Kappa-opioid receptor-mediated antinociceptive effects of stereoisomers and derivatives of (+)-matrine in mice

• Published in: Planta medica Vol. 65; no. 3; pp. 230 - 233
• Main Authors: Xiao, P, Kubo, H, Ohsawa, M, Higashiyama, K, Nagase, H, Yan, Y, Li, J, Kamei, J, Ohmiya, S
• Format: Journal Article
• Language: English
• Published: Germany 01.04.1999
• Subjects: alkaloids; Alkaloids - chemistry; Alkaloids - pharmacology; Analgesics - chemistry; Analgesics - pharmacology; Animals; antinociceptive properties; chemical structure; dosage; dose response; Fabaceae - chemistry; Male; medicinal properties; Mice; Mice, Inbred ICR; pain; Plants, Medicinal; Quinolizines; receptors; Receptors, Opioid, kappa - drug effects; Sophora; sophora alopeculoides; Stereoisomerism; structure-activity relationships
• ISSN: 0032-0943; 1439-0221
• DOI: 10.1055/s-1999-14080

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 kappa-opioid receptors, while the antinociceptive effect of (+)-matrine was mediated by both mu- and kappa-opioid receptors. (-)-Sophoridine, the C-6 epimer of (+)-matrine, (+)-sophoranol, (-)-14 beta-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.