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Chromenone Derivatives as Monoamine Oxidase Inhibitors from Marine-Derived MAR4 Clade Streptomyces sp. CNQ-031
- Title
- Chromenone Derivatives as Monoamine Oxidase Inhibitors from Marine-Derived MAR4 Clade Streptomyces sp. CNQ-031
- Authors
- Oh, Jong Min; Lee, Chaeyoung; Nam, Sang-Jip; Kim, Hoon
- Ewha Authors
- 남상집
- SCOPUS Author ID
- 남상집
- Issue Date
- 2021
- Journal Title
- JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY
- ISSN
- 1017-7825
1738-8872
- Citation
- JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY vol. 31, no. 7, pp. 1022 - 1027
- Keywords
- Monoamine oxidases; chromenone derivatives; Streptomyces sp; CNQ-031; reversible competitive inhibitors
- Publisher
- KOREAN SOC MICROBIOLOGY &
BIOTECHNOLOGY
- Indexed
- SCIE; SCOPUS; KCI
- Document Type
- Article
- Abstract
- Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC50) of 2.70 mu M and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC50 of 3.42 mu M and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The K-i value of compound 1 for MAO-A was 0.94 +/- 0.28 mu M, and the K-i values of compound 2 for MAO-A and MAO-B were 3.57 +/- 0.60 and 1.89 +/- 0.014 mu M, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.
- DOI
- 10.4014/jmb.2105.05003
- Appears in Collections:
- 자연과학대학 > 화학·나노과학전공 > Journal papers
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