Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization
Under healthy conditions, the cornea is an avascular structure which allows for transparency and optimal visual acuity. Its avascular nature is maintained by a balance of proangiogenic and antiangiogenic factors. An imbalance of these factors can result in abnormal blood vessel proliferation into th...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-07-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/25/15/3468 |
| _version_ | 1797560819942162432 |
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| author | Zachary Barry Bomina Park Timothy W. Corson |
| author_facet | Zachary Barry Bomina Park Timothy W. Corson |
| author_sort | Zachary Barry |
| collection | DOAJ |
| description | Under healthy conditions, the cornea is an avascular structure which allows for transparency and optimal visual acuity. Its avascular nature is maintained by a balance of proangiogenic and antiangiogenic factors. An imbalance of these factors can result in abnormal blood vessel proliferation into the cornea. This corneal neovascularization (CoNV) can stem from a variety of insults including hypoxia and ocular surface inflammation caused by trauma, infection, chemical burns, and immunological diseases. CoNV threatens corneal transparency, resulting in permanent vision loss. Mainstay treatments of CoNV have partial efficacy and associated side effects, revealing the need for novel treatments. Numerous natural products and synthetic small molecules have shown potential in preclinical studies in vivo as antiangiogenic therapies for CoNV. Such small molecules include synthetic inhibitors of the vascular endothelial growth factor (VEGF) receptor and other tyrosine kinases, plus repurposed antimicrobials, as well as natural source-derived flavonoid and non-flavonoid phytochemicals, immunosuppressants, vitamins, and histone deacetylase inhibitors. They induce antiangiogenic and anti-inflammatory effects through inhibition of VEGF, NF-κB, and other growth factor receptor pathways. Here, we review the potential of small molecules, both synthetics and natural products, targeting these and other molecular mechanisms, as antiangiogenic agents in the treatment of CoNV. |
| first_indexed | 2024-03-10T18:06:00Z |
| format | Article |
| id | doaj.art-4384f12bb60c4ad3bd08a614ab0260be |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T18:06:00Z |
| publishDate | 2020-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-4384f12bb60c4ad3bd08a614ab0260be2023-11-20T08:30:25ZengMDPI AGMolecules1420-30492020-07-012515346810.3390/molecules25153468Pharmacological Potential of Small Molecules for Treating Corneal NeovascularizationZachary Barry0Bomina Park1Timothy W. Corson2Eugene and Marilyn Glick Eye Institute, Department of Ophthalmology, Indiana University School of Medicine, Indianapolis, IN 46202, USAEugene and Marilyn Glick Eye Institute, Department of Ophthalmology, Indiana University School of Medicine, Indianapolis, IN 46202, USAEugene and Marilyn Glick Eye Institute, Department of Ophthalmology, Indiana University School of Medicine, Indianapolis, IN 46202, USAUnder healthy conditions, the cornea is an avascular structure which allows for transparency and optimal visual acuity. Its avascular nature is maintained by a balance of proangiogenic and antiangiogenic factors. An imbalance of these factors can result in abnormal blood vessel proliferation into the cornea. This corneal neovascularization (CoNV) can stem from a variety of insults including hypoxia and ocular surface inflammation caused by trauma, infection, chemical burns, and immunological diseases. CoNV threatens corneal transparency, resulting in permanent vision loss. Mainstay treatments of CoNV have partial efficacy and associated side effects, revealing the need for novel treatments. Numerous natural products and synthetic small molecules have shown potential in preclinical studies in vivo as antiangiogenic therapies for CoNV. Such small molecules include synthetic inhibitors of the vascular endothelial growth factor (VEGF) receptor and other tyrosine kinases, plus repurposed antimicrobials, as well as natural source-derived flavonoid and non-flavonoid phytochemicals, immunosuppressants, vitamins, and histone deacetylase inhibitors. They induce antiangiogenic and anti-inflammatory effects through inhibition of VEGF, NF-κB, and other growth factor receptor pathways. Here, we review the potential of small molecules, both synthetics and natural products, targeting these and other molecular mechanisms, as antiangiogenic agents in the treatment of CoNV.https://www.mdpi.com/1420-3049/25/15/3468corneal neovascularizationangiogenesisinflammationnatural productssmall moleculesnatural molecules |
| spellingShingle | Zachary Barry Bomina Park Timothy W. Corson Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization Molecules corneal neovascularization angiogenesis inflammation natural products small molecules natural molecules |
| title | Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization |
| title_full | Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization |
| title_fullStr | Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization |
| title_full_unstemmed | Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization |
| title_short | Pharmacological Potential of Small Molecules for Treating Corneal Neovascularization |
| title_sort | pharmacological potential of small molecules for treating corneal neovascularization |
| topic | corneal neovascularization angiogenesis inflammation natural products small molecules natural molecules |
| url | https://www.mdpi.com/1420-3049/25/15/3468 |
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