Stabilised pathway and its anti-oxygen/glucose deprived activity about ligustilide, as a pharmacodynamic marker for Angelica sinensis (Oliv) Diles or Ligusticum chuanxiong Hort

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 Angelica sinensis (Oliv) Diles or Ligusticum chuanxiong Hort, which generated correspond phthalide derivatives by nucleophilic additive and substituted reaction. During this process, four phthalide derivatives have been obtained and two compounds (3 and 4) 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.