<p>The new chromone derivative 1-[(2-methylpropanoyl)chromone]-<i>β</i>-D-glucopyranoside (<b>1</b>) together with eight known compounds (<b>2–9</b>) were isolated from <i>Humulus lupulus</i> (common hops). The structures of the isolated compounds were confirmed by detailed analyses of NMR and HR-ESI-MS data. The glucose fragment in <b>1</b> was determined as the D-glucoside based on GC analysis. Compounds <b>2</b>, <b>4</b>, and <b>5</b> exhibited significant inhibitory activity against diacylglycerol kinase ζ (DGKζ). Compound <b>5</b> demonstrated strong inhibition of DGKζ with an IC<sub>50</sub> value of 1.60 μM. Molecular docking studies gave important information about the role of the galloyl group in DGKζ inhibition.</p>

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New Phenolic Glycosides from Humulus lupulus and Their Inhibitory Activity Against DGKζ

  • Y. Wang,
  • H. A. Aisa,
  • G. Zou,
  • Z. Li

摘要

The new chromone derivative 1-[(2-methylpropanoyl)chromone]-β-D-glucopyranoside (1) together with eight known compounds (2–9) were isolated from Humulus lupulus (common hops). The structures of the isolated compounds were confirmed by detailed analyses of NMR and HR-ESI-MS data. The glucose fragment in 1 was determined as the D-glucoside based on GC analysis. Compounds 2, 4, and 5 exhibited significant inhibitory activity against diacylglycerol kinase ζ (DGKζ). Compound 5 demonstrated strong inhibition of DGKζ with an IC50 value of 1.60 μM. Molecular docking studies gave important information about the role of the galloyl group in DGKζ inhibition.