一种适用于推算气态乙烷系氟里昂粘度的基团贡献法

根据关系式与大量的实验数据分析，提出了一种新的适用于常压下气态乙烷系氟里昂粘度推算的基团贡献法，用有可靠实验数据的７种乙烷系氟里昂对新方法进行检验，优于已有的Ｒｄｃｂｅｎｂｅｒｇ法和法．一般偏差在±５％以内，可以满足ＣＦＣｓ替代物合成和应用研究以及一般工程计算的需要．用新方法对低压下ＨＣＦＣ－１３３ａ气态的粘度进行了计算，所得结果可供ＨＦＣ－１３４ａ合成工艺及装置设计和其它工程计算应用．     

Ultra-remote stereocontrol by conformational communication of information along a carbon chain

Many receptors and allosteric proteins function through binding of a molecule to induce a conformational change, which then influences a remote active site. In synthetic systems, comparable intramolecular information transfer can be effected by using the shape of one part of a molecule to control the stereoselectivity of reactions occurring some distance away. However, the need for direct communication with the reaction site usually limits such remote stereocontrol to distances of not more than about five bond lengths. Cyclic structures overcome this problem by allowing the controlling centre and the reaction site to approach each other, but the information transfer spans only short absolute distances. Truly remote stereocontrol can, however, be achieved with rigid compounds containing amide groups: the conformation of the amides can be controlled by stereogenic centres and responds to that of neighbouring amide groups and in turn influences stereoselective reactions. This strategy has allowed remote stereocontrol spanning 8 (ref. 11) or 9 (ref. 12) bonds. Here we demonstrate stereocontrol over a reaction taking place more than 20 bond lengths from the controlling centre, corresponding to a linear distance of over 2.5 nm. This transmission of information, achieved by conformational changes relayed through the molecule, provides a chemical model of allostery and might serve as a molecular mechanism for communicating and processing information.     

On the synthesis of poliovirus RNA at supraoptimal temperatures

Riassunto La scarsa incorporazione di precursori dello ARN in cellule infette da poliovirus ed incubate a 41,5°C è dovuta ad una inibizione della sintesi dello ARN virale più che non ad una sua digestione ad opera di nucleasi.

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Work supported by a Grant of Consiglio Nazionale delle Ricerche, Rome.     

MDR1, cholesterol certification and cell growth: a comparative study in normal and multidrug-resistant KB cell lines

The product of the MDR1 gene (P-gp) has been implicated in the transport of cholesterol from plasma membrane to endoplasmic reticulum for esterification. In previous studies on leukemia cell lines, we suggested that cholesterol esterification may regulate the rate of cell growth and that the MDR1 gene might be involved in this process by modulating intracellular cholesterol esters levels. To further investigate this matter, the rate of cell growth, cholesterol metabolism, expression of the MDR1 gene, and P-gp activity were compared in KB cell lines displaying differences in expression and function of P-gp (drug-sensitive phenotype versus MDR phenotype). The rate of cell growth correlated with cholesterol esterification in all KB cell lines, whereas the over-expression of MDR1 observed in the MDR cell lines was not always associated with an increased capacity of cells to esterify cholesterol. Two known inhibitors of P-gp activity, progesterone and verapamil, strongly inhibited both cholesterol esterification and cell proliferation in all KB cell lines, but they affected intracellular accumulation of labeled vinblastine only in MDR cell lines. These results further support a role for cholesterol esters in the regulation of cell growth and suggest that the P-gp expressed in MDR KB cells is not involved in the general process leading to cholesterol esterification. Received 14 February 2000; received after revision 10 April 2000; accepted 8 May 2000     

Bidirectional control of airway responsiveness by endogenous cannabinoids

Smoking marijuana or administration of its main active constituent, delta9-tetrahydrocannabinol (delta9-THC), may exert potent dilating effects on human airways. But the physiological significance of this observation and its potential therapeutic value are obscured by the fact that some asthmatic patients respond to these compounds with a paradoxical bronchospasm. The mechanisms underlying these contrasting responses remain unresolved. Here we show that the endogenous cannabinoid anandamide exerts dual effects on bronchial responsiveness in rodents: it strongly inhibits bronchospasm and cough evoked by the chemical irritant, capsaicin, but causes bronchospasm when the constricting tone exerted by the vagus nerve is removed. Both effects are mediated through peripheral CB1 cannabinoid receptors found on axon terminals of airway nerves. Biochemical analyses indicate that anandamide is synthesized in lung tissue on calcium-ion stimulation, suggesting that locally generated anandamide participates in the intrinsic control of airway responsiveness. In support of this conclusion, the CB1 antagonist SR141716A enhances capsaicin-evoked bronchospasm and cough. Our results may account for the contrasting bronchial actions of cannabis-like drugs in humans, and provide a framework for the development of more selective cannabinoid-based agents for the treatment of respiratory pathologies.     

Direct evidence that reverse cholesterol transport is mediated by high-density lipoprotein in rabbit

Mammalian cells obtain cholesterol for membrane synthesis mostly via the receptor-mediated endocytosis of low-density lipoprotein (LDL). Macrophages and vascular endothelium additionally have receptors that recognize certain modified forms of LDL (for example, acetyl-LDL). The process by which cholesterol returns from peripheral cells to hepatocytes (reverse cholesterol transport) has not been established; although tissue culture studies have favoured high-density lipoprotein (HDL) as the principal vehicle, the in vivo evidence for this is meagre. When cholesterol-loaded macrophages are incubated in medium containing plasma, cholesterol moves from the cells to HDL and is then esterified by lecithin/cholesterol acyltransferase. The accumulation of cholesteryl esters in the particles increases their size and decreases their density; enrichment with apoprotein E (apo E) also occurs, producing a decrease in electrophoretic mobility. We now report that similar changes occur in the circulating HDL of rabbits, when their peripheral tissues are loaded with cholesterol by intravenous (i.v.) injection of acetylated or native human LDL. This result suggests that HDL is involved in reverse cholesterol transport in vivo.     

多柱体波浪荷载数值分析的边界元法

本文用边界元法计算线性势波对大尺寸多柱体的绕射问题，选用了满足自由表面 及无穷远边界条件的基本解，使问题变量大大减少。文中给出单柱、双柱、四柱的数 值结果，并分析多柱体排列间距对柱体波浪荷载的影响．本文方法适用于任意形状等 截面多柱体波浪荷载的数值分析。     

珍稀濒危药材蛇足石杉的研究概况及开发前景

蛇足石杉中有较高含量的石杉碱甲,对治疗老年痴呆症和提高记忆力有显著疗效,备受国内外学者们的关注.系统总结了近年来国内外学者对蛇足石杉的相关研究成果,旨在为蛇足石杉资源保护与可持续利用、开展蛇足石杉繁殖技术的研究,为解决蛇足石杉原料生产的瓶颈提供理论依据.