异甘草素
甘草苷元
神经保护
化学
药理学
代谢物
查尔酮
谷氨酸受体
氧化应激
程序性细胞死亡
生物化学
立体化学
医学
细胞凋亡
替代医学
受体
病理
作者
Eun‐Ju Yang,Minjun Kim,Ji Eun Woo,Tae‐Ho Lee,Jae‐Kyung Jung,Kyung‐Sik Song
标识
DOI:10.1016/j.bmcl.2016.10.072
摘要
It is becoming increasingly important to investigate drug metabolites to evaluate their toxic or preventive effects after administration of the parent compound. In our previous study, isoliquiritigenin isolated from Glycyrrhizae Radix effectively protected mouse-derived hippocampal neuronal cells (HT22) against 5mM glutamate-induced oxidative stress. However, there is little information on the protective effects of the metabolites of isoliquiritigenin on HT22 cells. In this study, isoliquiritigenin and its Phase I metabolites were prepared and their neuroprotective activities on glutamate-treated HT22 cells were compared. The prepared metabolites were liquiritigenin (1), 2',4,4',5'-tetrahydroxychalcone (2), sulfuretin (3), butein (4), davidigenin (5), and cis-6,4'-dihydroxyaurone (6). Among the six metabolites, 4 showed better neuroprotective effects than the parent compound, isoliquiritigenin. Our study suggests that the neuroprotective effect of isoliquiritigenin could be elevated by its active metabolite 4, which is a chalcone containing a catechol group in the B ring.
科研通智能强力驱动
Strongly Powered by AbleSci AI