中药对单胺氧化酶抑制作用的研究进展

中药对单胺氧化酶抑制作用的研究进展湖北中医学院附属医院（４３００６１）周群，刘小平脑和神经系统中各种单胺类递质如多巴胺、去甲肾上腺素、５－羟色胺等是在单胺氧化酶（ＭｏｎｏａｍｉｎｅＯｘｉｄａｓｅ，ＭＡＯ）催化下发生氧化脱氨作用的。１９７１年Ｒｏｂｉｓ...     

罗布麻浸膏对小鼠脑内单胺氧化酶活性的影响

目的:研究罗布麻叶对小鼠脑内单胺氧化酶活性的影响。方法:用罗布麻叶醇提物以及醇提物的水萃取部位和氟西汀灌胃小鼠7d后,用UV法测定小鼠脑内单胺氧化酶(MAO)的活性。结果:与0．9％氯化钠溶液组比较,罗布麻叶醇提物的水萃取部位可以显著地降低MAO-A、MAO-B的活性;罗布麻叶醇提物有降低MAO-A、MAO-B的趋势,但作用不显著;氟西汀对MAO-A、MAO-B的活性没有显著的影响。结论:本实验首次发现罗布麻叶醇提物的水萃取部位可以显著地降低小鼠脑内单胺氧化酶的活性,这可能是罗布麻叶抗抑郁作用机理之一。     

何首乌及其制剂对鼠脑单胺氧化酶-B 活性的影响

本文成用放射性同位素14C方法,在体外检测鼠脑内单胺氧化酶-B活性。因该酶活性与年龄成正相关,对研究首乌及其他中药的抗衰老作用是一个较新的参考指标,并讨论了方法学上应注意的事项。     

单胺氧化酶抑制药的药物相互作用

综述单胺氧化酶抑制药与其他药物及食物的相互作用.对近10年来单胺氧化酶及单胺氧化酶抑制药的有关文献进行归纳,发现一系列药物及食物不宜与单胺氧化酶抑制药合用.单胺氧化酶抑制药与其他药物合用时要慎重.     

天麻对小鼠脑内单胺氧化酶活性的影响

目的：考察天麻提取物对D－半乳糖所致亚急性损伤小鼠脑内单胺氧化酶B（MAO－B）活性的影响。方法：采用D－半乳糖诱导小鼠脑内MAO－B活性升高，小鼠腹腔注射（ip)天麻提取物30d后，测定其脑内MAO－B的活性。结果：小鼠ip天麻提取物0．25，0．5，1．0g.kg^-1 30d后，均能显著降低MAO－B活性，与D－半乳糖模型组比较，差异有极显著性（P＜0．01），结论：说明天麻提取物能抑制D－半乳糖所致亚急性损伤小鼠脑内MAO－B的活性，减缓生化损害。     

次黄嘌呤对单胺氧化酶的抑制作用

实验证明给小鼠po次黄嘌呤25～500 mg/kg时,对肝和脑中单胺氧化酶B(MAOB)活性的抑制作用与剂量成明显的量—效关系,对MAO-A活性的抑制较弱,且无明显的量—效关系。给小鼠一次po次黄嘌呤500 mg/kg,于给药后16h,对MAO抑制作用最明显。sc时,对肝中MAO活性抑制也以给药后16 h最明显,但对脑中MAO活性抑制不明显。离体实验证明,次黄嘌呤对MAO-B的抑制为竞争性,对MAO-A则为混合型抑制。     

单胺氧化酶和白蛋白联合测定对肝硬化诊断价值的探讨

病毒性肝炎后肝硬化已成为我国的常见病 ,对肝硬化的早期诊断与适宜治疗 ,对于稳定病情 ,延长患者的生命年限具有积极的意义。为此 ,我们探讨了适合各级医院开展的血清单胺氧化酶 (MAO)和白蛋白 (Alb)联合测定对肝硬化早期诊断的价值。1　材料与方法1.1　材料　 2 6 0例肝病与其它疾病血清标本均采自于本院门诊和住院患者。采取标本后即时完成测定。1.2　方法　检测试剂 :MAO测定试剂盒由温州伊利康生物技术公司提供 (苯醛腙法 ,参考值 <36 U/ ml) ;Alb测定试剂盒由上海科欣生物技术研究所提供 (溴甲酚绿法 ) ,两项测定每批试验均做室内…     

超氧化物歧化酶单胺氧化酶联合检测对肺癌的诊断价值

原发性支气管肺癌是当今危害人类健康最常见的恶性肿瘤之一 ,其中 70 %～ 80 %就诊时已是中、晚期患者 ,从而失去了手术机会 ,而早期发现和早期诊断可使肺癌患者的5 a生存率提高到 80 %,因而肺癌的早期诊断至关重要。近年来 ,肿瘤标记物的研究和发展迅速 ,为肺癌的早期诊断提供了依据 ,但单项指标的检测仍有一定的局限性 ,因此学者们强调多项肿瘤标记物联合检测 ,以利于肺癌的早期准确诊断。本文以我科 1997、1998年度 112例肺癌患者血清的超氧化物歧化酶 (SOD)和单胺氧化酶 (MDA)为观测指标 ,分析讨论肺癌患者与肺部良性病变和正常健康…     

Platelet monoamine oxidase and erythrocyte Catechol-o-Methyltransferase activity in alcoholism and controlled abstinence

This study substantiates previous reports that low platelet monoamine oxidase (MAO) activity is associated with alcoholism. Catechol-o-methyltransferase (COMT) activity in erythrocytes of alcoholics did not differ from that of controls. In 20 male alcoholics low platelet MAO activity was found during the first 3 days after hospitalization. The MAO activity increased in the next 2 weeks of abstinence and then tended to decrease again.     

Effects of UP 614-04, a potential antidepressant,on cerebral monoamine oxidase activity

The effects of UP 614-04, a potential antidepressant agent, and those of some known antidepressant agents on cerebral monoamine oxidase (MAO) activity were compared in rats and mice. Using ex vivo and in vitro techniques, it was shown that UP 614-04, a viloxazine analogue, inhibited cerebral MAO activity in rats and mice ex vivo, but that it was not effective in vitro. Time-course studies revealed that the action of UP 614-04 was more sustained than that of viloxazine, but much less potent or sustained than those of pargyline or isocarboxazide. The effect of UP 614-04 was not selective to the A or B forms of MAO.     

Alterations in monoamine oxidase activity after single and repeated exposure of rats to chlorphentermine

Monoamine oxidase (MAO) activity was determined in rat tissues following in vivo treatments with chlorphentermine (CP). Oxidation of seven amine substrates by liver, lung or brain mitochondrial MAO was investigated at 2 h after a single i.p. injection (60 mg/kg) or after repeated injection (once daily for 3 days, 20 mg/kg, i.p.). Deamination of the type A substrates, norepinephrine, serotonin and octopamine, was decreased significantly in liver, lung and brain after both single and repeated injections. Oxidative deamination of tyramine and dopamine (type A + B substrates) was also lowered in all organs after single and repeated exposure to CP, but to a lesser degree than the type A substrates. However, oxidation of the type B substrates, benzylamine and tryptamine, was unaffected by CP administration in comparison to control. These data indicate that CP is a specific inhibitor of mitochondrial MAO, form A.     

当归注射液对老年小鼠脑、肝脏MAO-B活性的影响

当归注射液不同剂量给老年小鼠灌胃,每天1次,连用4周,可显著降低老年小鼠脑、肝脏MAO-B活性。结果提示、当归注射液具有延缓衰老作用。     

Orientation of oxazolidinones in the active site of monoamine oxidase

Oxazolidinone inhibitors of monoamine oxidase (MAO) and oxazolidinone antibacterials are two distinct classes of drug, often with linear structures and overlapping activities for some derivatives. By synthesizing novel dimerised derivatives with identical substitution of the two C-5 side chains, we have obtained experimental evidence for the orientation of oxazolidinones in the active site of MAO A. Two types of spectral changes, either increasing the absorbance at 510 nm or decreasing it at 495 nm depending on the group nearest to the flavin cofactor, were seen on ligand binding to MAO A. Side chain derivatives with amine substituents are very poor substrates so that it was possible to examine the spectral change due to binding of a substrate before reduction of the flavin occurred. Binding of these amino derivative substrates to MAO A induced a spectral change characterized by a strong decrease in absorbance at 495 nm. These substrates reduced the enzyme fully without any trace of a semiquinone intermediate. Only oxazolidinone inhibitors with a bromo-imidazole substituent increased the yield of semiquinone intermediate obtained during chemical reduction. In accord with the experimental data, results of docking experiments showed that binding of the oxazolidinone ring in the aromatic cage close to the flavin was favored and that the nitrogen of the derivatives that were substrates was within van der Waals distance of N-5 of the flavin.     

Acute dieldrin exposure in relation to brain monoamine oxidase activity and concentration of brain serotonin and 5-hydroxyindoleacetic acid

Rainbow trout, White Leghorn chickens and golden hamsters were administered dieldrin or the vehicle in various dosages and routes of injection. Whole brain serotonin (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) concentrations were measured. In separate experiments, monoamine oxidase (MAO) activity was determined in brain homogenates incubated with pargyline or dieldrin. Serotonin content increased maximally at 10 mg/kg dieldrin. Brain MAO activity was significantly decreased by dieldrin in chicken and hamster, but trout enzyme activity was unaffected. The 5-HIAA content reflected MAO inhibition and interference with 5-HIAA transport from brain.     

Effect of styrene on levels of serotonin,noradrenaline, dopamine and activity of acetyl cholinesterase and monoamine oxidase in rat brain

Oral intubation of styrene (1 ml/kg body weight daily) in adult male albino rats for 15 days produced a significant increase in serotonin and nor-adrenaline but no change in dopamine contents in brain. The brain of treated animals also showed a significant decrease in monoamine oxidase (MAO) but no change in acetyl cholinesterase (AChE) activity. The neurotoxic effects of styrene may be mediated through alterations in levels of these biogenic amines in the brain tissue.     

BCEF0083抗单胺氧化酶作用的研究

目的　研究一种白僵菌代谢产物提取物 (BCEF0 0 83)对单胺氧化酶 (MAO)的抑制作用。方法　提取动物脑组织重线粒体应用荧光分光光度计法检测MAO活性 ;采用大、小鼠体内外给药研究BCEF抗MAO作用的量效、时效关系 ,应用林 -贝氏法测定MAOKm值。结果　小鼠BCEF 50 0mg·kg- 1 ,ig给药后 0 5hMAO活性已有抑制 ,2～ 8h活性抑制明显 ,一次给药后 72h抑制作用基本消失 ;小鼠BCEF50 0、40 0、2 0 0、1 0 0、50、2 5mg·kg- 1 ,ig后 2h取脑组织测MAO活性 ,BCEF对MAO活性的抑制呈现一定的量效关系。BCEF体外给药对大鼠脑组织MAO活性的抑制随药物浓度增加而增强 ,BCEF体外给药对MAO A、MAO B抑制的IC50 (95 %可信限 )分别为 1 2 8 88(82 70～ 2 0 0 86)mg·L- 1 、1 84 1 4 (1 56 1 7～ 2 1 7 1 1 )mg·L- 1 ;BCEF对MAO A ,B抑制呈混合型抑制作用 ,Km值分别为 1 1 97、 8 1 3μmol·L- 1 。结论　BCEF0 0 83体内外给药对大、小鼠脑组织MAO活性具有抑制作用     

Effects of chronic monoamine oxidase inhibitor treatment on biogenic amine metabolism in rat brain.

The effects of acute and chronic administration of phenelzine and tranylcypromine on rat brain monoamine metabolism have been examined. Peak increases in norepinephrine, dopamine and 5-hydroxytryptamine occurred between 1 and 7 days with monoamine oxidase inhibitor treatments followed by a gradual decline in brain monoamines towards control levels with continued chronic drug administration. There was an associated adaptive increase in tryptophan hydroxylase but no change in tyrosine hydroxylase activity with chronic phenelzine treatment. Tranylcypromine did not affect tryptophan hydroxylase or tyrosine hydroxylase activities but was associated with a significant increase in aromatic amino acid decarboxylase activity after 14 and 21 days of treatment.