8 Incarvilleae Alkaloidsと鎮痛・鎮静活性成分(口頭発表の部)

概要

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The whole plant of Incarvillea sinensis has been used as anti-rheumatic and analgesic medicine in China. We have examined the constituents of this crude drug in order to reveal active principle(s), and obtained a number of novel alkaloids, which were classified into two groups: monoterpene alkaloid derivatives (1-10) and spermine related compounds (12-17), whose chemical structures have been clarified by the mass measurements, various NMR techniques and X-ray analyses. In parallel with this chemical investigation, the anti-inflammatory and analgesic activities of several fractions derived from the methanolic extract have been examined by formalin test in mice. This test has revealed that incarvillateine (8) has strong analgesic and sedative activities: Compound 8 (10mg/kg, i.p.) gradually inhibited both the first (neurogenic) and second (inflammatory) phases of formalin-induced pain and reduce the spontaneous motor activity. In this experiment, it has been suggested that anti-inflammatory and analgesic activity of 8 might be induced by its sedative action. However, 8 has showed the analgesic action for this test even in the range of 1-5mg/kg, i.p., in which 8 didn't show the effect toward the spontaneous motor activity in mice. Therefore, it has become clear that 8 could be accounted for the analgesic and sedative substance, whose actions are related to influence on the central nervous system.
天然有機化合物討論会の論文
1996-09-02