药物的定量构效关系的方法学研究——改进的逐步回归算法

在定量的构效关系研究中,多重回归分析选人的参数,多是用穷举所有方程实现的。本文提出一种改进的逐步回归算法,计算实例表明,是个行之有效的方法。     

Synthesis and cytotoxic activity of new alkyl[3-(2-chloroethyl)ureido]benzene derivatives

Several alkyl[3-(2-chloroethyl)ureido] (CEU) benzene derivatives were prepared as potential anticancer agents. These new compounds were readily prepared in good yields by addition of anilines to 2-chloroethylisocyanate. Their cytotoxic activity was evaluated on human breast cancer (MDA-MB-231), human colon adenocarcinoma (LoVo) and mouse lymphocytic leukemia (P388D₁) tumor cell lines. Several new CEUs were significantly more cytotoxic than the nitrogen mustard chlorambucil. The biological activity of these aromatic urea derivatives seems to be related to the nature and position of the alkyl substituents on the aromatic ring. Substitution by branched alkyl groups on position 4 of the aromatic ring led to cytotoxic molecules which are up to 5 times more potent than the standard chlorambucil.     

双氢杨梅树皮素对兔胸主动脉条平滑肌收缩反应的影响

用兔胸主动脉条研究双氢杨梅树皮素对去甲肾上腺素（NE）、KCl和CaCl2所致兔胸主动脉条收缩反应量效曲线的影响。双氢杨梅树皮素能显著地抑制NP、KCl和CaCl2所致兔胸主动脉杂的收缩，量效曲线右移，最大反应降低，对高K 所致兔胸主动脉条收缩的抑制作用明显大于NE所致兔胸主动脉条收缩的抑制作用。双氢杨梅树皮素对NE引起的依赖内Ca2 释放的收缩有明显抑制作用，而对NE依赖细胞外Ca2 性收缩区在较高浓度时才显示抑制作用，提示双氢杨梅树皮素可能对电压依赖性钙通道（PDC）有选择性阻滞作用。     

建立新型医患关系是医院工作的当务之急

《医疗事故处理条例》《最高人民法院关于民事诉讼证据的若干规定》这两个法规的出台，给医院提出了新的课题，结合目前实际，提出了医院全面贯彻执行这两个法规，必须从围绕改善医患关系这个中心问题入手。建立新型和医患关系，并根据多年的观察与实践，着重论述了如下见解：医务人员在为患者的攻关服务过程中，要真正认识自己是医患矛盾中的主要方面；医务人员要转变传统的服务思维定势，尊重和理解患者，医务人员要确立既为患者生命和利益负责，又重视患者权利的观念，医务人员要增强法制观念，做到依法行医，医院要设置监控部门或配备专兼职人员，对全院的医疗服务进行检查监督。     

两种剂量奥曲肽治疗食管及胃曲张静脉出血效果比较

①目的　比较两种剂量奥曲肽治疗食管、胃曲张静脉出血的临床效果。②方法　将 88例食管、胃曲张静脉出血病人随机分为奥曲肽 5 0 μg/h和 2 5 μg/h剂量组 ,观察平均止血时间、止血率、再出血率和不良反应。 ③结果　 5 0 μg/h组平均止血时间明显短于 2 5 μg/h组 (t=2 .2 4 ,P <0 .0 5 ) ,总止血率明显高于 2 5 μg/h组 (χ2 =5 .36 0 ,P <0 .0 5 ) ,再出血率较 2 5 μg/h组低 (χ2 =7.990 ,P <0 .0 5 )。两组均有 1例病人出现恶心。④结论　奥曲肽 5 0 μg/h剂量治疗食管、胃曲张静脉出血的效果优于 2 5 μg/h剂量     

Influence of the mother-child relationship on the development of the Type A Behavior Pattern

Investigation of the Type A Behavior Pattern (TABP) of pre-school children was conducted to determine the influence of the mother-child relationship on the development of TABP. The incidence of TABP was 44.2% (51.7% in boys and 38.7% in girls). The TABP tendency of the boys decreased as the manifest dissension or conflict in the family grew, in marked contrast with the tendency seen in girls, suggesting that conflict in the family can either weaken or reinforce TABP.     

In vitro determination of lung airway compliance in small animals

An in vitro method for obtaining pressure/volume curves from the lungs of small animals is described. The excised lungs were inflated and deflated with saline or air by a motor-driven syringe controlled by a microcomputer. The computer was programmed to display the curves in real time, correcting when necessary for the compressibility of air in the system. Volume compliance (K=dV/dP×1/V) was calculated by differentiating a polynomial fitted to the measured pressure/volume points. Repeatable curves were obtained from mice aged 24h (body weight 1·3±0·14g (SD), residual lung volume 8·43±1·5 μl (SD). A nonlinear decrease in differential compliance (K=dV/dP×1/V) with increasing strain was observed while the ratio K_saline/K_air increased from 2·5 to 10 over the range of strains investigated (ε=1–5). The relative surface tension (calculated from the difference between the pressures required to inflate the air and saline-filled organs to a given volume) increased exponentially with increasing volume. We conclude that it is now possible to obtain reproducible pressure/volume curves for lungs with a residual volume of less than 10 μl, from animals weighing approximately 1·5 g and, from these curves, estimate airway compliance and surface tension.     

Aromatic ethers of 1-aryl 2-(1H-azolyl)ethanol: study of antifungal activity

Aromatic ethers related to antifungal azole miconazole were synthesized and tested against various strains of Candida. We found that activity is related to the nature of the aromatic ring and the position of substituents on this ring. Activity is more strongly dependent on the substituent in the 2 position of the ethyl chain than on the aromatic group linked through the oxygen. Triazoles were always less potent than the corresponding imidazole analogues.     

流行性出血热病毒感染黑线姬鼠有效剂量的观察

用Hantaan病毒(76-118株)悬液以不同感染剂量采用灌胃和浸泡毒米任实验鼠自行取食两种方法,对捕自非疫区的黑线姬鼠进行实验感染。结果表明:实验鼠未能通过完整的消化道粘膜感染,但可通过破损的消化道粘膜感染,感染剂量与感染率呈正相关,最低感染剂量为10ID_(so)/ml。     

开展电话回访搭建医患沟通桥梁

通过对3 500余人次的有效电话回访,实施健康教育、健康指导3000余人次,受理健康咨询500余人次,协调和化解各类医疗纠纷20余起。电话回访搭起了和谐医患关系的桥梁。