Inhibition of rat brain monoamine oxidase activities by psoralen and isopsoralen: Implications for the treatment of affective disorders
Inhibition of rat brain monoamine oxidase activities by psoralen and isopsoralen: Implications for the treatment of affective disorders
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DOI：
10.1034/j.1600-0773.2001.d01-86.x
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发表时间：
2001-02-01
期刊：
影响因子：
--
通讯作者：
Cheng, CHK
中科院分区：
文献类型：
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作者：
Kong, LD;Tan, RX;Cheng, CHK
异戊烯和异戊烯。分离自植物Papplea corylifolia L.的呋喃香豆素，在体外实验中，对大鼠脑线粒体单胺氧化酶（MAO）活性有明显的抑制作用，且对MAO-A的抑制作用优于对MAO-B的抑制作用。发现这种酶活性抑制具有剂量依赖性和可逆性。对于MAO-A，IC 50值为15.2+/-1.3 μ M pepsilen和9.0+/-0.6 μ M isopsilen。对于MAO-B，IC 50值为61.8+/-4.3 μ M pepsilen和12.8+/-0.5 μ M isopsilen。抑制数据的Lineweaver-Burk转换表明，由peguelen和isopuelen两者引起的抑制对MAO-A是非竞争性的。计算出的Ki值为：对于补骨脂素为14.0 μ M，对于异补骨脂素为6.5 μ M。在另一方面，抑制由pegalene和isopalene是竞争性的单胺氧化酶-B。计算出的Ki值对于补骨脂素为58.1 μ M，对于异补骨脂素为10.8 μ M。这些抑制作用的pepsilen和isopsilen对大鼠脑线粒体单胺氧化酶的活动进行了讨论，其毒性和潜在的应用，以治疗情感障碍。
Psoralen and isopsoralen. furocoumarins isolated from the plant Psoralea corylifolia L., were demonstrated to exhibit in vitro inhibitory actions on monoamine oxidase (MAO) activities in rat brain mitochondria, preferentially inhibiting MAO-A activity over MAO-B activity. This inhibition of enzyme activities was found to be dose-dependent and reversible. For MAO-A, the IC50 values are 15.2+/-1.3 muM psoralen and 9.0+/-0.6 muM isopsoralen. For MAO-B, the IC50 values are 61.8+/-4.3 muM psoralen and 12.8+/-0.5 muM isopsoralen. Lineweaver-Burk transformation of the inhibition data indicates that inhibition by both psoralen and isopsoralen is non-competitive for MAO-A. The K-i values were calculated to be 14.0 muM for psoralen and 6.5 muM for isopsoralen. On the other hand, inhibition by both psoralen and isopsoralen is competitive for MAO-B. The K-i values were calculated to be 58.1 muM for psoralen and 10.8 muM for isopsoralen. These inhibitory actions of psoralen and isopsoralen on rat brain mitochondrial MAO activities are discussed in relation to their toxicities and their potential applications to treat affective disorders.