Antiproliferative effects of 4′, 5′-unsaturated adenine nucleosides on leukemia L 1210 cells in vitro

Summary Several 4, 5-unsaturated adenine nucleosides were shown to have antiproliferative activity against L 1210 leukemia cells in vitro. The active nucleosides were cytotoxic to the L 1210 cells as demonstrated by Trypan Blue uptake. The cytotoxicity was not induced by alterations in the ribonucleoside and deoxyribonucleoside triphosphate levels of the L 1210 cells.     

Novel rearrangement of purines

Summary 6-Trichloromethyl-9-methylpurine (1) rearranges to 6-dichloromethyl-9-methyl-8-oxopurine (2) in aqueous mild acidic solution. The rearrangement is rationalized in terms of a reaction involving protonation, covalent hydration, prototropic equilibrium and/or a hydride transfer. An alternative mechanism involving a positive halogen compound and hypochlorous acid as an intermediary is also proposed. Compound1 condenses with 4,5-diaminopyrimidine to give the purine-pyrimidine Schiff base pair4.Acknowledgments. We are deeply indebted to Professor S. Cohen of the Sackler School of Medicine, Tel Aviv University (Ramat Aviv, Isreal) for his advice and encouragement. Support of this research by the Israel Cancer Association, the Ber-Lamsdorf Foundation Switzerland Israel and by the Advancement of Mankind Foundation, is gratefully acknowledged. We thank Proff. D. Arigoni and A. Eschenmoser, ETH Zürich, for their valuable proposals and comments on the mechanism of the rearrangement.     

Mn-V-Nb重轨钢组织与性能的研究

以研制特级耐磨重轨钢为目的,在 U 74普碳耐磨重轨钢化学成分的基础上,加入微量V,Nb 元素并适当提高 C,Mn 元素的含量,设计并冶炼出 Mn-V-Nb 重轨钢。研究了该钢的组织及性能。结果表明:Mn-V-Nb 钢的常规力学性能达到了特级耐磨轨钢的要求。在实验室条件下,抗磨损性能和抗接触疲劳性能分别较 U74 钢提高3.7 倍和 4.6倍。提高的原因在于珠光体片间距的细化及 V,Nb 元素的沉淀强化作用。     

普适费米气体型能级密度公式及其参数

在费米气体模型基础上,考虑了低能修正,建立起了普适费米气体型能级密度公式。使用27.8个核素的平均中子共振间隔D数据及268个核素的能级累计数sN(E)数据,用最小二乘法,在高速计算机上拟合得到了一组普适参数。使用这组参数,D计算值的平均相对误差为36.51％,比实验值平均相对误差(26.69％)高38.6％。能级累计数N(E)的计算结果也有较大改进,其平均相对误差为40.56％,仅比在D计算值的平均相对误差高 14.3％。我们用若干组不同参数分别计算诸核素的D值和N(E)值,相对误差控制在20％以内。然后按核素列出它们的实验值和计算值,连同其相应参数,均在附录中给出,以便查阅。     

Alzheimer's disease: fundamental and therapeutic aspects

Alzheimer's disease is the most common type of progressive and debilitating dementia affecting aged people. In some early — as well as late-onset familial cases, a genetic linkage with chromosomes 14, 21 (early-onset) or 19 (late-onset) has been indicated. Furthermore, a direct or indirect role has been attributed to normal or structurally altered amyloid -protein (concentrated in senile plaques) and/or excessively phosphorylated tau protein (located in neurofibrillary tangles). Degeneration of cholinergic neurons and concomitant impairment of cortical and hippocampal neurotransmission lead to cognitive and memory deficits. Several compounds are being tested in attempts to prevent and/or cure Alzheimer's disease, including tacrine, which has very modest efficacy in a sub-group of patients, and new acetylcholinesterase inhibitors. Pilot experiments have also been launched using nerve growth factor (NGF) to prevent or stabilize the processes of cholinergic pathway degeneration. Alternatively, antioxidants, free radical scavengers and/or non steroidal anti-inflammatory agents may be screened as potential therapies for neurodegenerative diseases induced by multiple endogenous and/or exogenous factors. The recent use of transgenic mice, in parallel with other genetic, biochemical and neurobiological systems, in vivo and/or in vitro (cell cultures), should accelerate the discovery and development of specific drugs for the treatment of Alzheimer's disease.     

17β-Estradiol-sensitivity of cultured myometrial cells

Summary The estrogen sensitivity of cells cultured from the rat myometrium was studied by growing the cells in the absence or presence of 1 nM 17-estradiol. Following a time lag of 10 days, exposure to estrogen resulted in increased incorporation of radiothymidine by the cells. Estrogen treatment also decreased isoproterenol-dependent and GTP-dependent adenylate cyclase activity, but had no effect on basal activity. These cultured cells have been shown previously to have some properties of uterine smooth muscle. The effects estrogen has in viyro, therefore, may reflect important properties in vivo that account for the mechanism by which the sex steroid decreases the sensitivity of the myometrium to isoproterenol.     

不同车头间距下交通流的速度分布

在传统的交通流理论中,通常用确定性函数来描述交通流的速度-密度关系.但实际上,交通流存在着相当大的随机性和波动性:在一定局部密度的情况下,往往存在多种短时局部速度.为了能更加真实地描述速度和间距之间的关系,对NGSIM数据进行了研究和统计,对不同车头间距情况下的交通流速度分布建模.结果表明:当交通流密度较小时,速度分布...     

电渣重熔工艺参数对钢锭凝固质量的影响

应用以前所建立的数学模型,确定了几种渣系重熔冷轧辊用钢的最优工艺,对重熔钢锭的质量进行了分析,研究了工艺制度对重熔钢锭凝固质量的影响.实验表明,通过工艺参数的合理选择,控制重熔过程的局部凝固时间和二次枝晶间距长度,进而控制重熔钢锭的偏析程度的方法是可行的.对于Cr5冷轧辊用钢而言,局部凝固时间越长,对应的二次枝晶间距越长,由于元素偏析所引起的碳化物含量越高.     

采用WD倒谱法分析人体肾组织的超声散射微结构特征

提出了一种对超声散射信号分析的新方法———WD倒谱法 .利用该方法对人体正常肾和肾肿瘤组织的回波信号进行分析 ,与用AR倒谱法所得结果进行了比较 .结果表明 ,两种肾组织散射子的平均间距明显不同 ,WD倒谱比AR倒谱更能反映软组织的微观结构特征 ,说明WD倒谱是软组织超声散射信号分析与软组织散射子平均间距定征的一种有效方法