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Planta Med 1999; 65(3): 230-233
DOI: 10.1055/s-1999-14080
Original Paper

Georg Thieme Verlag Stuttgart · New York

Kappa-Opioid Receptor-Mediated Antinociceptive Effects of Stereoisomers and Derivatives of (+)-Matrine in Mice

Ping Xiao1 , Hajime Kubo1 , Masahiro Ohsawa2 , Kimio Higashiyama1 , Hiroshi Nagase3 , Yu-Ning Yan4 , Jia-Shi Li4 , Junzo Kamei2 , Shigeru Ohmiya1
  • 1Institute of Medicinal Chemistry, Hoshi University, Tokyo, Japan
  • 2Department of Pathophysiology and Therapeutics, Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan
  • 3Basic Research Laboratories, Toray Industries Inc., Kamakura, Japan
  • 4Department of Pharmacognosy, Beijing University of Traditional Chinese Medicine, Beijing, China
Weitere Informationen

Publikationsverlauf

June 29, 19

October 11, 1998

Publikationsdatum:
31. Dezember 1999 (online)

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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