It is important that pharmacy students taking basic courses in pharmacology and toxicology are taught about function, regulation and multiplicity of drug metabolizing enzymes. We have developed an easy, reliably reproducible and relatively inexpensive laboratory work based on the different fluoresence properties of coumarin and its metabolites, 7-hydroxycoumarin and 7-O-glucuronide coumarin, to...

Twenty-five compounds, widely occurring in nature, were tested individually in vitro at 0 . 5 and 2 . 0 mM concentrations for effects on two isolates of Poria weirii Murr., a serious root pathogen of conifers in western North America. Growth of both isolates was strongly inhibited in media containing coumarin, 4-hydroxycoumarin, or 7-hydroxycoumarin at either concentration, but o-catechol, sali...

Bis-(4-hydroxycoumarin-3-yl) methane derivatives 3(a-l) were synthesized from 4-hydroxycoumarin and substituted aromatic aldehydes using succinimide-N-sulfonic acid as catalyst and evaluated for their in vitro antileishmanial activity against promastigotes form of Leishmania donovani. Compounds 3a (IC50= 155 μg/mL), 3g (IC50= 157.5 μg/mL) and 3l (IC50= 150 μg/mL) were shown significant antileis...

Herein, the integrated raw data regarding the (1)H-NMR, experiments of Aesculetin, 4-Methylumbelliferone, and umbelliferone, in Acetone-d(6) at 25 °C, are presented for further analysis and comparison purposes, for whom may be interested.

In this study, a fully automated incapillary system was developed to monitor the activity of CYP1A1 (Cytochrome P450, family 1, subfamily A, polypeptide 1) in physiological conditions. Ethoxycoumarin, the selected substrate, undergoes an inline bioreaction in the presence of CYP1A1 supersomes and Nicotinamide adenine dinucleotide phosphate reduced as cofactor, giving rise to hydroxycoumarin, th...

Mutation of a gatekeeper residue, tryptophan 37, in E. coli lipoic acid ligase (LplA), expands substrate specificity such that unnatural probes much larger than lipoic acid can be recognized. This approach, however, has not been successful for anionic substrates. An example is the blue fluorophore Pacific Blue, which is isosteric to 7-hydroxycoumarin and yet not recognized by the latter's ligas...

Silica sodium carbonate (SSC) has been used as a valuable silica-supported catalyst for the preparation of a range of known and novel pyrano coumarins via the three-component reactions of aryl aldehydes, active methylene compound (malononitrile or ethyl cyanoacetate), and hydroxycoumarin (5,7-dihydroxy-4-substituted coumarins or 4-hydroxycoumarin). The heterogeneous catalyst showed much the sam...