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首页> 外文期刊>Journal of biochemical and molecular toxicology >Identification of 7,8-dihydroxy-3-phenylcoumarin as a reversible monoamine oxidase enzyme inhibitor
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Identification of 7,8-dihydroxy-3-phenylcoumarin as a reversible monoamine oxidase enzyme inhibitor

机译：鉴定可逆单胺氧化酶抑制剂的7,8-二羟基-3-苯基伞蛋白

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摘要

We herein report the biological evaluation of 3-arylcoumarin derivatives (3a-l) as potential human monoamine oxidase-A and -B (hMAO-A and hMAO-B) inhibitors. The result indicated that 7,8-dihydroxy-3-(4-nitrophenyl)coumarin (3j) was most effective against MAO-A (inhibition concentration [IC_50] = 6.46 ±0.02 μM) and MAO-B (IC_50 = 3.8±0.3μM) enzymes than other synthesized compounds and reference compounds (pargyline and moclobemide). Furthermore, compound (3j) showed (a) nonselectivity against hMAO enzymes, (b) reversible hMAO enzymes inhibition, and (c) neuroprotection against H_2O_2-treated human neuroblastoma (N2a) cells. Finally, a molecular modeling study revealed that the hMAO enzymes inhibitory activity of the compound (3j) may be due to the orientation where the nitro (NO_2) group lies deep into the receptor and the phenyl ring directed toward flavin adenosine dinucleotide via hydrogen bond interaction, and possible π-π interaction with various important residues. Thus, the results of the present study demonstrate that compound (3j) can be considered as a promising scaffold for the development of hMAO-A and hMAO-B inhibitors.
机译：我们在此报告3-芳基香豆素衍生物（3a-l）作为潜在的人类单胺氧化酶-A和-B（hMAO-A和hMAO-B）抑制剂的生物学评价。结果表明，7,8-二羟基-3-（4-硝基苯基）香豆素（3j）对MAO-A（抑制浓度[IC_50]=6.46±0.02μM）和MAO-B（IC_50=3.8±0.3μM）酶的抑制效果优于其他合成化合物和对照化合物（帕吉林和吗氯贝胺）。此外，化合物（3j）显示出（a）对hMAO酶的非选择性，（b）可逆的hMAO酶抑制，以及（c）对H_2O_2处理的人类神经母细胞瘤（N2a）细胞的神经保护作用。最后，一项分子模拟研究表明，化合物（3j）的hMAO酶抑制活性可能是由于硝基（NO_2）深入受体和苯环的方向，苯环通过氢键相互作用指向黄素腺苷二核苷酸，以及可能与各种重要残基的π-π相互作用。因此，本研究的结果表明，化合物（3j）可以被认为是开发hMAO-a和hMAO-B抑制剂的有希望的支架。

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