Abstract:
The antinociceptive effects of seven matrine-type lupin alkaloids were
examined using the acetic acid-induced abdominal contraction test (the writhing
test) and the tail-flick test in mice. (+)-Allomatrine, the C-6 epimer of
(+)-matrine, produced the antinociceptive effect at 1/3 potency of (+)-matrine
or pentazocine. It was demonstrated that the antinociceptive effects of (+)-allomatrine
were mediated through the activation of κ-opioid receptors, while the
antinociceptive effect of (+)-matrine was mediated by both μ- and κ-opioid
receptors. (-)-Sophoridine, the C-6 epimer of (+)-matrine, (+)-sophoranol,
(-)-14β-hydroxymatrine and (+)-matrine N-oxide,
which possess a hydrophilic group, and (-)-sophocarpine and (-)-sophoramine
having a double bond(s) did not show significant antinociceptive activity.
Key words:
Sophora
- Leguminosae - lupin alkaloid - derivatives of (+)-matrine - antinociception - κ-opioid receptor
