Regulation of divalent metal transporter-1 by serine phosphorylation.

Divalent metal transporter-1 (DMT1) mediates dietary iron uptake across the intestinal mucosa and facilitates peripheral delivery of iron released by transferrin in the endosome. Here, we report that classical cannabinoids (Δ-tetrahydrocannabinol, Δ-THC), nonclassical cannabinoids (CP 55,940), aminoalkylindoles (WIN 55,212-2) and endocannabinoids (anandamide) reduce Fe and Mn uptake by HEK293T(DMT1) cells stably expressing the transporter. siRNA knockdown of cannabinoid receptor type 2 (CB2) abrogated inhibition.

Automated screening platform with isochronal-parallel analysis and conditioning for rapid method development of chiral separations.

An automated chiral separation-screening platform was developed, allowing separation analysis on one column while another column is simultaneously equilibrated with a different mobile phase (MP). The platform can be set up from usual HPLC components at moderate cost and it considerably speeds up the screening process, allowing numerous chromatographic conditions to be tested within a short period of time and leading to a significant gain in time and productivity in preparative separations.

Small-molecule screening identifies the selanazal drug ebselen as a potent inhibitor of DMT1-mediated iron uptake.

HEK293T cells overexpressing divalent metal transporter-1 (DMT1) were established to screen for small-molecule inhibitors of iron uptake. Using a fluorescence-based assay, we tested 2000 known bioactive compounds to find 3 small molecules that potently block ferrous iron uptake. One of the inhibitors, ebselen, is a seleno compound used in clinical trials as a protective agent against ischemic stroke.

A gamma-glutamyl peptide isolated from onion (Allium cepa L.) by bioassay-guided fractionation inhibits resorption activity of osteoclasts.

One gram of onion added to the food of rats inhibits significantly (p < 0.05) bone resorption as assessed by the urinary excretion of tritium released from bone of 9-week-old rats prelabeled with tritiated tetracycline from weeks 1 to 6. To isolate and identify the bone resorption inhibiting compound from onion, onion powder was extracted and the extract fractionated by column chromatography and medium-pressure liquid chromatography.

Various selected vegetables, fruits, mushrooms and red wine residue inhibit bone resorption in rats.

To make a broad survey of the effect of components of the human diet on bone resorption, a few items from the following categories were added to rat diets: vegetables, fruits, beans, nuts and seeds, mushrooms, carbohydrate sources and beverages. The effect on bone resorption was measured by the urinary excretion of tritium released from bones of 9-wk-old rats prelabeled with tritiated tetracycline from weeks 1 to 6. The number of rats per experiment was 26--6, 5, 5, 5 and 5 in the untreated control group fed the plain semipurified diet, the positive control group fed onions and three groups fed one of the newly investigated items, respectively.