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...     

小柴胡汤对大鼠肝线粒体的单胺氧化酶的抑制作用

小柴胡汤对大鼠肝线粒体单胺氧化酶B(MAO-B)有显著的抑制作用。IC~(50)为91.20mg/ml.单味药研究表明,组成小柴胡汤的7味中药显著地抑制MAO-B活性。按作用强弱依次为甘草>半夏>柴胡>党参>大枣>生姜>黄芩。动力学研究表明,小柴胡汤对MAO-B活性抑制作用属底物竞争性抑制。提示小柴胡汤对肝脏疾患及神经功能失调的治疗作用可能与其对MAO的抑制有关。     

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.     

遍地金提取物对大鼠脑突触体单胺氧化酶抑制作用

目的 评价遍地金提取物对大鼠脑突触体单胺氧化酶的抑制作用。方法 通过大鼠脑突触体单胺氧化酶的抑制实验，测定其重摄取量cmp及抑制百分率。结果 遍地金提取物浓度为48．66mg／ml时取得最大抑制百分率96．87％，St．John’s Wort提取物浓度为11．44mg／ml时取得最大抑制百分率99．74％。结论 遍地金提取物与抗抑郁药物St．John‘s Wort均能抑制大鼠脑突触体单胺氧化酶的活性，二者差异无统计学意义。     

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…     

以单胺氧化酶B为靶点的抗帕金森病药物的研究进展

单胺氧化酶B（MAO-B）抑制剂包括可逆性抑制剂和不可逆性抑制剂,可用于帕金森病的治疗。不可逆性抑制剂的副作用较大,临床应用受到限制。寻求抑制性强、选择性高、毒副作用小的MAO-B可逆性抑制剂已成为药物化学研究的热点。本文回顾了近年对MAO-B抑制剂的研究进展,按照化学结构进行了分类阐述,并对其作用机制进行了概括性的总结。     

高效液相色谱法测定单胺氧化酶B

<正> 单胺氧化酶B(MAO—B)与人体衰老过程有密切关系。测定MAO—B含量可作为研究衰老及抗衰老药筛选的一种指标。常用的同位素法虽具有特异性且敏感性高,但价格较昂贵,且国内~(14)C—标记的底物来源尚有困难。高效液相色谱法(HPLC)也是测定脑内儿茶酚胺代谢酶的一种精确、敏感的方法。作者通过实践.对Nissinen E,方法作了修改。现报道如下。1 原理     

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。     

EFFECT OF STYRENE ON MONOAMINE OXIDASE B ACTIVITY IN RAT BRAIN

Previous studies have indicated that workers exposed to styrene present a decreased activity of platelet monoamine oxidase B (MAO B), suggesting that this biochemical assay may represent a biomarker for styrene-induced neurotoxicity. This study was undertaken to determine whether exposure to styrene would cause changes in MAO B activity in the target organ-the brain. Groups of rats were exposed to styrene by inhalation at concentrations of 300 ppm for 4 wk or 50 ppm for 13 wk. Both treatments caused significant decreases of MAO B activity in several brain areas, while MAO A activity was not affected. Decreases in MAO B activity were also found in brainstem of rats given styrene (400 mg/ kg) or styrene oxide (100 mg/ kg) by ip injection for 2 wk. Styrene, styrene oxide, and other styrene metabolites (mandelic acid, phenylglyoxylic acid, and styrene glycol) had no direct inhibitory effect on brain MAO B activity when tested in vitro. These results indicate that exposure to low concentrations of styrene alters MAO B activity in rat brain, suggesting that the observed changes in human platelets may reflect alterations in the nervous system.     

LACK OF EFFECT OF CHLORAMPHENICOL ON MONOAMINE, DIAMINE AND PLASMA AMINE OXIDASE ACTIVITIES

Chloramphenicol treatment in rabbits (60 mg/kg i.m. for 5 days) did not affect significantly (P greater than 0.1) the activities of monoamine oxidase (MAO) or diamine oxidase (DAO) in liver, heart or brain. Plasma amine oxidase (PAO) was not significantly inhibited (P greater than 0.1) in goats treated with chloramphenicol (60 mg/kg i.m. for 5 days). Chloramphenicol (2 X 10(-3) mol/l) preincubated with rabbit hepatic MAO had no significant effect (P greater than 0.1) on the enzyme activity.     

肼类和非肼类化合物抑制单胺氧化酶作用的研究

本文除报导了筛选单胺氧化酶抑制剂(MAOI)的常规。并讨论了非肼类和肼类化合物(包括吲哚类、氨基酸类、胍类、石蒜生物碱、及酰肼类)等49种药物的初筛结果。经体外、体内筛选和毒性试验,发现4-硫杂庚二酰(2-异丙基)肼,简称硫双肼(CH-6),具有较强的抑制单胺氧化酶的作用,作用强度与苯乙肼相似。毒性较低,仅为苯乙肼的1/50。     

PLATELET MONOAMINE OXIDASE ACTIVITY IN PATIENTS WITH HUNTINGTON''S DISEASE

1. Platelet monoamine oxidase (MAO) activity was investigated in 30 patients with Huntington's disease and compared with the activity in a control group. 2. Significantly elevated activity was found in the patients (P less than 0.05; t-test) when same sex contrasts were carried out to account for the well known influence of sex on MAO activity. 3. The mean MAO activity in male patients was 23.5 +/- 6.0 nmol/mg protein per h and female patients was 29.5 +/- 8.9 nmol/mg protein per h using tyramine as the substrate. 4. The possible influence of environmental factors on the results is discussed.     

千金藤啶碱对大鼠脑内单胺代谢的影响

1-千金藤啶碱(1-SPD 15～120 mg/kg)能增加大鼠纹状体和边缘区的多巴胺代谢物DOPAC和HVA(+150～300%),并有剂量相关关系。此作用于给药后60 min达峰值,给药后4 h虽有恢复趋势,但仍明显高于对照值。SPD还能中等度地降低上述两个脑区的DA和NA(-18～48%)。DA转换率(表现为代谢物增加)的升高支持SPD为DA受体阻断剂。但DA和NA下降表明,除有受体阻断作用外,不能排除药物对单胺递质的贮存、释放或再摄取的影响。纹状体内的5-HIAA含量亦有明显升高。     

千金藤啶碱对大鼠脑内单胺代谢的影响

1-千金藤啶碱(1-SPD 15～120 mg/kg)能增加大鼠纹状体和边缘区的多巴胺代谢物DOPAC和HVA(+150～300%),并有剂量相关关系。此作用于给药后60 min达峰值,给药后4 h虽有恢复趋势,但仍明显高于对照值。SPD还能中等度地降低上述两个脑区的DA和NA(-18～48%)。DA转换率(表现为代谢物增加)的升高支持SPD为DA受体阻断剂。但DA和NA下降表明,除有受体阻断作用外,不能排除药物对单胺递质的贮存、释放或再摄取的影响。纹状体内的5-HIAA含量亦有明显升高。     

吲哚醌对大鼠杏仁核点燃的抑制作用

目的：研究吲哚醌对大鼠杏仁核点燃发作的影响及其抗惊厥作用。方法：建立大鼠杏仁核点燃模型,观察发作的电生理指标和行为学变化;在小鼠最大电休克惊厥、戊四唑惊厥和氨基脲惊厥模型计数惊厥发生率。结果： ip吲哚醌50～200 mg.kg-1均可升高杏仁核点燃大鼠的局灶性后放电阈值,降低发作强度和全身性发作 (stage 5) 百分率;可剂量依赖性地对抗小鼠最大电休克发作,并能取消戊四唑惊厥和氨基脲惊厥的强直相,降低戊四唑惊厥的死亡率。结论：吲哚醌对癫痫发作有抑制作用,其机制与抑制MAO-B活性、升高发作阈值有关。     

SOME CARDIOVASCULAR EFFECTS OF MONOAMINE OXIDASE INHIBITORS IN UNANAESTHETIZED RATS

The effects of four monoamine oxidase (MAO) inhibitors on the blood pressure of conscious normotensive and DOC-salt hypertensive rats were measured. Harmaline (20 mg/kg p.o.), pargyline (100 mg/kg p.o.) and tranylcypromine (10 mg/kg p.o.) all lowered blood pressure significantly in both normotensive and hypertensive rats whereas methylaplysinopsin (10 mg/kg p.o.) had no effect on blood pressure. The effects of these MAO inhibitors on blood pressure responses to serotonin, tyramine and beta-phenylethylamine were determined in conscious normotensive rats. Pargyline and tranylcypromine shifted the dose-response curves for tyramine and beta-phenylethylamine, but not serotonin, to the left, indicating inhibition of type B MAO. Harmaline and methylaplysinopsin shifted the dose-response curves for tyramine and serotonin but not beta-phenylethylamine, to the left, indicating inhibition of type A MAO. Since the four antagonists tested inhibited at least one form of MAO, and yet not all of these MAO inhibitors lowered blood pressure, we suggest that our results are consistent with the view that the hypotensive action of MAO inhibitors is not necessarily related to inhibition of MAO.     

人参茎叶皂甙及其单体对大鼠脑内B型单胺氧化酶活性的影响

本文用体外法研究了人参茎叶皂甙(GSLS)及其单体Rg_1,Rg_2,Re和Rh_1大鼠脑内B型单胺氧化酶(MAO-B)活性的影响。结果表明,GSLS和Rh_1可加强MAO-B的活性。Rg_1和Rg_2可抑制MAO-B的活性,其抑制强度与3.3×10~(-5)mg/ml优降宁相当。抑制特征曲线表明Rg_1和Rg_2对MAO-B的抑制作用均属竞争性抑制。