ACTION OF 2-HYDROXY-4,6-DIMETHOXYACETOPHENONE ISOLATED FROM SEBASTIANIA-SCHOTTIANA
ACTION OF 2-HYDROXY-4,6-DIMETHOXYACETOPHENONE ISOLATED FROM SEBASTIANIA-SCHOTTIANA
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DOI：
10.1055/s-2006-960878
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发表时间：
1990-02-01
期刊：
影响因子：
2.7
通讯作者：
RAE, GA
中科院分区：
文献类型：
--
作者：
CALIXTO, JB;MIGUEL, OG;RAE, GA
本文分析了狼毒的主要成分2-羟基-4，6-二甲氧基苯乙酮（花椒碱）对激动剂和电刺激引起的平滑肌和心肌收缩的抑制作用。花椒碱（30 - 300 μ M）以非竞争性、非选择性、浓度相关的方式抑制由几种激动剂诱导的大鼠子宫、豚鼠回肠和膀胱的收缩，IC 50在47 - 190 μ M之间。通过电刺激豚鼠纵向回肠、膀胱、狗输尿管和大鼠左心房的条引起的抽搐也被累积添加的花椒碱（IC 50在50和480 μ M之间）剂量依赖性地抑制。发现花椒碱是狗输尿管环形平滑肌层自发收缩的有效抑制剂，产生54 μ M的IC 50。重复洗涤所有制剂完全逆转花椒碱的抑制作用。因此，似乎花椒碱诱导由平滑肌和心肌制剂的激动剂或电刺激触发的收缩的直接和非选择性抑制。花椒碱诱导肌肉松弛的机制需要进一步研究。
The inhibitory action of the major constituent of Sebastiania schottiana (Euphorbiaceae), 2-hydroxy-4,6-dimethoxyacetophenone (xanthoxyline) on contractions induced by agonists and electrical stimulation of smooth and cardiac muscle preparations was analysed. Xanthoxyline (30 to 300 .mu.M) inhibited contractions of the rat uterus, guinea-pig ileum, and urinary bladder induced by several agonists in a non-competitive, non-selective, concentration-related manner, with the IC50''s ranging between 47 and 190 .mu.M. Twitches evoked by electrical-stimulation of strips of guinea-pig longitudinal ileum, urinary bladder, dog ureter, and rat left atrium were also inhibited dose-dependently by cumulative additions of xanthoxyline (IC50''s between 50 and 480 .mu.M). Xanthoxyline was found to be a potent inhibitor of spontaneous contractions of the circular smooth muscle layer of the dog ureter, yielding an IC50 of 54 .mu.M. Repeated washing of all preparations completely reversed the inhibitory effects of xanthoxyline. Therefore, it appears that xanthoxyline induces a direct and non-selective inhibition of contractions triggered by agonists or electrical stimulation of smooth and cardiac muscle preparations. The elucidation of the mechanism(s) by which xanthoxyline induced muscle relaxation requires further investigations.