| In vivo: |
| Planta Med. 2012 Sep;78(14):1543-8. Epub 2012 Jul 16. | | Antinociceptive effects of a chloroform extract and the alkaloid dicentrine isolated from fruits of Ocotea puberula.[Pubmed: 22815198] | The present work describes the chemical characterization of a chloroform fraction (CF) obtained from an extract of Ocotea puberula (Lauraceae) fruits, and preliminary antinociceptive analysis of CF and the alkaloid Dicentrine, isolated from this fraction.
METHODS AND RESULTS:
CF (30-300 mg/kg, p. o.) caused dose-related inhibition of abdominal constrictions caused by acetic acid and also inhibited both phases of formalin-induced nociception. Furthermore, Dicentrine (30-300 mg/kg, p. o.) produced dose-related inhibition of acetic acid-induced pain without causing changes in the motor performance of mice.
CONCLUSIONS:
The results show, for the first time, that CF from Ocotea puberula fruits produced marked antinociception in different models of chemical pain, and this effect appears to be, at least in part, due to the presence of Dicentrine. The mechanism by which CF and the alkaloid produced antinociception still remains unclear, but the adenosinergic or opioid system seems unlikely to be involved in this action. | | Drug Metab Dispos. 2010 Oct;38(10):1714-22. | | Metabolism of dicentrine: identification of the phase I and phase II metabolites in miniature pig urine.[Pubmed: 20622045] |
METHODS AND RESULTS:
The metabolic profile of Dicentrine, a selective α(1)-adrenoceptor antagonist with potent antiarrhythmic and antihypertensive activities, in miniature pig urine via oral administration was investigated for the first time. The urine, collected after a single oral administration of Dicentrine, was pretreated using solvent extraction and column chromatographic methods to identify the metabolites containing fractions.
CONCLUSIONS:
The phase I metabolic transformations of Dicentrine were found to be N-demethylation, N-oxidation, O-demethylation (9,10-OMe), O,O-demethylenation (1-OCH(2)O-2), and hydroxylation at the benzylic (C-4) and the aromatic (C-3) positions, whereas those for the phase II were O-glucuronidation and O-glucosylation of the phenolic group of the phase I metabolites. |
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