Identification and evaluation of a napyradiomycin as a potent Nrf2 activator: antioxidative and anti-inflammatory activities

Title
Identification and evaluation of a napyradiomycin as a potent Nrf2 activator: antioxidative and anti-inflammatory activities
Authors
박기덕박종현최지원김현정김주신김금진남주원진정욱최혁재
Issue Date
2020-12
Publisher
Bioorganic chemistry
Citation
VOL 105, 104434
Abstract
Natural products with antioxidant and anti-inflammatory properties are important sources of therapeutic agents. The nuclear factor E2-related factor 2 (Nrf2)/antioxidant response element (ARE) pathway is a well-known defense system against oxidative stress. In this study, a panel of extracts of plants, fungi, and bacteria were screened for Nrf2 activation in a cell-based assay and a crude extract of cultured marine Streptomyces sp. YP127 was found to activate Nrf2. Chemical investigation of the extracts led to isolation of a series of napyradiomycins that activate Nrf2. Among them, napyradiomycin, 16Z-19-hydroxynapyradiomycin A1 (1) exhibited the highest Nrf2-activating efficacy. Compound 1 was further confirmed to induce both mRNA and protein levels of Nrf2-dependent antioxidant enzyme genes in BV-2 microglial cells and suppress inflammatory mediators and intracellular reactive oxygen species. Our findings confirm the antioxidant and anti-inflammatory properties of compound 1, making it a promising therapeutic natural compound for various diseases associated with oxidative stress and inflammation.
URI
http://pubs.kist.re.kr/handle/201004/72139
ISSN
0045-2068
Appears in Collections:
KIST Publication > Article
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