期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 23, 页码 5639-5643出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.10.072
关键词
Isoliquiritigenin; Phase I metabolites; Butein; Neuroprotection; HT22; Glutamate
资金
- Rural Development Administration, Republic of Korea [PJ011344]
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 5 mM 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), 20,4,40,50-tetrahydroxychalcone (2), sulfuretin (3), butein (4), davidigenin (5), and cis-6,40-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. (C) 2016 Elsevier Ltd. All rights reserved.
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