Pannorin isolated from marine Penicillium sp. SG-W3: a selective monoamine oxidase A inhibitor

IF 2.3 3区农林科学 Q3 FOOD SCIENCE & TECHNOLOGY

Applied Biological Chemistry Pub Date : 2024-03-01 DOI:10.1186/s13765-024-00878-7

Jong Min Oh, Qian Gao, Woong-Hee Shin, Eun-Young Lee, Dawoon Chung, Grace Choi, Sang-Jip Nam, Hoon Kim

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Abstract

Six compounds were isolated from Penicillium sp. SG-W3, a marine-derived fungus, and their inhibitory activities against target enzymes relating to neurological diseases were evaluated. Compound 1 (pannorin) was a potent and selective monoamine oxidase (MAO)-A inhibitor with a 50% inhibitory concentration (IC₅₀) of 1.734 μM and a selectivity index (SI) of > 23.07 versus MAO-B, and it showed an efficient antioxidant activity. All compounds showed weak inhibitory activities against acetylcholinesterase, butyrylcholinesterase, and β-secretase. The inhibition constant (K_i) of 1 for MAO-A was 1.049 ± 0.030 μM with competitive inhibition. Molecular docking simulation predicted that compound 1 forms hydrogen bonds with MAO-A, and binds more tightly to MAO-A than to MAO-B (− 25.02 and − 24.06 kcal/mol, respectively). These results suggest that compound 1 is a selective, reversible, and competitive MAO-A inhibitor that can be a therapeutic candidate for treating neurological diseases.

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从海洋青霉 SG-W3 中分离出的 Pannorin：一种选择性单胺氧化酶 A 抑制剂

从海洋源真菌青霉 SG-W3 中分离出了六种化合物，并评估了它们对神经系统疾病相关靶酶的抑制活性。化合物 1（pannorin）是一种强效、选择性的单胺氧化酶（MAO）-A 抑制剂，其 50％抑制浓度（IC50）为 1.734 μM，对 MAO-B 的选择性指数（SI）大于 23.07，并显示出高效的抗氧化活性。所有化合物对乙酰胆碱酯酶、丁酰胆碱酯酶和 β-分泌酶都有微弱的抑制活性。1 对 MAO-A 的抑制常数（Ki）为 1.049 ± 0.030 μM，具有竞争性抑制作用。分子对接模拟预测，化合物 1 与 MAO-A 形成氢键，与 MAO-A 的结合比与 MAO-B 的结合更紧密（分别为 - 25.02 和 - 24.06 kcal/mol）。这些结果表明，化合物 1 是一种选择性、可逆性和竞争性 MAO-A 抑制剂，可作为治疗神经系统疾病的候选药物。

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来源期刊

Applied Biological Chemistry Chemistry-Organic Chemistry

CiteScore

5.40

自引率

6.20%

发文量

审稿时长

20 weeks

期刊介绍： Applied Biological Chemistry aims to promote the interchange and dissemination of scientific data among researchers in the field of agricultural and biological chemistry. The journal covers biochemistry and molecular biology, medical and biomaterial science, food science, and environmental science as applied to multidisciplinary agriculture.