Interactions of Desmethoxyyangonin, a Secondary Metabolite from Renealmia alpinia, with Human Monoamine Oxidase-A and Oxidase-B.
Interactions of Desmethoxyyangonin, a Secondary Metabolite from Renealmia alpinia, with Human Monoamine Oxidase-A and Oxidase-B.
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DOI：
10.1155/2017/4018724
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Tekwani BL
中科院分区：
文献类型：
--
作者：
Chaurasiya ND;León F;Ding Y;Gómez-Betancur I;Benjumea D;Walker LA;Cutler SJ;Tekwani BL
高良姜是热带雨林的一种药用植物，用于治疗蛇咬伤和其他伤害，也可用作退烧、止痛、止吐、抗溃疡和抗惊厥药物。高良姜叶二氯甲烷提取物对人单胺氧化酶--(MAOS-)A和MAO-B有较强的抑制作用。植物化学研究表明，化合物6对MAO-B的亲和力比MAO-A高约30倍，Ki值分别为31和922 NM。酶抑制动力学分析和平衡-透析解离实验表明，去甲氧基杨柳素6与MAO-A和MAO-B可逆结合。通过分子模拟算法研究了化合物6在MAO-A和MAO-B同工酶活性部位的结合作用，证实了去甲氧基杨柳素6与MAO-B的结合优先于MAO-A。MAO-B的选择性可逆抑制剂，如去甲氧基杨柳素6，可能对治疗神经退行性疾病具有重要的治疗意义，如帕金森氏病和阿尔茨海默病。
Renealmia alpinia (Zingiberaceae), a medicinal plant of tropical rainforests, is used to treat snakebites and other injuries and also as a febrifuge, analgesic, antiemetic, antiulcer, and anticonvulsant. The dichloromethane extract of R. alpinia leaves showed potent inhibition of human monoamine oxidases- (MAOs-) A and B. Phytochemical studies yielded six known compounds, including pinostrobin 1, 4′-methyl ether sakuranetin 2, sakuranetin 3, pinostrobin chalcone 4, yashabushidiol A 5, and desmethoxyyangonin 6. Compound 6 displayed about 30-fold higher affinity for MAO-B than MAO-A, with Ki values of 31 and 922 nM, respectively. Kinetic analysis of inhibition and equilibrium-dialysis dissociation assay of the enzyme-inhibitor complex showed reversible binding of desmethoxyyangonin 6 with MAO-A and MAO-B. The binding interactions of compound 6 in the active site of the MAO-A and MAO-B isoenzymes, investigated through molecular modeling algorithms, confirmed preferential binding of desmethoxyyangonin 6 with MAO-B compared to MAO-A. Selective reversible inhibitors of MAO-B, like desmethoxyyangonin 6, may have important therapeutic significance for the treatment of neurodegenerative disorders, such as Parkinson's disease and Alzheimer's disease.
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影响因子：
3.7
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