Antioxidant, anti-inflammatory, and neuroprotective effects of novel vinyl sulfonate compounds as Nrf2 activator

Title
Antioxidant, anti-inflammatory, and neuroprotective effects of novel vinyl sulfonate compounds as Nrf2 activator
Authors
배애님박기덕박종현최지원신수정김현지김현정이회진Yong Sun Bahn
Issue Date
2019-07
Publisher
ACS MEDICINAL CHEMISTRY LETTERS
Citation
VOL 10-1067
Abstract
The main pathway responsible for cellular regulation against oxidative stress is nuclear factor E2-related factor-2 (Nrf2) signaling. We previously synthesized and reported a novel vinyl sulfone (1) as an Nrf2 activator with therapeutic potential for Parkinson’s disease (PD). In this study, we changed the vinyl sulfone to vinyl sulfonamide or vinyl sulfonate to improve Nrf2 activating efficacy. We observed that the introduction of vinyl sulfonamide led to a reduction of the effects on Nrf2 activation, whereas vinyl sulfonate compounds exhibited superior activity compared to the vinyl sulfone compounds. Among the vinyl sulfonates, 3c exhibited 6.9- and 83.5-fold higher effects on Nrf2 activation than the corresponding vinyl sulfone (1) and vinyl sulfonamide (2c), respectively. Compound 3c was confirmed to induce expression of the Nrf2-dependent antioxidant enzymes at the protein level in cells. In addition, 3c mitigated PD-associated behavioral deficits by protecting DAergic neurons in the MPTP-induced mouse model of PD.
URI
http://pubs.kist.re.kr/handle/201004/69837
ISSN
1948-5875
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KIST Publication > Article
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