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从一种内生地衣真菌中分离出的5-羟基-2-甲基色满-4-酮对人单胺氧化酶B的选择性抑制作用

Selective Inhibition of Human Monoamine Oxidase B by 5-hydroxy-2-methyl-chroman-4-one Isolated from an Endogenous Lichen Fungus .

作者信息

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

机构信息

Department of Pharmacy, and Research Institute of Life Pharmaceutical Sciences, Sunchon National University, Suncheon 57922, Korea.

Department of Predictive Toxicology, Korea Institute of Toxicology, Daejeon 34114, Korea.

出版信息

J Fungi (Basel). 2021 Jan 26;7(2):84. doi: 10.3390/jof7020084.

DOI:10.3390/jof7020084
PMID:33530616
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7911959/
Abstract

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 ) extract showed the highest inhibitory activity against MAO-B, and 5-hydroxy-2-methyl-chroman-4-one (HMC) was isolated as a ~ 4-fold selective inhibitor of MAO-B (IC = 3.23 µM) compared to MAO-A (IC = 13.97 µM). HMC is a reversible competitive inhibitor with a K value of 0.896 µM. No cytotoxicity was observed in normal and cancer cells at 50 µM 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 Å), 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.

摘要

对来自乌克兰的内生地衣真菌（ELF）的195种提取物进行了针对单胺氧化酶（MAO）和胆碱酯酶（ChE）的抑制活性以及抗氧化活性评估。其中，一种ELF13（鉴定为 ）提取物对MAO-B表现出最高的抑制活性，5-羟基-2-甲基色满-4-酮（HMC）被分离出来，相对于MAO-A（IC = 13.97 μM），它是一种对MAO-B的约4倍选择性抑制剂（IC = 3.23 μM）。HMC是一种可逆竞争性抑制剂，K值为0.896 μM。在50 μM的HMC浓度下，正常细胞和癌细胞均未观察到细胞毒性。HMC在计算机模拟药代动力学中显示出血脑屏障通透性和高胃肠道吸收性。对接模拟结果表明，HMC与MAO-B的结合亲和力（-7.3 kcal/mol）高于MAO-A（-6.1 kcal/mol），并且HMC与MAO-B的Cys172形成了氢键相互作用（距离：3.656 Å），而预测与MAO-A没有氢键。这些结果表明，HMC可被视为治疗神经退行性疾病如阿尔茨海默病和帕金森病的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/3dbaca01fa7b/jof-07-00084-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/47117dd44209/jof-07-00084-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/877e4c4e48c2/jof-07-00084-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/008c325f3274/jof-07-00084-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/64fcd3c5de7d/jof-07-00084-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/39c3f7649471/jof-07-00084-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/3dbaca01fa7b/jof-07-00084-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/47117dd44209/jof-07-00084-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/a436b87aa999/jof-07-00084-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/877e4c4e48c2/jof-07-00084-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/008c325f3274/jof-07-00084-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/64fcd3c5de7d/jof-07-00084-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/39c3f7649471/jof-07-00084-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bfe/7911959/3dbaca01fa7b/jof-07-00084-g007a.jpg

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