Abstract
Vascular endothelial cell growth factor (VEGF) is increased in diabetic macular edema. Compound 49b, a novel β-adrenergic receptor agonist, is protective in a type 1 diabetic rat model. We questioned whether Compound 49b could decrease VEGF levels, suggesting that Compound 49b may be effective against edema. Two-month diabetic rats received topical Compound 49b for 7 days only and/or insulin-like growth factor binding protein 3 (IGFBP-3) siRNA. We also measured endothelial nitric oxide synthase (eNOS) and protein kinase C (PKC)ζ and PKCδ phosphorylation. Retinal endothelial cells (RECs) cultured in high glucose were treated with Compound 49b and IGFBP-3 siRNA for evaluation of the same signaling pathways. Compound 49b significantly decreased VEGF through increased IGFBP-3 in the diabetic retina. Compound 49b also reduced eNOS, PKCζ and PKCδ phosphorylation in the diabetic retina and REC. Compound 49b regulated a number of proteins involved in REC barrier properties.
Keywords:
Beta-adrenergic receptor; VEGF; diabetic retinopathy.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic beta-Agonists / pharmacology*
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Animals
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Cells, Cultured
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Diabetes Mellitus, Experimental / pathology*
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Diabetic Retinopathy / pathology*
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Endothelial Cells / cytology
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Insulin-Like Growth Factor Binding Protein 3 / genetics*
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Isoenzymes / metabolism
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Macular Edema / pathology
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Male
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Nitric Oxide Synthase Type III / metabolism*
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Norepinephrine / analogs & derivatives*
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Norepinephrine / pharmacology
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Phenethylamines / pharmacology*
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Protein Kinase C / metabolism*
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Protein Kinase C-delta / metabolism
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Protein Kinase C-theta
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RNA Interference
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RNA, Small Interfering / genetics
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Rats
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Rats, Inbred Lew
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Retina / cytology
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Retina / pathology
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Streptozocin
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Vascular Endothelial Growth Factor A / metabolism*
Substances
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Adrenergic beta-Agonists
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Insulin-Like Growth Factor Binding Protein 3
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Isoenzymes
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Phenethylamines
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RNA, Small Interfering
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Vascular Endothelial Growth Factor A
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vascular endothelial growth factor A, rat
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Streptozocin
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Nitric Oxide Synthase Type III
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Nos3 protein, rat
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protein kinase C zeta
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Prkcq protein, rat
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Protein Kinase C
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Protein Kinase C-delta
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Protein Kinase C-theta
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Norepinephrine