角蒿生物碱及镇痛活性物质(英文)

Incarvilleae Alkaloids and Antinociceptive Substances

角蒿(Incarvilleasinensis)为透骨草的主要来源之一,称为“羊角透骨草”,具有祛风除湿、消肿止痛之功效。从其全草分离得到了多种新的单萜生物碱和大环精胺类生物碱,其中单萜生物碱之一角蒿酯碱(incarvillateine),具有很强的镇痛活性,且作用机理不同于吗啡。角蒿酯碱已成为开发新型非麻醉性镇痛新药的重要先导化合物,本文对角蒿的化学成分、镇痛活性、作用机理和构效关系的研究作一综述。

Incarvillae sinensis LAM.,a traditional Chinese medicine,has been used to treat rheumatism and to relieve pain.From the whole plants,a number of novel monoterpene alkaloids and macrocyclic spermine alkaloids have been identified.One of the monoterpene alkaloids,incarvillateine,demonstrated higher antinociceptive effect than morphine in the formalin test,and the mechanism of antinociception was different from that of morphine.Incarvillateine has become an important lead compound for developing new natural medicinal drugs.In this paper,the chemical investigation as well as the biological activity and structure-activity relationship were reviewed.