首页> 外文期刊>Pharmacology and Toxicology: An International Journal >Inhibition of rat brain monoamine oxidase activities by psoralen and isopsoralen: implications for the treatment of affective disorders.
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Inhibition of rat brain monoamine oxidase activities by psoralen and isopsoralen: implications for the treatment of affective disorders.

机译:补骨脂素和异补骨脂素抑制大鼠脑单胺氧化酶活性:对情感障碍的治疗意义。

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摘要

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 microM psoralen and 9.0 +/- 0.6 microM isopsoralen. For MAO-B, the IC50 values are 61.8 +/- 4.3 microM psoralen and 12.8 +/- 0.5 microM isopsoralen. Lineweaver-Burk transformation of the inhibition data indicates that inhibition by both psoralen and isopsoralen is non-competitive for MAO-A. The Ki values were calculated to be 14.0 microM for psoralen and 6.5 microM for isopsoralen. On the other hand, inhibition by both psoralen and isopsoralen is competitive for MAO-B. The Ki values were calculated to be 58.1 microM for psoralen and 10.8 microM 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.
机译:补骨脂素和异补骨脂素是从植物补骨脂中分离出来的呋喃香豆素,被证明对大鼠脑线粒体中的单胺氧化酶(MAO)活性具有体外抑制作用,相对于MAO-B活性,其抑制MAO-A的活性优先。发现对酶活性的这种抑制是剂量依赖性的和可逆的。对于MAO-A,IC50值为15.2 +/- 1.3 microM补骨脂素和9.0 +/- 0.6 microM异补骨脂素。对于MAO-B,IC50值为61.8 +/- 4.3 microM补骨脂素和12.8 +/- 0.5 microM异补骨脂素。抑制数据的Lineweaver-Burk转换表明补骨脂素和异补骨脂素的抑制作用对MAO-A是不竞争的。补骨脂素的Ki值经计算为14.0 microM,异补骨脂素的Ki值为6.5 microM。另一方面,补骨脂素和异补骨脂素的抑制作用对MAO-B是竞争性的。补骨脂素的Ki值经计算为58.1 microM,异补骨脂素的Ki值为10.8 microM。讨论了补骨脂素和异补骨脂素对大鼠脑线粒体MAO活性的这些抑制作用,涉及它们的毒性及其在治疗情感障碍中的潜在应用。

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