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Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp CNQ-027

Title
Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp CNQ-027
Authors
Lee, Hyun WooChoi, HansolNam, Sang-JipFenical, WilliamKim, Hoon
Ewha Authors
남상집
SCOPUS Author ID
남상집scopus
Issue Date
2017
Journal Title
JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY
ISSN
1017-7825JCR Link1738-8872JCR Link
Citation
vol. 27, no. 4, pp. 785 - 790
Keywords
Monoamine oxidasepiloquinoneStreptomyces sp CNQ-027potent selective inhibitorcompetitive inhibitor
Publisher
KOREAN SOC MICROBIOLOGY & BIOTECHNOLOGY
Indexed
SCIE; SCOPUS; KCI WOS
Abstract
Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an IC50 value of 1.21 mu M; in addition, it was found to be highly effective against MAO-A, with an IC50 value of 6.47 mu M. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B (IC50 = 14.50 mu M) but not for MAO-A (IC50 > 80 mu M). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with K-i values of 0.573 and 0.248 mu M, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.
DOI
10.4014/jmb.1612.12025
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자연과학대학 > 화학·나노과학전공 > Journal papers
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