title: Inhibition of Monoamine Oxidase by Anithiactins from Streptomyces sp.
abstract: Monoamine oxidase (MAO) is found in most cell types and catalyzes the oxidation of monoamines. Three anithiactins (A-C, modified 2-phenylthiazoles) isolated from Streptomyces sp. were tested for inhibitory activity of two isoforms, MAO-A and MAO-B. Anithiactin A was effective and selective for the inhibition of MAO-A, with an IC50 value of 13.0 µM; however, it was not effective for the inhibition of MAO-B. Anithiactins B and C were weaker inhibitors for MAO-A and MAO-B. Anithiactin A was a reversible and competitive inhibitor for MAO-A with a Ki value of 1.84 µM. The hydrophobic methyl substituent in anithiactin A may play an important role in the inhibition of MAO-A. It is suggested that anithiactin A is a selective reversible inhibitor for MAO-A, with moderate potency, and can be considered a new potential lead compound for further development of novel reversible inhibitors for MAO-A.
authors.affiliation: Department of Pharmacy, Sunchon National University, Suncheon 540-950, Republic of Korea.
authors.forename: Hyun Woo
authors.initials: HW
authors.lastname: Lee
authors.affiliation: Research Institute of Life Pharmaceutical Sciences, Sunchon National University, Suncheon 540-950, Republic of Korea.
authors.forename: Won Kyeong
authors.initials: WK
authors.lastname: Jung
authors.affiliation: Department of Pharmacy, Sunchon National University, Suncheon 540-950, Republic of Korea.
authors.forename: Hee Jung
authors.initials: HJ
authors.lastname: Kim
authors.affiliation: Department of Pharmacy, Sunchon National University, Suncheon 540-950, Republic of Korea.
authors.forename: Yu Seok
authors.initials: YS
authors.lastname: Jeong
authors.affiliation: Department of Chemistry and Nano Science, Ewha Women's University, Seoul 120-750, Republic of Korea.
authors.forename: Sang-Jip
authors.initials: SJ
authors.lastname: Nam
authors.affiliation: Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul 151-747, Republic of Korea.
authors.forename: Heonjoong
authors.initials: H
authors.lastname: Kang
authors.affiliation: Department of Pharmacy, Sunchon National University, Suncheon 540-950, Republic of Korea.|Research Institute of Life Pharmaceutical Sciences, Sunchon National University, Suncheon 540-950, Republic of Korea.
authors.forename: Hoon
authors.initials: H
authors.lastname: Kim
mesh_terms: D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D008995:Monoamine Oxidase / Q000378:metabolism*; D013302:Streptomyces / Q000201:enzymology*; D013844:Thiazoles / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D013844:Thiazoles; C000595539:anithiactin A; C000595540:anithiactin B; C000595541:anithiactin C; D008995:Monoamine Oxidase
keywords: Anithiactin A; Streptomyces sp.; competitive inhibitor; monoamine oxidase; selective inhibitor