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Selective Inhibition of Human Monoamine Oxidase B by 5-hydroxy-2-methyl-chroman-4-one Isolated from an Endogenous Lichen Fungus Daldinia fissa
- Selective Inhibition of Human Monoamine Oxidase B by 5-hydroxy-2-methyl-chroman-4-one Isolated from an Endogenous Lichen Fungus Daldinia fissa
- Jeong, Geum-Seok; Kang, Myung-Gyun; Han, Sang-Ah; Noh, Ji-In; Park, Jong-Eun; Nam, Sang-Jip; Park, Daeui; Yee, Sung-Tae; Kim, Hoon
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- JOURNAL OF FUNGI
- JOURNAL OF FUNGI vol. 7, no. 2
- endogenous lichen fungus; Daldinia fissa; 5-hydroxy-2-methyl-chroman-4-one; selective monoamine oxidase B inhibitor; blood-brain barrier permeability; docking simulation
- SCIE; SCOPUS
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- Inhibitory activities against monoamine oxidases (MAOs) and cholinesterases (ChEs) and antioxidant activity were evaluated for 195 extracts from Ukraine-derived endogenous lichen fungi (ELF). Among them, an ELF13 (identified as Daldinia fissa) extract showed the highest inhibitory activity against MAO-B, and 5-hydroxy-2-methyl-chroman-4-one (HMC) was isolated as a similar to 4-fold selective inhibitor of MAO-B (IC50 = 3.23 mu M) compared to MAO-A (IC50 = 13.97 mu M). HMC is a reversible competitive inhibitor with a K-i value of 0.896 mu M. No cytotoxicity was observed in normal and cancer cells at 50 mu M of HMC. HMC showed blood-brain barrier permeability and high gastrointestinal absorption in silico pharmacokinetics. The docking simulation results showed that the binding affinity of HMC for MAO-B (-7.3 kcal/mol) was higher than that of MAO-A (-6.1 kcal/mol) and that HMC formed a hydrogen bond interaction with Cys172 of MAO-B (distance: 3.656 angstrom), whereas no hydrogen bonding was predicted with MAO-A. These results suggest that HMC can be considered a candidate for the treatment of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.
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