Abstract
Diabetic retinopathy (DR), a secondary complication of diabetes, is a leading cause of irreversible blindness accounting for 5% of world blindness cases in working age. Oxidative stress and inflammation are considered causes of DR. Curcumin, a product with anti-oxidant and anti-inflammatory properties, is currently proposed as oral supplementation therapy for retinal degenerative diseases, including DR. In this study we predicted the pharmacodynamic profile of curcumin through an in silico approach. Furthermore, we tested the anti-oxidant and anti-inflammatory activity of curcumin on human retinal pigmented epithelial cells exposed to oxidative stress, human retinal endothelial and human retinal pericytes (HRPCs) cultured with high glucose. Because currently marketed curcumin nutraceutical products have not been so far evaluated for their ocular bioavailability; we assessed retinal distribution of curcumin, following oral administration, in rabbit eye. Curcumin (10 μM) decreased significantly (p < 0.01) ROS concentration and TNF-α release in retinal pigmented epithelial cells and retinal endothelial cells, respectively. The same curcumin concentration significantly (p < 0.01) protected retinal pericytes from high glucose damage as assessed by cell viability and LDH release. Among the tested formulations, only that containing a hydrophilic carrier provided therapeutic levels of curcumin in rabbit retina. In conclusion, our data suggest that curcumin, when properly formulated, may be of value in clinical practice to manage retinal diseases.
Highlights
Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is an active ingredient extracted from the root of Curcuma longa showing anti-inflammatory and antioxidant properties, to be exploited for treatment of diabetes and diabetic retinopathy (Jimenez-Osorio et al, 2015)
The most interesting targets that are involved in diabetic retinopathy and can bind curcumin were Toll-like 9 (Stewart et al, 2015; Jiang and Chen, 2017) receptor and Akt kinases (RAC serine/threonine protein kinase) (Jacot and Sherris, 2011)
We explored the binding of curcumin as IκKβ inhibitor
Summary
Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is an active ingredient extracted from the root of Curcuma longa showing anti-inflammatory and antioxidant properties, to be exploited for treatment of diabetes and diabetic retinopathy (Jimenez-Osorio et al, 2015). Curcumin was found to be effective in inhibition of retinal vascular leakage in an animal model of diabetic retinopathy (DR) (Li et al, 2016). Early/mild NPDR can progress to moderate/severe NPDR, characterized by retinal hemorrhages and diabetic macular edema (DME). When DR progresses to PDR with DME the risk of retinal detachment and irreversible blindness increases. Diabetic patients need to undergo to early and frequent ophthalmologic examinations in order to monitor the development of retinopathy. There are no therapies of early DR and approved treatments are addressed to DME: photocoagulation laser therapy, intravitreal administration of corticosteroids and anti-VEGF drugs (Wykoff, 2017)
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