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Flavonoid Compounds Contained in Epimedii Herba Inhibit Tumor Progression by Suppressing STAT3 Activation in the

Cheng Pan1, Yukio Fujiwara1, Hasita Horlad1

  • 1Department of Cell Pathology, Graduate School of Medical Sciences, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan.

Frontiers in Pharmacology
|April 8, 2020
PubMed

Insights

Compounds from Epimedii Herba, particularly epimedokoreanin B, inhibit M2-like tumor-associated macrophages (TAMs). This action suppressed tumor growth and may offer new therapeutic strategies for malignant tumors.

Area of Science:

  • Immunology
  • Pharmacology
  • Oncology

Background:

  • M2-like tumor-associated macrophages (TAMs) promote tumor progression and are potential therapeutic targets.
  • Epimedii Herba is a traditional herbal medicine with potential antitumor properties.

Purpose of the Study:

  • To investigate whether Epimedii Herba compounds inhibit M2 macrophage polarization and prevent tumor progression.
  • To identify specific active compounds and their mechanisms of action.

Main Methods:

  • Human monocyte-derived macrophages (HMDMs) were used to assess M2 polarization markers (CD163, IL-10) and STAT3 activation.
  • In vitro studies utilized Saos-2 and LM8 sarcoma cell lines to evaluate the effects of compounds on proliferation and STAT3 activation.
  • An in vivo murine model (LM8 tumor-bearing mice) was employed to assess the antitumor effects of epimedokoreanin B via oral administration.

Main Results:

  • Four Epimedii Herba flavonoids (limonianin, epimedokoreanin B, icaritin, desmethylicaritin) inhibited M2 markers (CD163, IL-10).
  • Epimedokoreanin B and limonianin suppressed STAT3 activation in HMDMs.
  • Epimedokoreanin B inhibited sarcoma cell proliferation by blocking STAT3 activation and reduced tumor growth in vivo.

Conclusions:

  • Epimedii Herba compounds, especially epimedokoreanin B, can inhibit M2 macrophage polarization.
  • Epimedokoreanin B demonstrates direct antitumor effects by suppressing STAT3 activation and proliferation.
  • Epimedii Herba and its derivatives show potential as novel therapeutic agents for malignant tumors by targeting TAMs and the tumor microenvironment.
Keywords:
Epimedii HerbaSTAT3flavonoidmacrophagetumor cells

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