Xu Jianhui, Zhao Pan, Pan Wenhao, Zhang Yuanyuan, Liu Junxi
Chinese Academy of Sciences Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou, P.R. China.
University of Chinese Academy of Sciences, Beijing, P.R. China.
Nat Prod Res. 2024 Sep 10:1-7. doi: 10.1080/14786419.2024.2396467.
The inherent structural instability and very low bioavailability of ligustilide (Lig) lead to the limited application of the clinical neuroprotection. We developed a stabilised method for Lig, which involved a chemical synthesis between cyclopropylamine and the active phthalides extract included Lig from (Oliv) Diles or Hort, which generated correspond phthalide derivatives by nucleophilic additive and substituted reaction. During this process, four phthalide derivatives have been obtained and two compounds ( and ) stands out as an unprecedented dimeric phthalide entity. This research has meticulously delineated the stabilised pathway and polymerisation mechanics of Lig or its derivatives, an oxygen/glucose deprived PC12 cells experiment model utilised to screen the anti-stroke activity of this isolated Lig derivatives and the results supported this chemical transformation could achieve the stabilised goal of Lig and improved its anti-oxygen/glucose deprived activity.
藁本内酯(Lig)固有的结构不稳定性和极低的生物利用度导致其在临床神经保护中的应用受限。我们开发了一种藁本内酯的稳定化方法,该方法涉及环丙胺与从藁本(Oliv)Diles或 Hort中提取的含藁本内酯的活性邻苯二甲酸酯提取物之间的化学合成,通过亲核加成和取代反应生成相应的邻苯二甲酸酯衍生物。在此过程中,获得了四种邻苯二甲酸酯衍生物,其中两种化合物( 和 )作为前所未有的二聚体邻苯二甲酸酯实体脱颖而出。本研究详细描述了藁本内酯或其衍生物的稳定化途径和聚合机制,利用氧/葡萄糖剥夺的PC12细胞实验模型筛选这种分离的藁本内酯衍生物的抗中风活性,结果支持这种化学转化可以实现藁本内酯的稳定化目标并提高其抗氧/葡萄糖剥夺活性。