Chem Biol Drug Des. 2011 Jun;77(6):494-9. doi: 10.1111/j.1747-0285.2011.01104.x. Epub 2011 Mar 25.
Inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II with some natural phenolic derivatives was investigated using the esterase assay with 4-nitrophenyl acetate as substrate. Resveratrol, catechin, silymarin, dobutamin, and curcumin showed K(I) values in the range of 4.47-9.47 mm for hCA I and of 2.86-7.44 μm against hCA II, respectively. These natural product phenols were generally competitive inhibitors with 4-nitrophenylacetate as substrate. Some natural phenols investigated here showed effective hCA II inhibitory effects, in the same range as the clinically used sulfonamide acetazolamide, and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms that have not been yet assayed for their interactions with such agents.
采用 4-硝基苯乙酸酯作为底物的酯酶检测法，研究了一些天然酚类衍生物对两种人胞质碳酸酐酶（hCA，EC 4.2.1.1）同工酶 I 和 II 的抑制作用。白藜芦醇、儿茶素、水飞蓟素、多巴丁胺和姜黄素对 hCA I 的 K(i) 值范围分别为 4.47-9.47mm，对 hCA II 的 K(i) 值范围分别为 2.86-7.44μm。这些天然产物酚类通常是竞争性抑制剂，以 4-硝基苯乙酸酯作为底物。本文研究的一些天然酚类化合物对 hCA II 具有有效的抑制作用，与临床使用的磺胺类药物乙酰唑胺相当，可作为潜在的酶抑制剂先导化合物，可能针对尚未对其与这些药物相互作用进行评估的其他 CA 同工酶。
