碳酸酐酶抑制剂：一系列酚酸对人红细胞同工酶 I 和 II 的抑制作用。
Carbonic anhydrase inhibitors: Inhibition of human erythrocyte isozymes I and II with a series of phenolic acids.
机构信息
Ataturk University, Department of Chemistry, Erzurum, Turkey.
出版信息
Chem Biol Drug Des. 2010 May;75(5):515-20. doi: 10.1111/j.1747-0285.2010.00965.x.
The inhibitory effects of some phenolic acids on the cytosolic human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes hCA I and hCA II were investigated. Ellagic acid, gallic acid, ferulic acid, caffeic acid, quercetin, p-coumaric acid, p-hydroxybenzoic acid, and syringic acid showed K(I) values in the range of 99-1061 microm for hCA I and of 105-758 microm against hCA II, respectively. Quercetin (for hCA I), p-coumaric acid (for hCA II), and gallic acid (for hCA II) exhibited competitive inhibitory effects with 4-nitrophenyl acetate as substrate. All of the other phenolic acids were found as non-competitive inhibitors with 4-nitrophenylacetate as substrate for hCA I and hCA II. The phenolic acids investigated here showed thus interesting hCA I and hCA II inhibitory effects and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms which have not been yet assayed for their interactions with such agents.
研究了一些酚酸对人胞质碳酸酐酶（hCA，EC 4.2.1.1）同工酶 hCA I 和 hCA II 的抑制作用。鞣花酸、没食子酸、阿魏酸、咖啡酸、槲皮素、对香豆酸、对羟基苯甲酸和丁香酸对 hCA I 的 K（I）值分别在 99-1061 μM 范围内，对 hCA II 的 K（I）值分别在 105-758 μM 范围内。槲皮素（针对 hCA I）、对香豆酸（针对 hCA II）和没食子酸（针对 hCA II）对 4-硝基苯乙酸酯作为底物表现出竞争性抑制作用。其他所有的酚酸均被发现为 hCA I 和 hCA II 的非竞争性抑制剂，以 4-硝基苯乙酸酯作为底物。因此，所研究的酚酸对 hCA I 和 hCA II 具有有趣的抑制作用，并且可能被用作生成酶抑制剂的先导化合物，这些抑制剂可能针对尚未对其与这些化合物的相互作用进行测定的其他 CA 同工酶。
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