Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 21, Issue 21, Pages -Publisher
MDPI
DOI: 10.3390/ijms21217949
Keywords
antioxidants; free radical scavengers; homo-tris-nitrones; neuroprotection; nitrones; oligomycin A; rotenone; oxygen-glucose-deprivation model; α -phenyl-N-tert-butylnitrone; synthesis
Funding
- Spanish Ministry of Economy and Competitiveness [SAF2015-65586-R]
- Camilo Jose Cela University [UCJC-2018-04]
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Herein we report the synthesis, antioxidant and neuroprotective power of homo-tris-nitrones (HTN) 1-3, designed on the hypothesis that the incorporation of a third nitrone motif into our previously identified homo-bis-nitrone 6 (HBN6) would result in an improved and stronger neuroprotection. The neuroprotection of HTNs 1-3, measured against oligomycin A/rotenone, showed that HTN2 was the best neuroprotective agent at a lower dose (EC50 = 51.63 +/- 4.32 mu M), being similar in EC50 and maximal activity to alpha-phenyl-N-tert-butylnitrone (PBN) and less potent than any of HBNs 4-6. The results of neuroprotection in an in vitro oxygen glucose deprivation model showed that HTN2 was the most powerful (EC50 = 87.57 +/- 3.87 mu M), at lower dose, but 50-fold higher than its analogous HBN5, and approximate to 1.7-fold less potent than PBN. HTN3 had a very good antinecrotic (IC50 = 3.47 +/- 0.57 mu M), antiapoptotic, and antioxidant (EC50 = 6.77 +/- 1.35 mu M) profile, very similar to that of its analogous HBN6. In spite of these results, and still being attractive neuroprotective agents, HTNs 2 and 3 do not have better neuroprotective properties than HBN6, but clearly exceed that of PBN.
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