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中草药对单胺氧化酶B(MAO-B)的抑制作用。

Inhibition of monoamine oxidase B (MAO-B) by Chinese herbal medicines.

作者信息

Lin R D, Hou W C, Yen K Y, Lee M H

机构信息

Department of Internal Medicine, Municipal Taipei Ho-Ping Hospital, Taiwan.

出版信息

Phytomedicine. 2003 Nov;10(8):650-6. doi: 10.1078/0944-7113-00324.

Abstract

Monoamine oxidase (MAO) catalyzes the oxidative deamination of biogenic amines accompaned by the release of H2O2. Two subtypes, MAO-A and MAO-B, exist on the basis of their specificities to substrates and inhibitors. The regulation of MAO-B activity is important in the treatment of neurodegenerative diseases. Twenty-seven species of plants used in traditional Chinese medicines, selected from an enthnobotanical survey, were used in an investigation of their inhibitory effect on MAO-B in rat brain homogenates. The 50% aqueous methanol extracts of four active extracts, Arisaema amurense, Lilium brownii var. colchesteri, Lycium chinense, and Uncaria rhynchophylla, exhibited the best activity and selectivity towards MAO-B with IC50 values of 0.44, 0.29, 0.40, and 0.03 mg/ml, respectively. A kinetic study of MAO-B inhibition by the four extracts using the Lineweaver-Burk plot for each active extract revealed the IC50 concentrations, and results show that: Ki = 0.59 mg/ml for A. amurense for the mixed-type mode, Ki = 0.58 mg/ml for L. brownii var. colchesteri for the mixed-type mode, Ki = 5.01 mg/ml for L. chinense for the uncompetitive mode, and Ki = 0.02 mg/ml for U. rhynchophylla for the uncompetitive mode. These may therefore be candidates for use in delaying the progressive degeneration caused by neurological diseases.

摘要

单胺氧化酶(MAO)催化生物胺的氧化脱氨反应,并伴有过氧化氢的释放。根据对底物和抑制剂的特异性,存在两种亚型,即MAO - A和MAO - B。MAO - B活性的调节在神经退行性疾病的治疗中很重要。从民族植物学调查中选出的27种用于传统中药的植物,被用于研究它们对大鼠脑匀浆中MAO - B的抑制作用。四种活性提取物,即东北天南星、百合(卷丹)、枸杞和钩藤的50%甲醇水溶液提取物,对MAO - B表现出最佳的活性和选择性,IC50值分别为0.44、0.29、0.40和0.03 mg/ml。使用Lineweaver - Burk图对每种活性提取物进行MAO - B抑制的动力学研究,得出了IC50浓度,结果表明:东北天南星在混合型模式下的Ki = 0.59 mg/ml,百合(卷丹)在混合型模式下的Ki = 0.58 mg/ml,枸杞在非竞争性模式下的Ki = 5.01 mg/ml,钩藤在非竞争性模式下的Ki = 0.02 mg/ml。因此,这些植物可能是用于延缓神经疾病所致进行性退化的候选药物。

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