College of Environment and Resources, Chongqing Technology and Business University, Chongqing 400067, China.
Department of Medicinal Chemistry, School of Pharmacy, Chongqing Medical University, Chongqing 400016, China.
Molecules. 2022 Mar 18;27(6):1984. doi: 10.3390/molecules27061984.
In the present study, we confirmed that α-asaronol, which is a product of the active metabolites of alpha Asarone, did not affect n-butylphthalide efficacy when n-butylphthalide and α-asaronol were co-administered to rats with cerebral ischemia-reperfusion injury. Our research revealed that the co-administration of α-asaronol and n-butylphthalide could further improve neurological function, reduce brain infarct volume, increase the number of Nissl bodies, and decrease the ratios of apoptotic cells and the expression of the caspase-3 protein for cerebral ischemia-reperfusion injury model compared to n-butylphthalide alone. Additionally, α-asaronol could significantly decrease the incidence of post-stroke epilepsy versus n-butylphthalide. This study provides valuable data for the follow-up prodrug research of α-asaronol and n-butylphthalide.
在本研究中,我们证实了当α-细辛脑(α-Asarone 的活性代谢产物之一)与脑缺血再灌注损伤大鼠同时给予丁基苯酞时,α-细辛醇并不影响丁基苯酞的疗效。我们的研究表明,与丁基苯酞单独给药相比,α-细辛醇和丁基苯酞联合给药可进一步改善神经功能,减少脑梗死体积,增加尼氏体数量,降低细胞凋亡率和半胱氨酸天冬氨酸蛋白酶-3 蛋白的表达,减轻脑缺血再灌注损伤模型。此外,α-细辛醇可显著降低丁基苯酞治疗后的卒中后癫痫发生率。本研究为α-细辛醇和丁基苯酞的后续前药研究提供了有价值的数据。