Synthesis and Antitumour Activity of New Derivatives of Flavone-8-acetic Acid (FAA). Part 2: Ring-Substituted Derivatives

A range of 18 derivatives of flavone-8-acetic acid (FAA) with substituents on the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. There was no clear-cut relationship between in vitro and in vivo activity but the activity in each situation was found to be very sensitive to the precise substitution pattern with closely related isomers giving widely different activities. Some of the compounds, notably 10b,cj , and r , were active in vivo and these require further studies in order to evaluate their potential for development.     

Synthesis and Structure Elucidation of 5-Aminomethinimino-3-methyl-4-isoxazolecarboxylic Acid Phenylamides and Their Immunological Activity

A series of 5-aminomethinimino-3-methyl-4-isoxazolecarboxylic acid phenylamides 4 has been prepared by condensation of 5-amino-3-methyl-4-isoxazolecarboxylic acid phenylamides 1 with trichloroacetic aldehyde. Alcoholysis of trichloro derivatives 2 gave 5-alkoxymethine derivatives 3 which, on reaction with an appropriate amine, formed the corresponding compounds 4 . The compounds obtained were evaluated for their immunological activity. The properties of three compounds, described in this report, permitted inhibition of the immune response in all possible ways: diminishing both types of immune response ( 4d ), humoral immune response ( 4a ), or cellular immune response ( 4c ). Preparation 4d is comparable in its effectiveness to CsA, so it may be potentially used as an agent for prolongation of the function of transplanted organs. Two other compounds may potentially be used in cases where only one type the immune response is required for combating pathogen invasion.     

An XPS and SEM evaluation of six chemical and physical techniques for cleaning of contaminated titanium implants

The purpose of the present study was to analyse clinically failed and retrieved implants prior to and after cleaning by means of scanning electron microscopy (SEM) and X-ray induced photoelectron spectroscopy (XPS) as compared to unused controls. Six different chemical and physical techniques for cleaning of contaminated titanium implants were evaluated: 1) rinsing in absolute ethanol for 10 min, 2) cleaning in ultrasonic baths containing trichloroethylene (TRI) and absolute ethanol, 10 min in each solution, 3) abrasive cleaning for 30 s, 4) cleaning in supersaturated citric acid for 30 s, 5) cleaning with continuous CO2-laser in dry conditions at 5 W for 10 s, 6) cleaning with continuous CO2-laser in wet conditions (saline) at 5 W for 10 s. SEM of failed implants showed the presence of contaminants of varying sizes and XPS showed almost no titanium but high carbon signals. XPS of unused titanium implants showed lower levels of titanium as previously reported, probably due to contamination of carbon which increased with time in room air. Cleaning of used implants in citric acid followed by rinsing with deionized water for 5 min followed by cleaning in ultrasonic baths with TRI and absolute ethanol gave the best results with regard to macroscopical appearance and surface composition. However, as compared to the unused implants the results from an element composition point of view were still unsatisfactory. It is concluded that further development and testing of techniques for cleaning of organically contaminated titanium is needed.     

铜绿假单胞菌全细胞脂肪酸气相色谱分析及应用

本研究用计算机控制，可程序升温的毛细管柱气相色谱（ＧＣ）仪分析４８株铜绿假单胞菌标准株和临床株、部分常见假单胞菌、肠杆菌的细胞脂肪酸。结果表明：月桂烯酸（Ｃ１２：１），月桂酸（Ｃ１２：０）、十三碳烯酸（Ｃ１３：１）、十三碳酸（Ｃ１３：０）、肉豆劳动脑酸（Ｃ１４：１）、十七碳稀酸（Ｃ１７：１）、十七碳酸（Ｃ１７：０）、硬脂酸（Ｃ１８：０）和花生四烯酸（Ｃ２０：４）是铜绿包菌有鉴别意义的脂肪酸，组成与     

中和法制备水杨酸微晶

为增加水杨酸在各类制剂中的分散度，便于制备，提高疗效，采用酸碱中和法将其制成微晶。先将水杨酸与１ｍｏｌ／Ｌ氢氧化钠反应成盐溶解，然后用１ｍｏｌ／Ｌ盐酸中和析出微晶。所得微晶呈针状，色白，膨松，在电镜下测得平均粒径为１６μｍ。各项理化标准符合中国药典１９９５年版规定。本法微晶得率为９８％。     

原发性小肠恶性肿瘤的CT诊断

本文回顾性分析３４例经病理证实的原发性小肠恶性肿瘤的ＣＴ表现。病变包括腺癌１６例，平滑肌肉瘤１２例，淋巴瘤６例。ＣＴ扫描能明确肿瘤向腔内和腔外侵犯的程度，清晰显示肿瘤与邻近结构的关系，有无局部及远处转移等，为临床治疗提供帮助。鉴别诊断应包括小肠良性肿瘤、炎性病变和转移性肿瘤等。     

10Gyγ线照射后小鼠两相邻肠段运动变化

本文用同时记录两相邻空肠段的收缩活动来观察经10Gyγ线照射后小肠运动的变化,以了解照射后是否出现逆蠕动,以便进一步分析肠套叠形成的原因.结果表明,照射后两相邻肠段出现强度不一的收缩活动,并且可以产生逆蠕动;但是这种逆蠕动发生的机率是不大的.本实验未观察到逆蠕动发生的规律性.因此,逆蠕动的产生可能是照射后发生肠套叠的部分原因.     

Serotonin and norepinephrine in the spinal cord of man

The content of serotonin (5-HT), 5-hydroxyindoleacetic acid (5-HIAA) and norepinephrine (NE) was analysed in 71 human spinal cords obtained post-mortem. The highest content of 5-HT, 5-HIAA and NE was found in the lumbar enlargement of the spinal cord. 5-HT and 5-HIAA content increased from fetal to adult spinal cord whereas the content of NE decreased. Characteristic segmental distribution of measured monoamines was present in adult spinal cord only. In two patients spinal cord lesion led to the reduction in spinal cord content of 5-HT, 5-HIAA and NE and loss of characteristic segmental distribution of these substances. These results are in general agreement with observations on spinal cord of different animal species.     

芳香PET树脂母粒的研制

通过丙烯酸和丙烯酸正丁酯溶液共聚合，得到丙烯酸－丙烯酸正丁酯共聚物，该树脂与环氧氯丙烷反应后再与PET树脂切片继续反应，可使PET树脂切片表面形成聚丙烯酸酯自膨润型吸油网络结构，将表面具有聚丙烯酸酯自身膨润型吸油网络结构的PET树脂切片（简称为留香剂）在油溶性香精中浸泡，香精就被吸附在留香剂表面，即得到芳香PET树脂母粒。用SEM观察了母粒的表面结构形态。     

花生四烯酸和二十二碳六烯酸对海马神经细胞生长发育的影响

【目的】观察不同浓度花生四烯酸 (AA)和 (或 )二十二碳六烯酸 (DHA)对体外培养海马神经细胞生长发育的影响。【方法】无血清培养液中分别加入不同剂量的AA和 (或 )DHA ,采用噻唑蓝比色试验 (MTT法 )反映各组海马神经细胞存活状况 ,神经元特异性烯醇化酶 (NSE)染色鉴定神经细胞 ,图像分析技术测量神经细胞的胞体大小和突起长度。【结果】培养液中分别添加AA为 4～ 8μmol/L、DHA为 2～ 8μmol/L时 ,神经细胞活力高于对照组 ;当培养液中AA和DHA总浓度为 4μmol/L、比例为 2∶1或 4∶1时 ,神经细胞的活力、胞体面积、最大长径、最大短径和平均突起长度均显著高于单一添加 4μmol/LAA、4μmol/LDHA和对照组。【结论】AA、DHA均具有促进体外培养海马神经细胞生长发育的作用 ;与单独添加AA、DHA相比 ,AA和DHA共同作用的促海马神经细胞生长发育作用更好。