The discovery of antidepressants: A winding path

Summary Modern treatment of mental depression started with the availability of monoamine oxidase (MAO) inhibitors and tricyclic antidepressants. These drugs also contributed to the early development of psychopharmacology. Attempts to improve the anti-tuberculous action of the hydrazine derivative isoniazid by developing derivatives thereof led to the synthesis of iproniazid. Its introduction as the first modern antidepressant was based on three unexpected actions of the drug: MAO-inhibition, reversal of reserpine-induced sedation, and the presence of psychostimulation as a clinical side effect in man. However, the initial success of iproniazid and other MAO inhibitors, hydrazides and non-hydrazides, was curtailed by the occurrence of undesirable side effects such as potentiation of the blood-pressure elevating action of food amines. The tricyclic antidepressants were a development of the class of antihistamines, one of which, chlorpromazine, showed neuroleptic activity. A congener of this compound, imipramine, was discovered by clinical observation to have unexpected antidepressant effects. The clinical success of this drug (which is still in use) led to the development of a successful series of other tricyclic and non-tricyclic antidepressants. Progress in the elucidation of possible mechanisms of the action of the tricyclic compounds has helped this development. Recent advances in basic research have also induced a revival of MAO-inhibitors since, due to the discovery of MAO-subtypes, inhibitors with higher specificity and fewer undesirable side effects are now available.     

睡莲科植物酯酶同功酶的数量分类研究

采用垂直平板聚丙烯酰胺凝胶盘状电泳技术,对国内睡莲科植物（包括６个属的６个代表种及３个品种）的叶片进行了酯酶同功酶的测定,初步结果表明被测植物均有各自稳定的酯酶酶谱．运用数量分类学方法对被测植物进行聚类,其中白睡莲与其派生的红睡莲和黄睡莲２品种聚为一类,南芡与北芡亦聚为一类,而此２类与萍蓬草、莲、莼菜和王莲的亲缘关系较远,且后４种植物之间亲缘关系亦远．该结果与由过氧化物同功酶酶谱的分析结果基本相似．     

电聚合吡咯膜修饰的葡萄糖氧化酶电极

自制的铂丝电极经铂化处理后,将葡萄糖氧化酶与单体吡咯用循环伏安法共聚合到电极上,铂化后电极表面积的增大增加了固定的酶量,同时也增大了电极对Ｈ２Ｏ２的催化能力,使电极对葡萄糖的响应电流增大到７．５ｍＡ／（ｍｏｌ·Ｌ＾－１）,还测试了聚合液中酶浓度、ｐＨ值和聚合时间等因素对电极特性的影响。     

再生丝心蛋白和羧甲基纤维素复合膜的特性及其在有机相葡萄糖生物传感器中的应用

用再生丝心蛋白和羧甲基纤维素构成的复合膜作为固定葡萄糖氧化酶的基质,并用红外光谱测试了该复合膜的结构,用扫描电子显微镜观察了其形态．用上述复合膜材料固定葡萄糖氧化酶和羧酸二茂铁（或７,７,８,８－四氰代二甲基苯醌,ＴＣＮＱ）制成的葡萄糖生物传感器具有较好的灵敏度与稳定性     

葡萄糖氧化酶及过氧化氢酶的生物合成

研究了黑曲霉细胞的生长及其葡萄糖氧化酶、过氧化氢酶的生物合成．ＣａＣＯ３是２种酶的产酶诱导因子,其产酶模式都是延续合成型,最大比生长速度μｍａｘ、菌体得率Ｙ（Ｘ／Ｓ）、葡萄糖氧化酶及过氧化氢酶合成得率Ｙ（ＧＯＤ／Ｓ）、Ｙ（ＣＡＴ／Ｓ）分别为０．０９７ｈ－１、０．０７５ｇ．ｇ－１、２９．３４μｍｏｌ·ｍｉｎ－１·ｇ－１、３８９．１７μｍｏｌ·ｍｉｎ－１·ｇ－１．也研究了各种物质对葡萄糖氧化酶及过氧化氢酶活力的影响,金属离子对葡萄糖氧化酶有抑制,阴离子对葡萄糖氧化酶和过氧化氢酶有抑制,还原性小分子化合物是葡萄糖氧化酶的激活剂     

Synthesis and Characterization of Porphyrin-Trisbenzimidazole Dinucleating Ligand and Its Heterodinuclear Complex as CcO Active Site Model

A new dinucleating ligand having two metal-binding sites has been designed and synthesized as model ligand for Cytochrome c Oxidase. The corresponding heterodi-nuclear complex, as an active site model of Cytochrome c Oxidase, consisting of a porphyrinatocobalt compound covalently linked with a copper derivative of tris(2-benzimidazylmethyl) amine bearing three benzimidazole ligands for copper was synthesized and spectroscopically characterized. The spectra data suggest that there are interactions between the cobalt and copper coordination units. The cobalt is coordinated to four central nitrogens of the porphyrin and the copper has pentaco-ordinate geometry with the four tertiary amine nitrogens and a chloride.     

烟草中多酚氧化酶的生理生化特征及其活性控制的研究

对烟草叶中的多酚氧化酶(PPO)进行了部分纯化，对比了叶中PPO在苗期和田间的活性差异，研究了其活性变化规律，发现生长旺盛期PPO活性高于其他时期，研究了烟叶在不同水势条件下PPO活性变化规律，发现水势过高、过低，PPO活性均较低，在一872．78kPa水势条件下，PPO活性最高，所以细胞中的含水量是影响PPO活性的因素之一．研究了PPO在35℃、40℃、45℃、50℃、55℃、60℃、65℃、70℃和75℃等烘烤温度条件下的热敏感性，发现：酶的最适反应温度为35℃；温度由35℃升至75℃，活性逐渐下降，在每一温度下保持5min，活性趋于稳定，用回归法得出了烟叶中PPO的下降百分数与温度之间的关系式．用双倒数作图法比较了NaDiCa、EDTA、巯基乙醇和硫脲4种常用抑制剂对烟叶中PPO活性的抑制强度，结果表明：同一浓度下它们对PPO的抑制强度依次递减，而NaDiCa抑制效率明显高于其他3种抑制剂；CuCl2可以促进PPO活性，用回归法得出了活力增加百分数与二价铜离子浓度的关系式。     

西藏黄牛血清淀粉酶（Am）、酯酶（Es）同工酶遗传特性的研究

应用聚丙烯酰胺凝胶电泳法研究了西藏黄牛的Ａｍ和Ｅｓ同工酶，得出了其基因频率和基因型频率．结果表明，西藏黄牛的Ａｍ和Ｅｓ两个同工酶位点的基因分布及其频率与瘤牛种（Ｂｏｓｉｎｄｉｃｕｓ）差异较大，而与普通牛种（Ｂｏｓｔａｕｒｕｓ）较为一致，这进一步从同工酶位点上验证了我们对西藏黄牛的Ｙ染色体特征和血液蛋白多态性的研究结果     

葡萄糖的六种荧光检测法研究

介绍了6种葡萄糖荧光检测法.详细介绍了每种检测方法的荧光强度变化机理和葡萄糖检测原理,并在此基础上对葡萄糖荧光传感器的发展趋势作了展望.     

盲蝽科(半翅目异翅亚目)部分昆虫酯酶同工酶比较研究

运用酯酶同工酶电泳技术获得盲蝽亚科Mirinae、合垫盲蝽亚科Orthotylinae、叶盲蝽亚科Phylinae和齿爪盲蝽亚科Deraeocorinae 4个亚科12个属的23种盲蝽的酯酶同工酶(EST)酶谱．将所获得的酶谱数据(酶带和相对迁移率Rf)转化为二态特征数据，建立矩阵，用系统发育分析软件包WinClada 1．00．04对数据矩阵进行分析运算，分别获得各个亚科内和亚科间的系统发育树．分析结果表明：①酯酶同工酶酶谱特征在不同属级单元之间以及同属的不同种类之间都存在着明显的差异；②不同属种之间酯酶同工酶特征的相似程度与外部形态特征之间的相似程度不一致，以外部形态为主要依据的传统分类的一些属不是真正的单系群；③酯酶同工酶酶谱特征所反映出的盲蝽科4个亚科间的相互关系与Sehuh 1974年所做的盲蝽科内系统发育部分一致，但合垫盲蝽亚科与叶盲蝽亚科之间不是直接的姐妹群关系．4个亚科的关系为(((盲蝽亚科Mirinae，齿爪盲蝽亚科Deraeocorinae)叶盲蝽亚科Phylinae)合垫盲蝽亚科Orthotylinae)；④盲蝽亚科内存在着明显的异质性，需要进一步分类修订．