Retinal Protection of New Nutraceutical Formulation

<b>Background/Objectives:</b> Retinal ganglion cell (RGC) protection represents an unmet need in glaucoma. This study assessed the neuroprotective, antioxidant, and anti-inflammatory effect of a new nutraceutical formulation named Epicolin, based on citicoline, homotaurine, epigallocatec...

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Main Authors: Luca Rosario La Rosa, Veronica Pepe, Francesca Lazzara, Giovanni Luca Romano, Federica Conti, Erika Giuffrida, Claudio Bucolo, Santa Viola, Giuseppe De Pasquale, Maria Cristina Curatolo, Cristina Zappulla
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/1/73
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Summary:<b>Background/Objectives:</b> Retinal ganglion cell (RGC) protection represents an unmet need in glaucoma. This study assessed the neuroprotective, antioxidant, and anti-inflammatory effect of a new nutraceutical formulation named Epicolin, based on citicoline, homotaurine, epigallocatechin-3-gallate, forskolin, and vitamins, through in vitro and in vivo studies. <b>Methods:</b> The neuroprotective effect of Epicolin or its single components, and Epicolin compared to an untreated control and two marketed formulations [Formulation G (FG) and N (FN)], was evaluated in neuroblastoma cells (SH-SY5Y) challenged with staurosporine. The antioxidant potential and the scavenging activity of Epicolin compared to the untreated control, and FG and FN, was evaluated in SH-SY5Y cells and through oxygen radical absorbance capacity acellular assay, respectively. Moreover, the protective effect against hypoxic damage was evaluated in Muller cells (MIO-M1) subjected to hypoxia. The efficacy of Epicolin was also evaluated in DBA/2J glaucomatous mice through the use of a pattern electroretinogram (PERG), immunostaining, and real-time PCR. <b>Results:</b> Among the nutraceutical formulations tested, only Epicolin showed a significant neuroprotective effect on SH-SY5Y attributable to the synergistic action of its single ingredients. As for antioxidant and scavenging activity, Epicolin showed a higher efficacy compared to FG and FN. Furthermore, Epicolin showed the same protective effect on MIO-M1 cells reducing HIF-1α expression. Finally, Epicolin treatment on DBA/2J mice protected the RGCs from loss of function, as demonstrated by PERG analysis, and attenuated their death by enhancing brain-derived neurotrophic factor (<i>BDNF</i>) and reducing interleukin-1 beta (<i>IL-1β</i>) and tumor necrosis factor-alpha (<i>TNF-α</i>) expression. <b>Conclusions:</b> Epicolin, due to its neuroprotective, antioxidant, and anti-inflammatory properties, represents a promising potential treatment for glaucoma.
ISSN:1999-4923