and intra-day variations in spiked human plasma spiked with 50, 250 and 500 ng /mL were less than 3.16%. The repeatability and reproducibility and other parameters of the methods were also validated. The method was employed for the analysis of the imatinib in human plasma and bone marrow samples. The drug levels in bone marrow and plasma samples were correlated to the degree of cytogenetic response. No significant difference of imatinib level between blood and bone marrow in IM-treated patients dosed to steady state was observed

Annona muricata (graviola): toxic or therapeutic

This paper examines annona muricata (graviola): toxic or therapeutic

Hardcoding and dynamic implementation of finite automata

The theoretical complexity of a string recognizer is linear to the length of the string being tested for acceptance. However, for some kind of strings the processing time largely depends on the number of states visited by the recognizer at run-time. Various experiments are conducted in order to compare the time efficiency of both hardcoded and table-driven algorithms when using such strings patterns. The results of the experiments are cross-compared in order to show the efficiency of the hardcoded algorithm over its table-driven counterpart. This help further the investigations on the problem of the dynamic implementation of finite automata. It is shown that we can rely on the history of the states previously visited in the dynamic framework in order to predict the suitable algorithm for acceptance testing

Niosomes and polymeric chitosan based vesicles bearing transferrin and glucose ligands for drug targeting

PURPOSE: To prepare polymeric vesicles and niosomes bearing glucose or transferrin ligands for drug targeting. METHODS: A glucose-palmitoyl glycol chitosan (PGC) conjugate was synthesised and glucose-PGC polymeric vesicles prepared by sonication of glucose-PGC/cholesterol. N-palmitoylglucosamine (NPG) was synthesised and NPG niosomes also prepared by sonication of NPG/ sorbitan monostearate/ cholesterol/ cholesteryl poly-24-oxyethylene ether. These 2 glucose vesicles were incubated with colloidal concanavalin A gold (Con-A gold), washed and visualised by transmission electron microscopy (TEM). Transferrin was also conjugated to the surface of PGC vesicles and the uptake of these vesicles investigated in the A431 cell line (over expressing the transferrin receptor) by fluorescent activated cell sorter analysis. RESULTS: TEM imaging confirmed the presence of glucose units on the surface of PGC polymeric vesicles and NPG niosomes. Transferrin was coupled to PGC vesicles at a level of 0.60+/-0.18 g of transferrin per g polymer. The proportion of FITC-dextran positive A431 cells was 42% (FITC-dextran solution), 74% (plain vesicles) and 90% (transferrin vesicles). CONCLUSIONS: Glucose and transferrin bearing chitosan based vesicles and glucose niosomes have been prepared. Glucose bearing vesicles bind Con-A to their surface. Chitosan based vesicles are taken up by A431 cells and transferrin enhances this uptake

Functional correlates of positional and gender-specific renal asymmetry in drosophila

Accordingly, the physical asymmetry of the tubules in the body cavity is directly adaptive. Now that the detailed machinery underlying internal asymmetry is starting to be delineated, our work invites the investigation, not just of tissues in isolation, but in the context of their unique physical locations and milieux

The 50th ASMS Conference on Mass Spectrometry and Allied Topics

Development of new mass spectrometers and implementation of new analytical methods were the central themes of the conference. The majority of oral presentations and posters were concerned with the application of mass spectrometry to pharmaceutical and biotechnological research