蓝萼甲素的现代研究进展

Glaucocalyxin A： A Review

摘要:

蓝萼甲素（GLA）是由唇形科香茶菜属植物香茶菜中提取分离出来的一种天然二萜类化合物。现代药理研究表明，GLA具有抗炎、抗肿瘤、抗纤维化、改善骨质疏松和保护心血管等多种药理活性，且体内安全性好。此外，针对GLA在植物中含量低、溶解性差、代谢率高、生物利用度低等问题，研究者对其开展了全合成、结构修饰和开发纳米制剂等研究。查阅近5年来国内外有关GLA的文献报道，并对其全合成、药理活性及作用机制、体内代谢转化等进行归纳总结，为明确GLA药理活性的作用机制提供理论基础，以期为GLA的研究开发及进一步的临床应用提供参考。

Abstract:

Glaucocalyxin A （GLA） is a natural diterpenoid extracted from Isodon amethystoides belonging to Labiatae. Modern pharmacological research has shown that GLA has anti-inflammatory， anti-tumor， anti-fibrotic， osteoporosis-ameliorating， and cardiovascular system-protecting activities and good biosafety. However， the low content in plants， poor solubility， high metabolic rate， and low bioavailability limit the application of GLA. To address these issues， researchers have studied the total synthesis， structural modification， and nanomedicine development of GLA. By reviewing the available studies about GLA in the past five years， we summarize the research progress in the total synthesis， pharmacological activities and mechanisms， and in vivo metabolic transformation， aiming to provide a theoretical basis for clarifying the specific mechanisms underlying the pharmacological activities of GLA and for further research， development， and clinical applications of GLA.