Quinolone alkaloids with inhibitory activity against nuclear factor of activated T cells from the fruits of Evodia rutaecarpa.

Nine quinolone alkaloids (1-9) from the fruits of Evodia rutaecarpa were investigated for their inhibitory activity on nuclear factor of activated T cells (NFAT)-dependent transcription in comparison with nuclear factor (NF)-kappa B-dependent transcription using a reporter gene assay. These alkaloids showed inhibitory effects against NFAT activity, with IC(50) values between 0.91 microM and 15.

Novel bioactive and biodegradable glass ceramics with high mechanical strength in the CaO--SiO2--B2O3 system.

Novel bioactive and biodegradable glass ceramics with high mechanical strength in the (50-x/2)CaO. SiO(2)--xB(2)O(3) (4.2 < or = x < or = 17.

Magnesia-doped HA/beta-TCP ceramics and evaluation of their biocompatibility.

The sintering behavior, mechanical properties and biocompatibility of magnesia (MgO)-doped HA/TCP biphasic ceramics were studied. Pure HA/TCP ceramics showed poor sinterability due to the phase transformation of beta- to alpha-TCP. MgO-doped HA/TCP ceramics showed high density without any phase transformation of beta-TCP up to 1300 degrees C, for MgO dopants incorporated into the beta-TCP preferably and increased thermal stability of beta-TCP.

Cytotoxic flavone analogues of vitexicarpin, a constituent of the leaves of Vitex negundo.

Bioassay-guided fractionation of the chloroform-soluble extract of the leaves of Vitex negundo led to the isolation of the known flavone vitexicarpin (1), which exhibited broad cytotoxicity in a human cancer cell line panel. In an attempt to increase the cytotoxic potency of 1, a series of acylation reactions was performed on this compound to obtain its methylated (2), acetylated (3), and six new acylated (4-9) derivatives. Compound 9, the previously unreported 5,3'-dihexanoyloxy-3,6,7,4'-tetramethoxyflavone, showed comparative cytotoxic potency to compound 1 and was selected for further evaluation.

Synergistic antimicrobial activity of metabolites produced by a nonobligate bacterial predator.

A naturally occurring, gram-negative, nonobligate predator bacterial strain 679-2, exhibits broad-spectrum antimicrobial activity that is due, in part, to the production of three extracellular compounds. Antimicrobial-activity-directed fractionation of a culture of strain 679-2 against a panel of microorganisms has led to the isolation of three compounds: pyrrolnitrin, maculosin, and a new compound, which we have named banegasine. Although pyrrolnitrin is well known in the literature, it has not been found in cells with the herbicide maculosin.

Effect of the CYP2D6 genotype on the pharmacokinetics of tropisetron in healthy Korean subjects.

Objective: To evaluate the effect of the CYP2D6 genotype on the pharmacokinetics of tropisetron in healthy Korean subjects.

Methods: A single 5-mg capsule of tropisetron was administered orally to 13 healthy subjects. Plasma concentrations were determined by validated HPLC procedures and data were analyzed by using noncompartmental linear PK methods.

Bioactive prenylated flavonoids from the stem bark of Artocarpus kemando.

Four known prenylated flavonoids, artonins E (1) and O (2), artobiloxanthone (3), and cycloartobiloxanthone (4), were isolated from the stem bark of Artocarpus kemando by bioassay-guided fractionation using the DNA strand-scission and the KB cytotoxicity assays as monitors. Compounds 1 and 3 exhibited strong DNA strand-scission activity, and all four compounds were found to be cytotoxic.

Ellagic acid derivatives and cytotoxic cucurbitacins from Elaeocarpus mastersii.

Bioassay-guided investigation of the bark of Elaeocarpus mastersii using KB (human oral epidermoid carcinoma) cells as a monitor led to the isolation of two cucurbitacins, cucurbitacin D and cucurbitacin F as cytotoxic principles, together with two ellagic acid derivatives, 4'-O-methylellagic acid 3-(2",3"-di-O-acetyl)-alpha-L-rhamnoside (1) and 4,4'-O-dimethylellagic acid 3-(2",3"-di-O-acetyl)-alpha-L-rhamnoside (2). These compounds were evaluated against a panel of human tumor cell lines.