Kong L D, Cheng Christopher H K, Tan R X
Institute of Functional Biomolecule, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, PR China.
J Ethnopharmacol. 2004 Apr;91(2-3):351-5. doi: 10.1016/j.jep.2004.01.013.
A total of seventeen phytochemicals including seven alkaloids (piperine, strychnine, brucine, stachydrine, tetrandrine, frangchinoline and sinomenine), four phenols (paeonol, honokiol, magnolol and eugenol) and six anthraquinones (emodin, rhein, chrysorphanol, aloe-emodin, physcion and 1,8-dihydroxyanthraquinone) was examined for inhibitory activity of monoamine oxidase (MAO) A and B from rat brain mitochondrial. Among these compounds, piperine and paeonol were found to be inhibitory against MAO A in a dose-dependent manner with IC(50) values of 49.3 and 54.6 microM, respectively. Piperine, paeonol and emodin were shown to inhibit MAO B in a dose-dependent manner with the IC(50) data of 91.3, 42.5 and 35.4 microM, respectively. Lineweaver-Burk transformation of the inhibition data indicated that the inhibitory action of piperine on MAO A was of mixed type, and that of paeonol on the same type of the enzyme was of non-competitive type. For piperine, the K(i) and K(I) were determined to be 35.8 and 25.7microM, respectively. For paeonol, the K(i) was estimated to be 51.1 microM. The inhibition of piperine and paeonol on MAO B was of competitive type with K(i) values of 79.9 and 38.2 microM, respectively. The inhibition of emodin on MAO B was of mixed type with the K(i) and K(I) data of 15.1 and 22.9 microM, respectively. The present investigation showed that the phytochemicals piperine, paeonol and emodin are potent MAO inhibitors whereas other compounds were inactive against any type of MAO at 100 microM in the present assay.
共检测了17种植物化学物质,包括7种生物碱(胡椒碱、士的宁、马钱子碱、水苏碱、粉防己碱、异喹啉和青藤碱)、4种酚类(丹皮酚、厚朴酚、厚朴酚和丁香酚)和6种蒽醌类(大黄素、大黄酸、 Chrysophanol、芦荟大黄素、大黄素甲醚和1,8 - 二羟基蒽醌)对大鼠脑线粒体单胺氧化酶(MAO)A和B的抑制活性。在这些化合物中,发现胡椒碱和丹皮酚对MAO A有剂量依赖性抑制作用,IC(50)值分别为49.3和54.6 microM。胡椒碱、丹皮酚和大黄素对MAO B有剂量依赖性抑制作用,IC(50)数据分别为91.3、42.5和35.4 microM。抑制数据的Lineweaver - Burk转换表明,胡椒碱对MAO A的抑制作用为混合型,而丹皮酚对同一类型酶的抑制作用为非竞争性类型。对于胡椒碱,K(i)和K(I)分别确定为35.8和25.7 microM。对于丹皮酚,K(i)估计为51.1 microM。胡椒碱和丹皮酚对MAO B的抑制作用为竞争性类型,K(i)值分别为79.9和38.2 microM。大黄素对MAO B的抑制作用为混合型,K(i)和K(I)数据分别为15.1和22.9 microM。本研究表明,植物化学物质胡椒碱、丹皮酚和大黄素是有效的MAO抑制剂,而在本试验中,其他化合物在100 microM时对任何类型的MAO均无活性。