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.     

Inhibition of the growth of cariogenic bacteria in vitro by plant falvanones

Phytoalexins, defensive compounds produced by plants against microbial infections, were purified fromSophora exigua (Leguminosae) and their growth inhibitory effects on oral cariogenic bacteria were determined in vitro. Among three isolated compounds, 5,7,2,4-tetrahydroxy-8-lavandulylflavanone completely inhibited the growth of oral bacteria including primary cariogenic mutans streptococci, other oral streptococci, actinomycetes, and lactobacilli, at concentrations of 1.56 to 6.25 g/ml.     

Carbohydrate interference of complement-dependent cell lysis

Summary The antibody-mediated cytotoxicity of three autoreactive sera, an allogeneic hyperimmune serum and a xenogeneic hyperimmune serum was abrogated by the presence of either glucosamine, galactosamine, lactulose or lactose. This inhibition could be overcome in a dose-dependent fashion by increasing the amount of complement in the cytotoxicity assay, but not by increasing the amount of antibody. Furthermore, the inhibition was specific for these sugars in that isomers and N-acetylated derivatives were not inhibitory. The results suggest that these sugars directly blocked events of the complement cascade.     

A new indolic antiauxin, α-(5,7-dichloroindole-3-)isobutyric acid: its chemical synthesis and biological activity

Summary A new potent antiauxin, -(5,7-dichloroindole-3-)isobutyric acid has been synthesized and shown to inhibit auxin-mediated elongation ofAvena coleoptiles and to stimulate root growth of rice seedlings. Its activity is stronger than -(p-chlorophenoxy)isobutyric acid and is comparable to that of 2,3,5-triiodobenzoic acid, which are typical antiauxins.     

复合型酸化缓蚀剂的性能研究

以喹啉为母体,配以有机胺和芳香族化合物,与卤代烃反应合成了一种复合缓蚀剂。采用静态失重法和电化学法评价了缓蚀剂的缓蚀性能,分析了缓蚀机理,并与目前国内常用的酸化缓蚀剂缓蚀效果进行了对比。结果表明,复合缓蚀剂为阳极抑制为主的混合型缓蚀剂,能够有效抑制盐酸对N80碳钢的腐蚀,比目前使用的缓蚀剂性能更优。     

新型仿生亲和介质纯化工艺生产效率分析

抗体的捕获层析的成本在整个抗体纯化工艺中占有相当的比例.分析比较了新型小分子仿生亲和介质和常规蛋白A的动态载量、循环使用次数和线性流速等参数,并计算了相应的生产效率,发现新型小分子仿生亲和介质最高生产效率能达到蛋白A亲和层析介质最高生产效率的3⁶.9倍.     

基于聚邻苯二胺和纳米金电位型免疫传感器的研究

利用电聚合和电沉积技术将邻苯二胺和纳米金固定在石墨电极上,通过白组装的方法使抗体（羊抗小鼠IgG）与石墨电极表面上的纳米金结合,制备了一种免疫传感器（Ab／GNPs／POPD／GE）,并对实验条件进行了优化。该传感器能够对抗原（小鼠IgG）进行定量检测,具有灵敏度高、响应速度快、检测范围宽等优良性能。其检测范围为4．0×10^-～1．0×10^-3ng／mL,检测下限为1．0×10^-3ng／mL．而且该免疫传感器具有较高的选择性和较好的稳定性,寿命可达15d左右。     

小茴香等7种植物蒸馏提取物的抑霉菌效果

以存在于水果的常见霉菌中的灰霉、黑根霉、交链孢、青霉和黑曲霉为研究对象,采用滤纸片扩散法和时倍稀释法,对小茴香、柠檬草、孜然、广藿香、肉桂叶、桉树叶和鼠尾草这7种植物的蒸馏提取物有效抑菌成分(精油)进行抑菌筛选研究.结果表明:小茴香抑菌效果最好且得率高,为1.90%,对青霉、黑根霉最低抑菌浓度(MIC)均为3.2μL/...     

野木瓜注射液对爪蟾坐骨神经传导的影响

野木瓜注射液（Ｉｎｊｅｃｔｉｏｎｓｔａｕｎｔｏｎｉａｅ,ＩＳ）涂布于脊爪蟾（ＸｅｎｏｐｕｓＬａｅｖｉｓ）坐骨神经４ｍｍ长的一段上．电刺激跗部皮肤,记录半膜肌肌电．１０％ＩＳ使肌电的潜伏期和问期分别延长（１．５１±１．１５）ｍｓ和（２６．６±１６．１）ｍｓ（Ｐ＜０．０１,ｎ＝９）;５０％ＩＳ则使潜伏期延长（２．８４±２．１８）ｍｓ和幅度下降到原来的０．２１±０．２６（Ｐ＜０．０１,ｎ＝７）．ＩＳ对神经传导的阻滞作用是量效关系,给药８ｍｉｎ后电刺激坐骨神经干能使已受５０％ＩＳ影响而刺激跗部皮肤几乎不再引起肌电的半膜肌产生同对照一样的肌电．这表明在给药期内５０％ＩＳ主要阻滞传入纤维的传导,而不影响传出纤维的功能．     

功能化氧化石墨烯的靶向肿瘤成像与光热治疗

整合素α_vβ₃是一种跨膜糖蛋白, 高表达于多种肿瘤细胞表面, 如人恶性胶质瘤(U87-MG). 它能够作为一类肿瘤标志物, 为肿瘤类型的诊断提供依据, 并为肿瘤治疗提供潜在作用靶点. 本文以人恶性胶质瘤细胞(U87-MG)为治疗模型, 利用靶向配体——整合素α_vβ₃单克隆抗体(integrin α_vβ₃ monoclonal antibody), 偶联新型纳米材料——氧化石墨烯(nano-graphene oxide, NGO), 构建成一种新型纳米探针(NGO-mAb-FITC)用于靶向成像及光热治疗. 这种纳米探针具有主动靶向功能, 可识别α_vβ₃阳性表达细胞U87-MG, 但不被α_vβ₃阴性表达的人乳腺癌细胞(MCF-7)摄取. 通过异硫氰酸荧光素(FITC)共价修饰靶向配体, 使纳米探针(NGO-mAb-FITC)获得对肿瘤细胞的靶向成像作用. 同时, 利用氧化石墨烯在808 nm近红外激光照射下的光热转化性能, 使得特异性摄取NGO-mAb-FITC纳米探针的肿瘤细胞内部产生过高热(hyperthermia), 从而诱导肿瘤细胞热损伤及细胞凋亡. 实验结果表明, NGO-mAb-FITC能有效识别靶细胞, 为肿瘤诊断提供依据, 而利用氧化石墨烯的高光热转换性能, 为肿瘤治疗提供新途径, 并有望成为一种有潜力的新型靶向光热转换探针而用于肿瘤的成像诊断与光热治疗.