2017 ; Vol.27-4: 785~790
|Author||Hyun Woo Lee, Hansol Choi, Sang-Jip Nam, William Fenical, Hoon Kim|
|Place of duty||Department of Pharmacy and Research Institute of Life Pharmaceutical Sciences, Sunchon National University, Suncheon 57922, Republic of Korea|
|Title||Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp. CNQ-027|
J. Microbiol. Biotechnol.2017 ;
|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 μM; in addition, it was found to be highly effective
against MAO-A, with an IC50 value of 6.47 μM. 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 μM) but not for MAO-A (IC50 > 80 μM).
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
Ki values of 0.573 and 0.248 μM, 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.|
|Key_word||Monoamine oxidase, piloquinone, Streptomyces sp. CNQ-027, potent selective inhibitor, competitive inhibitor|
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