The comparison of neuroprotective effects of isoliquiritigenin and its Phase I metabolites against glutamate-induced HT22 cell death

Eun Ju Yang, Minjun Kim, Ji Eun Woo, Taeho Lee, Jong Wha Jung, Kyung Sik Song

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

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), 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.

Original languageEnglish
Pages (from-to)5639-5643
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number23
DOIs
StatePublished - 2016

Keywords

  • Butein
  • Glutamate
  • HT22
  • Isoliquiritigenin
  • Neuroprotection
  • Phase I metabolites

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