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.
使用
乙酸诱导的小鼠腹部收缩试验(扭动试验)和尾巴弹跳试验,对七种苦叁碱型
羽扇豆生物碱的镇痛作用进行了研究。(+)-异苦叁碱是(+)-苦叁碱的C-6外消旋体,其镇痛作用是(+)-苦叁碱或喷他佐辛的1/3。实验证明,(+)-异苦叁碱的镇痛作用是通过激活γ-阿片受体实现的,而(+)-苦叁碱的镇痛作用则通过γ-和δ-阿片受体实现。(-)-
槐定碱是(+)-苦叁碱的C-6外消旋体,(+)-槐定醇、(-)-14β-羟基苦叁碱和(+)-苦叁碱N-氧化物具有亲
水基团,而(-)-
槐果碱和(-)-槐果胺则具有双键,它们均未显示出明显的镇痛活性。