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     

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.     

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。     

ALTERED HEPATIC METABOLISM OF FATTY ACIDS IN RATS FED A HYPOLIPIDAEMIC DRUG, FENOFIBRATE

The aim of this study was to examine the effects of dietary fenofibrate (0.05% in the diet) on ketone body production and lipid secretion in isolated perfused rat liver. Feeding with fenofibrate for 7–9 days caused an increased liver weight. Ketone body production was significantly greater in the livers perfused with oleic acid than in those perfused without fatty acid, with the elevation of the ratio ofβ-hydroxybutyrate:acetoacetate indicating an increased redox potential in mitochondrial compartments by exogenous fatty acid. On the other hand, fenofibrate feeding caused a further stimulation of ketone body production from both endogenous and exogenous fatty acid substrates, respectively, with a decreased ratio ofβ-hydroxybutyrate:acetoacetate as compared to respective control livers, indicating a decreased redox potential. Hepatic secretion of triglyceride, but not of cholesterol, was decreased markedly in the fenofibrate-fed rats, especially when oleate was provided, suggesting an inverse relationship between rates of ketogenesis and triglyceride secretion. These results suggest that the altered hepatic metabolism of long-chain fatty acids between oxidation and esterification caused by fenofibrate may thus be a factor responsible for the decreased secretion of triglyceride, hence leading to hypotriglyceridaemiain vivo.     

血清LSA测定在恶性肿瘤临床诊断中的初步应用

本文根据Svennerholm和蒋谷人等的方法略加改良,测定了蚌埠地区113例正常人,71例恶性肿瘤患者和82例非肿瘤疾病患者血清脂质结合唾液酸(LSA)的含量。正常值为12.4mg/dl(SD=±3.6mg/dl),71例不同肿瘤患者的平均值为28.2mg/dl(SD=±9.7mg/dl),阳性率为88.7％,82例非肿瘤疾病患者的平均值为16.82mg/dl(SD=±5.4mg/dl),假阳性率为17％。方法的灵敏度,重复性(平均CV=3.6％)和回收率(平均回收率=101.4％)测定结果是满意的。本研究的初步结果表明,血清LSA测定对肺癌、白血病、胃癌和食管癌具有一定的临床诊断价值。     

Spectrum of looping disturbances in stage 34 chicken hearts after retinoic acid treatment

Background: In a recently developed chick model the teratogen retinoic acid has appeared to induce a spectrum of double outlet right ventricle, which needs further detailed evaluation. It is known that retionic acid is able to induce cardiac malformations. Although the exact mechanism is not known, an interaction with neural crest cell function is thought to exist. Methods: After treatment with 1 μg all-trans retinoic acid at Hamburger and Hamilton stage 15 and reincubation until stage 34 of development 41 chicken embryos were evaluated macroscopically and microscopically, supported by graphic reconstructions. These retinoic acid treated embryos were compared with a control group (n = 8). Results: The retinoic acid treated embryos could be divided in three groups. Group 1 (23/41) had an intact septum, group 2 (11/41) had an isolated ventricular septal defect (VSD), and group 3 (7/41) had a double outlet right ventricle (DORV). Besides, in the group with an intact septum 11 hearts showed an abnormal course of the subaortic outflow tract. In the group with DORV a straddling tricuspid orifice (7/8) and a double inlet left ventricle (1/8) could be distinguished. Considering the external contour, the hearts in the DORV group all showed a dextroposed arterial pole. Malformed pharyngeal arch arteries were found in all three groups (11/41) and with a great diversity. Conclusions: The present cardiac malformations in the chicken as a result of retinoic acid treatment are part of a continuous spectrum, varying from hearts with an intact ventricular septum and a normal course of the subaortic outflow tract to a double outlet right ventricle with a straddling tricuspid orifice or even a double inlet left ventricle. A remarkable observation in this spectrum concerns the correlation of malformations of the inflow and outflow tracts, which is explained as a cardiac looping disturbance. The disturbance of the looping process seems to lead to malalignment of septal components, although, in the chick, retinoic acid does not in general interfere with the formation of these septal components themselves. © 1995 Wiley-Liss, Inc.     

用大肠杆菌CM89菌株对三种化学物抗突变作用的研究

本文以 E.coli CM891为靶细胞,用细菌内抗突变作用模式研究了肉桂醛,鞣酸,二烯丙三硫的抗4NQO 突变性及其作用机制。含质粒 pKM101的 CM891的高抗株(抗50μg/ml 氨苄青霉素)能提高该菌株的自发突变率和4NQO 诱发的突变率以及对鞣酸的杀伤抗性。肉桂醛的抗突变性不依赖质粒 pKM101效应,但与暂时性生长延搁有关。鞣酸及二烯丙三硫的抗突变机制可能包括质粒 pKM101介导的易误修复。上述三种化学物中每二种联合应用均显示抗4NQO 突变性的协同效应及对靶细胞的毒性杀伤作用。     

强化婴幼儿奶粉中叶酸的测定

强化叶酸的奶粉在0.05M K_2HPO_4缓冲液中,经均质,调pH4.5,15000g离心20分钟,其清液调pH4.0,进行CGS树脂离子交换层析,用10ml KClK_2HPO_4洗脱,调pH7.0,进行HPLC测定,采用300x3.9mm ODS反相柱,移动相0.05M K_2HPO+MeOH(91+9),流速1ml/分,紫外检测器波长285nm,灵敏度0.0050D。方法相对标准偏差为±3.3％,回收率为87％,最小检测量为0.02μg/ml。