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Characterization of tryptophan-containing dipeptides for anti-angiogenic effects
Sherif Khedr1,2, Anne Klotzsche-von Ameln1, Maha Khedr3,4
1Institute of Physiology, Faculty of Medicine, Technische Universität Dresden, Dresden, Germany.
Acta Physiologica (Oxford, England)
|September 7, 2020
Summary
The dipeptide WL demonstrates significant anti-angiogenic effects across various models, including in vitro, ex vivo, and in vivo studies. This peptide warrants further investigation for its potential therapeutic applications in diseases involving abnormal blood vessel formation.
Area of Science:
- Biochemistry
- Molecular Biology
- Vascular Biology
Background:
- Neo-angiogenesis is implicated in diseases like tumor growth.
- The anti-angiogenic potential of natural peptides is not fully understood.
- L-glutamyl-L-tryptophan (EW/IM862) has shown in vivo tumor growth inhibition.
Purpose of the Study:
- To explore the anti-angiogenic effects of dipeptides WL, EW, IW, and WE.
- To evaluate the impact of these dipeptides on VEGFR-2 signaling and angiogenesis.
- To identify potent anti-angiogenic dipeptides for further research.
Main Methods:
- Bottom-up strategy evaluating peptide effects on VEGFR-2 signaling.
- Quantification of anti-angiogenic effects using in vitro, ex vivo, and in vivo assays.
- Inclusion of 3D fibrin gel bead assay, mouse aortic ring assay, chorioallantoic membrane assay, matrigel plug assay, and oxygen-induced retinopathy model.
Main Results:
- WL showed the strongest effects on VEGFR-2 phosphorylation and downstream signaling.
- EW significantly inhibited sprout formation in the 3D fibrin gel bead assay.
- Both WL and EW decreased vessel sprouting in the mouse aortic ring assay and reduced blood vessel numbers in the chorioallantoic membrane assay.
- WL and EW treatments nearly abolished VEGF-induced increases in hemoglobin content in the matrigel plug assay.
- WL demonstrated a significant anti-angiogenic effect in the murine oxygen-induced retinopathy model.
Conclusions:
- Comprehensive screening indicates WL possesses anti-angiogenic properties.
- WL's anti-angiogenic effects are validated across in vitro, ex vivo, and in vivo models.
- The dipeptide WL is a promising candidate for further exploration in anti-angiogenic therapies.
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