A Novel Class of Dual-Acting DCH-CORMs Counteracts Oxidative Stress-Induced Inflammation in Human Primary Tenocytes
Carbon monoxide (CO) can prevent cell and tissue damage by restoring redox homeostasis and counteracting inflammation. CO-releasing molecules (CORMs) can release a controlled amount of CO to cells and are emerging as a safer therapeutic alternative to delivery of CO in vivo. Sustained oxidative stre...
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2021-11-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_b2ff742f5df44003bbfc475b14a2710c | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Federico Appetecchia |e author |
| 700 | 1 | 0 | |a Sara Consalvi |e author |
| 700 | 1 | 0 | |a Emanuela Berrino |e author |
| 700 | 1 | 0 | |a Marialucia Gallorini |e author |
| 700 | 1 | 0 | |a Arianna Granese |e author |
| 700 | 1 | 0 | |a Cristina Campestre |e author |
| 700 | 1 | 0 | |a Simone Carradori |e author |
| 700 | 1 | 0 | |a Mariangela Biava |e author |
| 700 | 1 | 0 | |a Giovanna Poce |e author |
| 245 | 0 | 0 | |a A Novel Class of Dual-Acting DCH-CORMs Counteracts Oxidative Stress-Induced Inflammation in Human Primary Tenocytes |
| 260 | |b MDPI AG, |c 2021-11-01T00:00:00Z. | ||
| 500 | |a 10.3390/antiox10111828 | ||
| 500 | |a 2076-3921 | ||
| 520 | |a Carbon monoxide (CO) can prevent cell and tissue damage by restoring redox homeostasis and counteracting inflammation. CO-releasing molecules (CORMs) can release a controlled amount of CO to cells and are emerging as a safer therapeutic alternative to delivery of CO in vivo. Sustained oxidative stress and inflammation can cause chronic pain and disability in tendon-related diseases, whose therapeutic management is still a challenge. In this light, we developed three small subsets of 1,5-diarylpyrrole and pyrazole dicobalt(0)hexacarbonyl (DCH)-CORMs to assess their potential use in musculoskeletal diseases. A myoglobin-based spectrophotometric assay showed that these CORMs act as slow and efficient CO-releasers. Five selected compounds were then tested on human primary-derived tenocytes before and after hydrogen peroxide stimulation to assess their efficacy in restoring cell redox homeostasis and counteracting inflammation in terms of PGE<sub>2</sub> secretion. The obtained results showed an improvement in tendon homeostasis and a cytoprotective effect, reflecting their activity as CO-releasers, and a reduction of PGE<sub>2</sub> secretion. As these compounds contain structural fragments of COX-2 selective inhibitors, we hypothesized that such a composite mechanism of action results from the combination of CO-release and COX-2 inhibition and that these compounds might have a potential role as dual-acting therapeutic agents in tendon-derived diseases. | ||
| 546 | |a EN | ||
| 690 | |a CO-releasing molecules | ||
| 690 | |a tenocytes | ||
| 690 | |a PGE<sub>2</sub> | ||
| 690 | |a 1,5-diarylpyrrole | ||
| 690 | |a 1,5-diarylpyrazole | ||
| 690 | |a carbon monoxide | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Antioxidants, Vol 10, Iss 11, p 1828 (2021) | |
| 787 | 0 | |n https://www.mdpi.com/2076-3921/10/11/1828 | |
| 787 | 0 | |n https://doaj.org/toc/2076-3921 | |
| 856 | 4 | 1 | |u https://doaj.org/article/b2ff742f5df44003bbfc475b14a2710c |z Connect to this object online. |