Antiproliferative Action of Benzodiazepines in Cultured Brain Cells Is Not Mediated Through the Peripheral-Type Benzodiazepine Acceptor

The benzodiazepines, Ro 5-4864, diazepam, clonazepam, and also PK-11195, inhibited, at micromolar concentrations, the proliferation of rat C6 glioma and mouse neuro-2A neuroblastoma cells in culture. The cells possessed high levels of "peripheral-type" high-affinity benzodiazepine binding sites as judged by binding assays and displacement potencies. However, the different potencies and specificities of compounds for the antiproliferative actions and binding affinities for the binding site suggest that the antiproliferative actions were not mediated through the peripheral-type binding site. In support of this, these compounds have also been shown to inhibit proliferation of some nonneuronal cultured cell lines, e.g., mouse SP2/O-Ag 14 hybridoma and rat NCTC epithelial cells, which have no detectable high-affinity peripheral-type benzodiazepine binding sites.     

Accumulation of Arachidonic Acid Cyclo- and Lipoxygenase Products in Rat Brain During Ischemia and Reperfusion: Effects of Treatment with GM1-Lactone

The aim of our study was to investigate the changes of various biochemical parameters (concentrations of lactate, free arachidonate, cyclo- and lipoxygenase products) in rat brain after ischemia and reperfusion and the effects of pretreatment with the ganglioside derivative GM1-lactone on the same parameters. Ischemia was induced by reversible occlusion of common carotid arteries for 20 min, which included a final 5 min of respiration of 5% oxygen in nitrogen. Reperfusion was obtained by removing the occlusion. Pre-ischemic conditions were obtained on sham-operated animals. Animals were killed by microwave irradiation of their heads. Brain levels of lactate and of free arachidonate were markedly increased after ischemia and returned to normal values at 5 min of reperfusion. Levels of the cyclooxygenase metabolites prostaglandin F2 alpha, 6-keto-prostaglandin F1 alpha, and thromboxane B2 were increased after ischemia, whereas levels of the lipoxygenase metabolite leukotriene C4 (LTC4) did not change. After reperfusion, a very marked increase of the cyclooxygenase products occurred but not of LTC4. Treatment with GM1-lactone prevented the elevation of cyclo- and lipoxygenase metabolites especially during reperfusion, with limited effects on lactate and free arachidonate levels.     

大熊猫与金黄地鼠体外异种受精的研究

在大熊猫精子与地鼠卵的体外异种受精中,发现大熊猫精子穿入地鼠卵后可以激活受精卵产生极区,释放第二极体,受精卵内雌性原核形成。与此同时,地鼠卵的胞质也能促使大熊猫精子头发育成雄性原核,异种精卵间的相互作用与同种受精的相似。 细胞松弛素B能阻抑大熊猫雄性原核从地鼠卵皮层迁移到卵的中央,实验表明大熊猫雄性原核的迁移也受异种卵的微丝的控制。     

亚洲高海拔锄足蟾属间分类研究(Amphibia:Pelobatidae)

本文比较研究了高海拔锄足蟾类29种成体和蝌蚪的外形,25种的骨骼,8种的核型和带型,9种的眼晶体薄层凝胶等电聚焦电泳图谱等性状,并结合地理分布、生态环境及习性等因素综合而较全面地对中国锄足蟾科Pelobatidae的齿突蟾属Scutiger,猫眼蟾属Aelurophryne和齿蟾属Oreo-lalax三个类群的属间分类问题进行了探讨。研究表明:齿蟾属Oreolalax应为有效属,不宜作为齿突蟾属Scutiger的亚属;猫眼蟾属Aelurophryne与齿突蟾属Scutiger应同归一属,前者应为后者之亚属。     

轴浆转运在神经再生中的作用

夹伤坐骨神经阻断标记蛋白在轴浆中的快、慢转运。3天后转运再现。第14天的转运距离与对照相似,说明再生神经的转运动能基本恢复。用快、慢转运测出的14天平均再生速度分别为1.77±0.14与1.96±0.07mm/d,比对照神经的正常生长速度快6.3—7倍,提示再生需要更多的转运物质。进一步发现再生神经中某些标记蛋白(慢转运波W1)的转运速度为10.25±0.66mm/d,约比对照快1倍,因此这些标记蛋白可能包含适应再生需要而加速转运的结构和功能物质。     

猪尾猴疟原虫（P.inui）广西株配子体感染性变化规律的实验研究

用P.inui广西株经蚊传和血传接种4只猴子,让大劣按蚊每6小时吸血感染1次,连续数周,以蚊胃感染情况判断配子体的感染性。结果发现:本虫株配子体发育成熟的需72n+K小时;配子体生理寿命约12小时;配子体的感染性具有每隔2天,在后半夜出现高峰的周期性变化;血中大环状体百分比高峰与蚊媒感染高峰一致。     

Supra-additive stimulation of adenylate cyclase activity by prostaglandin E2 andD-Ala2-met-enkephalinamide in the guinea-pig superior cervical ganglion: Role of Mg2+ ions

Agonists modulation of Mg²⁺-dependent adenylate cyclase activity has been studied in guinea-pig superior cervical ganglion crude membrane preparations. In the absence of receptors ligands, Mg²⁺ stimulates the enzyme in a concentration-dependent manner. The dose-activation curve shows heterogeneity and two components with higher and lower apparent affinity states, are extrapolated. In the presence ofD-Ala²-met-enkephalinamide only one component is present and the apparent affinity of the ganglionic adenylate cyclase system for the divalent cation as well as Vmax are inhibited. On the contrary, prostaglandin E₂ increases affinity and Vmax values of the lower and, to a lesser extent, of the higher Km component. When the two drugs are tested in combination, not only the inhibitory effect of the opiate is overcome, but a large increase of the apparent affinities and Vmax values for both components is obtained, suggesting the involvement of the Mg²⁺-regulated subunits of the adenylate cyclase system in the supra-additive stimulation mechanism of the enzyme.     

Selection of a pure cerebellar granule cell culture by kainate treatment

Chronic exposure of dissociated cerebellar cultures to 50M kainate results in a complete loss of [³H]-GABA release which is a marker of GABAergic interneurons. No loss of granule cells was found and the glutamatergic nature of the granule cells appeared unaltered by the kainate treatment, since evoked release of [³H]-d-aspartate was maintained after kainate exposure. Glial cells in such cultures are virtually eliminated by treatment with an antimitotic such as cytarabin. In consequence a pure culture of cerebellar granule cells virtually free of stellate, basket and glial cells may be obtained by a combined chronic treatment of the cultures with kainate and cytarabin.     

β-Dl-Methylene-aspartate,an inhibitor of aspartate aminotransferase,potently inhibitsl-glutamate uptake into astrocytes

[³H]Glutamate uptake into astrocytes in primary culture was potently inhibited by the aspartate analoguesl- andd-aspartic acid,Dl-threo--hydroxy-aspartic acid,l-aspartic acid--hydroxymate (IC50's: 136, 259, 168, and 560 M, respectively) and by -Dl-methylene-aspartate, a suicide inhibitor of asparate aminotransferase (IC50: 524 M), and by the endogenous sulphur-containing amino acidl-cysteinesulfinic acid (IC50: 114 M). [³H]Glutamate uptake was not significantly affected by either N-methyl-d-aspartate orDl-homocysteine thiolactone. These results demonstrate that other excitatory amino acids including aspartate andl-cysteinesulfinic acid (but excludingl-homocysteic acid) interact with the glutamate transport system of astrocytes. Inhibition of glutamate uptake may significantly increase the level of neuronal excitability.     

Chromosomal evolution withinPiperaceae

Chromosome numbers for 26 different species of the generaPiper, Peperomia andPothomorphe (Piperaceae) are reported. The basic chromosome numbers are 2n = 26, x = 13 (Piper, Pothomorphe) and 2n = 22, x = 11 (Peperomia), polyploid series are characteristic forPiper andPeperomia. Piper has the smallest chromosomes and prochromosomal interphase nuclei,Peperomia the largest ones and mostly reticulate to euchromatic nuclei.Pothomorphe is intermediate in both characters. The karyomorphological differences betweenPothomorphe andPiper underline their generic separation. Interspecific size variation of chromosomes occurs inPiper andPeperomia. Infraspecific polyploidy was observed inPiper betle. C-banding reveals different patterns of heterochromatin (hc) distribution between the genera investigated. The genome evolution is discussed.