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| | Antiangiogenic agents | Functional activity (in vivo and in vitro studies) |
|
| VEGF blockers and inhibitors | Soluble truncated VEGF receptors (Flt-1) | Inhibited the growth of human endometrium in mice |
| Anti-human VEGF antibody | Inhibited the growth of human endometrium and decreased the number of endometriotic lesions |
| TNP-470 (lodamin) | Inhibited the number of endometriosis lesions, suppressed the mobilization of circulating endothelial cells and endothelial progenitor cells |
| Endostatin and anginex | Inhibited the number of endometriosis lesions |
| Bevacizumab (recombinant humanized monoclonal antibody that inhibits VEGF) | Inhibited the development and cell proliferation in endometriotic lesions, reduced vascular density, increased apoptosis, and reduced VEGF levels |
| Sorafenib (an orally active multikinase inhibitor) | Interfered with the activity of the VEGF receptor reducing the microvessel density and lesion volume of endometrial implants |
| Romidepsin (a histone deacetylase inhibitor) | Inhibited VEGF gene transcription, protein expression and secretion of VEGF |
| Lipoxin A4 (LXA4, an endogenous eicosanoid) | Reduced the endometriosis lesion size and downregulated inflammation-associated proteins, including IL-6 VEGF and matrix metalloproteinase 9 |
| 4-Hydroxybenzyl alcohol (HBA, a naturally occurring phenolic compound) | Inhibited the initiation of the angiogenic process by downregulating VEGF and matrix-metalloproteinase-(MMP-) 9 expression and by affecting endothelial cell migration |
| Parecoxib (selective COX-2 inhibitor) | Reduced lesion size, microvessel density, the number of macrophages, and the expression of VEGF |
| Epigallocatechin gallate (major constituent of green tea) | Decreased endometriotic lesion size, microvessel diameter and density, and VEGF mRNA expression |
| SU6668 | Suppressed angiogenesis and vessel maturation in endometriotic lesions. |
| Macrophage migration inhibitory factor (MIF) antagonist | Reduced the expression of VEGF, cell adhesion receptors, MMP-2, MMP-9, IL-8, cyclooxygenase (COX)2 |
|
| Other anti-angiogenic agents | Xanthohumol (a prenylated flavonoid) | Inhibited the formation of new blood vessels |
| Rapamycin (an immunosuppressant drug) | Inhibited neovascularization and cell proliferation |
| Retinoic acid | Decreased the volume of endometriotic implants |
| Progestogens (progesterone, dydrogesterone, or its metabolite dihydrodydrogesterone) | Reduced proliferation of endometrial stromal cells and suppressed the transcription of VEGF-A and the microvessel density |
| Statins (atorvastatin, lovastatin) | Inhibited the inflammatory and angiogenic genes COX-2 and VEGF in endometriotic stromal cells |
| Dopamine agonists | Reduced microvessel density and angiogenic gene expression |
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