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Oleanolic Acids Inhibit Vascular Endothelial Growth Factor Receptor 2 Signaling in Endothelial Cells: Implication for

Da-Hye Lee1,2, Jungsul Lee3,4, Jongwook Jeon5

  • 1Vascular Microenvironment Laboratory, Department of Pharmacology and Ischemic/Hypoxic Disease Institute, College of Medicine, Seoul National University, Seoul 03080, Korea.

Molecules and Cells
|July 25, 2018
PubMed

Insights

Oleanolic acid, derived from anticancer herbs, inhibits vascular endothelial growth factor receptor 2 (VEGFR-2) activation and angiogenesis. This compound shows therapeutic potential for proangiogenic diseases like retinopathy.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Ophthalmology

Background:

  • Precise control of angiogenesis is crucial, as uncontrolled neovascularization exacerbates disease symptoms.
  • Vascular endothelial growth factor (VEGF)/VEGF receptor 2 (VEGFR-2) signaling is a central pathway regulating angiogenesis in endothelial cells (ECs).
  • Targeting the VEGF/VEGFR-2 pathway offers a strategy for modulating angiogenesis and alleviating disease.

Purpose of the Study:

  • To investigate oleanolic acid, identified from anticancer herbs, as a potential inhibitor of VEGFR-2 signaling and angiogenesis.
  • To evaluate the efficacy of oleanolic acid in inhibiting VEGF-induced angiogenesis both in vitro and in vivo.

Main Methods:

  • Oleanolic acid's binding affinity to VEGFR-2 was assessed using Protein Data Bank (PDB) entry 3CJG.
  • In vitro studies involved assessing oleanolic acid's effect on VEGF-induced VEGFR-2 activation and angiogenesis in human umbilical vascular endothelial cells (HU-VECs).
  • In vivo studies utilized a mouse model of retinopathy of prematurity (ROP) to evaluate oleanolic acid's impact on retinal angiogenesis.

Main Results:

  • Oleanolic acid demonstrated VEGFR-2 binding affinity comparable to a reference drug.
  • The compound effectively inhibited VEGF-induced VEGFR-2 activation and angiogenesis in HU-VECs without exhibiting cytotoxicity.
  • Oleanolic acid significantly inhibited in vivo angiogenesis in the mouse retinopathy of prematurity model.

Conclusions:

  • Oleanolic acid acts as a VEGFR-2 inhibitor, effectively suppressing angiogenesis.
  • The findings support the potential therapeutic application of oleanolic acid for managing proangiogenic diseases.
  • Oleanolic acid shows promise in treating conditions such as retinopathy.
Keywords:
VEGFR-2angiogenesisendothelial cellsoleanolic acidretinopathy of prematurity

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