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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2025-01-01
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| Online Access: | https://www.mdpi.com/1999-4923/17/1/73 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Luca Rosario La Rosa |
| collection | DOAJ |
| description | <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. |
| format | Article |
| id | doaj-art-34865c837f244badbebe6e06ac24235f |
| institution | Kabale University |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj-art-34865c837f244badbebe6e06ac24235f2025-01-24T13:45:50ZengMDPI AGPharmaceutics1999-49232025-01-011717310.3390/pharmaceutics17010073Retinal Protection of New Nutraceutical FormulationLuca Rosario La Rosa0Veronica Pepe1Francesca Lazzara2Giovanni Luca Romano3Federica Conti4Erika Giuffrida5Claudio Bucolo6Santa Viola7Giuseppe De Pasquale8Maria Cristina Curatolo9Cristina Zappulla10Innovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyDepartment of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, ItalyCenter for Research in Ocular Pharmacology–CERFO, University of Catania, 95125 Catania, ItalyDepartment of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, ItalyDepartment of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, ItalyDepartment of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, ItalyInnovation and Medical Science, SIFI S.p.A., 95025 Aci Sant’Antonio, Italy<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.https://www.mdpi.com/1999-4923/17/1/73retinal functionRGC degenerationneuroprotectiondietary supplementglaucomaciticoline |
| spellingShingle | 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 Retinal Protection of New Nutraceutical Formulation Pharmaceutics retinal function RGC degeneration neuroprotection dietary supplement glaucoma citicoline |
| title | Retinal Protection of New Nutraceutical Formulation |
| title_full | Retinal Protection of New Nutraceutical Formulation |
| title_fullStr | Retinal Protection of New Nutraceutical Formulation |
| title_full_unstemmed | Retinal Protection of New Nutraceutical Formulation |
| title_short | Retinal Protection of New Nutraceutical Formulation |
| title_sort | retinal protection of new nutraceutical formulation |
| topic | retinal function RGC degeneration neuroprotection dietary supplement glaucoma citicoline |
| url | https://www.mdpi.com/1999-4923/17/1/73 |
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