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The GPCR Antagonistic Drug CM-20 Stimulates Mitochondrial Activity in Human RPE Cells.
- Source :
-
The open biochemistry journal [Open Biochem J] 2022; Vol. 16. Date of Electronic Publication: 2022 Aug 22. - Publication Year :
- 2022
-
Abstract
- Background: Mitochondrial dysfunction in retinal pigment epithelium (RPE) is a pathogenic factor in age-related macular degeneration (AMD). Improvement of mitochondrial function may ameliorate RPE bioenergetics status, which may in turn nourish the retinal photoreceptors against degenerative loss.<br />Objective: The purpose of this study is to examine the G-protein coupled receptor (GPCR) antagonistic drug CM-20 in modulating mitochondrial function in RPE cells.<br />Methods: Human-derived ARPE-19 cell line was differentiated to improve RPE morphology. Dose response of CM-20 was performed to examine mitochondrial membrane potential (MMP). Secondary validation with multiplexed live-cell mitochondrial imaging was performed. Protection of CM-20 to mitochondria against oxidative stress was detected under co-treatment with hydrogen peroxide.<br />Results: Treatment with CM-20 elicited a dose-dependent increase of MMP. Multiplexed live-cell mitochondrial imaging showed consistent increase of MMP at an optimal concentration of CM-20 (12.5 μM). MMP was significantly reduced under hydrogen peroxide-induced oxidative stress and treatment with CM-20 showed rescue effects to MMP.<br />Conclusion: CM-20 increases mitochondrial function and protects mitochondria under oxidative stress. As both GPCRs and mitochondria are potential drug targets, retinal neuroprotective testing of CM-20 is warranted in animal models of retinal degeneration.<br />Competing Interests: CONFLICT OF INTEREST The authors declare no conflict of interest, financial or otherwise.
Details
- Language :
- English
- ISSN :
- 1874-091X
- Volume :
- 16
- Database :
- MEDLINE
- Journal :
- The open biochemistry journal
- Publication Type :
- Academic Journal
- Accession number :
- 36090845
- Full Text :
- https://doi.org/10.2174/1874091X-v16-e2206270