龙胆苦苷和龙胆碱的生物转化和药理活性研究进展

Progress in biotransformation and pharmacological activities of gentiopicroside and gentianine

龙胆苦苷是重要的环烯醚萜类成分之一,是龙胆属植物的主要活性成分,具有促进胃排空和肠蠕动,还有保肝、镇痛、抗炎等作用。龙胆碱具有抗炎、解热、镇静催眠、抗惊厥等作用。龙胆苦苷等环烯醚萜类化合物在植物内生真菌、人体肠内菌等生物转化作用下可以转化成龙胆碱和新的活性成分。笔者将龙胆苦苷和龙胆碱近年在药理活性、生物转化和体内代谢研究进行综述,为进一步开发利用环烯醚萜类成分及其代谢产物提供一定的理论依据。

Gentiopicroside is one of important iridoid compounds, and the main active constituents of plants of the genus Gentiana, and can promote the gastric emptying and intestinal peristalsis and protecting liver, analgesic, anti-inflammatory and action. Gentianine has anti-inflammatory, antipyretic, sedative hypnotic, and anticonvulsant effect. Researchers have found that gentiopicroside and other iridoid compounds can be converted to gentianine and novel active components under the action of plant endophytic fungi and human intestinal bacteria. The gentiopicroside and gentianine in recent years in the pharmacological activity, biotransformation and metabolism is summarized in the article, to provide a theoretical basis for the further development and utilization of iridoid compounds and their metabolites.