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角蒿生物碱及镇痛活性物质
引用本文:迟玉明,中村基之,赵唏瑛,吉泽丰吉,阎文玫,桥本文雄,野原稔弘,樱田忍. 角蒿生物碱及镇痛活性物质[J]. 天然产物研究与开发, 2005, 17(3): 362-365
作者姓名:迟玉明  中村基之  赵唏瑛  吉泽丰吉  阎文玫  桥本文雄  野原稔弘  樱田忍
作者单位:1. 日本正和药品株式会社,茨城,319-535
2. 北京中医药大学,北京,100029
3. 熊本大学,熊本,862-0973
4. 东北药科大学,仙台,981-0905
摘    要:角蒿(Incarvillea sinensis)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。

关 键 词:生物碱 角蒿 活性物质 镇痛活性 作用机理 先导化合物 化学成分 构效关系 透骨草 单萜 胺类 分离 新药

Incarvilleae Alkaloids and Antinociceptive Substances
CHI Yu-ming,NAKAMURA Motoyuki,ZHAO Xi-ying,YOSHIZAWA Toyokichi,YAN Wen-mei,HASHIMOTO Fumio,NOHARA Toshihiro,SAKURADA Shinobu. Incarvilleae Alkaloids and Antinociceptive Substances[J]. Natural Product Research and Development, 2005, 17(3): 362-365
Authors:CHI Yu-ming  NAKAMURA Motoyuki  ZHAO Xi-ying  YOSHIZAWA Toyokichi  YAN Wen-mei  HASHIMOTO Fumio  NOHARA Toshihiro  SAKURADA Shinobu
Abstract: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.
Keywords:Incarvillea sinensis  monoterpene alkaloid  incarvillateine  antinociceptive effect  
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