Abstract
Mitochondria-mediated oxidative stress and apoptosis contribute greatly to early brain injury (EBI) following subarachnoid hemorrhage (SAH). This study hypothesized that activation of melanocortin 1 receptor (MC1R), using BMS-470539, attenuates EBI by controlling mitochondrial metabolism after SAH. Methods: We utilized BMS-470539, MSG-606, selisistat, and PGC-1α to verify the neuroprotective effects of MC1R. We evaluated short- and long-term neurobehavior after SAH. Western blotting, immunofluorescence, and Golgi staining techniques were performed to assess changes in protein levels. Results: The results of western blotting suggested that the expression of SIRT1 and PGC-1α were increased, reaching their peaks at 24 h following SAH. Moreover, BMS-470539 treatment notably attenuated neurological deficits, and also reduced long-term spatial learning and memory impairments caused by SAH. The underlying neuroprotective mechanisms of the BMS-470539/MC1R system were mediated through the suppression of oxidative stress, apoptosis, and mitochondrial fission by increasing the levels of SIRT1, PGC-1α, UCP2, SOD, GPx, Bcl-2, cyto-Drp1, and ATP, while decreasing the levels of cleaved caspase-3, Bax, mito-Drp1, ROS, GSH/GSSG, and NADPH/NADP+ ratios. The neuroprotective effects of the BMS-470539/MC1R system were significantly abolished by MSG-606, selisistat, and PGC-1α siRNA. Conclusions: The activation of MC1R with BMS-470539 significantly attenuated EBI after SAH by suppressing the oxidative stress, apoptosis, and mitochondrial fission through the AMPK/SIRT1/PGC-1α signaling pathway.
| Original language | English |
|---|---|
| Pages (from-to) | 522-539 |
| Number of pages | 18 |
| Journal | Theranostics |
| Volume | 11 |
| Issue number | 2 |
| DOIs | |
| State | Published - Jan 1 2021 |
ASJC Scopus Subject Areas
- Medicine (miscellaneous)
- Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
Keywords
- Melanocortin 1 receptor
- Mitochondrial fission
- Oxidative stress
- Peroxisome proliferator-activated receptor gamma coactivator 1-alpha
- Subarachnoid hemorrhage
- Neuroprotective Agents
- Mitochondria/metabolism
- Oxidative Stress
- Signal Transduction
- Rats
- Male
- Brain Injuries/etiology
- Rats, Sprague-Dawley
- Subarachnoid Hemorrhage/complications
- Sirtuin 1/genetics
- Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha/genetics
- Animals
- AMP-Activated Protein Kinases/genetics
- Apoptosis
- Receptor, Melanocortin, Type 1/genetics
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