Choi, Ji Won Kim, Geum Jin Kim, Hyeon Jeong Nam, Joo-Won Kim, Jushin Chin, Jungwook Park, Jong-Hyun Choi, Hyukjae Park, Ki Duk 2024-01-19T16:02:39Z 2024-01-19T16:02:39Z 2021-09-02 2020-12 0045-2068 https://pubs.kist.re.kr/handle/201004/117784 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. English ACADEMIC PRESS INC ELSEVIER SCIENCE NEURODEGENERATIVE DISEASES OXIDATIVE STRESS SULFORAPHANE INDUCTION COMPOUND A1 Identification and evaluation of a napyradiomycin as a potent Nrf2 activator: Anti-oxidative and anti-inflammatory activities Article 10.1016/j.bioorg.2020.104434 1 BIOORGANIC CHEMISTRY, v.105 BIOORGANIC CHEMISTRY 105 scie scopus 000603572800010 2-s2.0-85095420930 Biochemistry & Molecular Biology Chemistry, Organic Biochemistry & Molecular Biology Chemistry Article NEURODEGENERATIVE DISEASES OXIDATIVE STRESS SULFORAPHANE INDUCTION COMPOUND A1 Napyradiomycin Nrf2 activator Oxidative stress Antioxidant Anti-inflammation