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The metabolism of flavopiridol (FLAP), a novel anticancer drug currently undergoing clinical development, was investigated in rat and human liver microsomes. In the presence of uridine 5'-diphosphoglucuronic acid, two biotransformation products (M1 and M2) could be detected. Formation of metabolite M1 and M2 in terms of enzymatic efficacy (Vmax/K(M)) was(More)
The outer surface of the cells of the hyperthermophile Methanothermus fervidus is covered by crystalline glycoprotein subunits (S-layer). From the purified S-layer glycoprotein, a heterosaccharide was isolated. The heterosaccharide consists of D-3-O-methylmannose, D-mannose, and D-N-acetylgalactosamine in a molar ratio of 2:3:1 corresponding to a relative(More)
Sulfation of resveratrol, a polyphenolic compound present in grapes and wine with anticancer and cardioprotective activities, was studied in human liver cytosol. In the presence of 3'-phosphoadenosine-5'-phosphosulfate, three metabolites (M1-3) whose structures were identified by mass spectrometry and NMR as trans-resveratrol-3-O-sulfate,(More)
From flower heads of Achillea asiatica (L.) Serg., three new guaianolides were isolated by repeated column chromatography and HPLC. The constitution and the stereochemistry of these new, labile compounds were determined by MS, one ((1)H, (13)C, selective (1)H-TOCSY and (1)H-NOESY) and two-dimensional NMR experiments ((1)H, (1)H-COSY, (1)H, (13)C-HSQC, (1)H,(More)
Abietic acid (1) and its methyl ester (2) were investigated under various storage conditions to provide an indication of their preferred oxidation mechanisms and to investigate the most susceptible positions for modification in the abietane skeleton. Six known compounds, methyl 7alpha,13beta-dihydroxyabiet-8(14)-enoate (4a), methyl(More)
Carvedilol, an antihypertensive agent, has been in clinical use for several years. In addition to its function as a beta-blocker, carvedilol has been shown to act as an antioxidant. However, there is some controversy as to how carvedilol achieves its antioxidative ability: by radical scavenging or ion chelation? We therefore used a method of radical(More)
Several problems limit quantification of gluconeogenesis. We applied in vitro 2H-nuclear magnetic resonance (NMR) spectroscopy to simultaneously measure 2H in all glucose carbons for direct assessment of gluconeogenesis. This method was compared with 2H measurement in carbons 5 and 2 using gas chromatography-mass spectrometry (hexamethylenetetramine [HMT])(More)
Resveratrol (3,4',5-trihydroxy- trans-stilbene) is a naturally occurring polyphenolic compound found in grapes, wine and medicinal plants with a variety of biological and pharmacological activities including pronounced anticancer properties. These effects are observed despite its extremely low bioavailability and rapid clearance from the circulation due to(More)