吲哚－2－羧酸脱羧基的改良方法

吲哚－２－羧酸脱羧基的改良方法ＪｏｎｅｓＧＢ等［ＪＯｒｇＣｈｅｍ，１９９３；５８（２０）：５５５８］取代吲哚－２－羧酸［Ｒ＝Ｈ，４（５或６）－ＭｅＯ，５（或６）－Ｆ］与重蒸喹啉放入一厚壁、锥底的硼硅玻璃管中，真空密封后于微波中加热１２ｍｉｎ（２４５０...     

以L-半胱氨酸和吲哚酶法合成L-色氨酸

用色氨酸酶基因工程菌ＷＷ－４催化Ｌ－半胱氨酸和吲哚合成Ｌ－色氨酸。８０ｍｌ反应液（Ｌ－半胱氨酸０．７５ｇ，吲哚０．７５ｇ）３７℃反应４８ｈ，可积累Ｌ－色氨酸１．１８ｇ。Ｌ－半胱氨酸转化率为９３．２％，吲哚转化率为９０．１％。产品总回收率达７０％，所得晶体在熔点、旋光性和红外吸收光谱等方面与标准品完全一致。     

5－氯－2－羟基吲哚的合成

５－氯－２－羟基吲哚的合成冯友建，王玉芝（徐州师范学院化学系，江苏２２１００９，徐州东方化工厂，江苏２２１００７）ＳＹＮＴＨＥＳＩＳＯＦ５－ＣＨＬＯＲＯ－２－ＨＹＤＲＯＸＹＩＮＤＯＬＥ￥ＦＥＮＧＹｏｕ－Ｊｉａｎ；ＷＡＮＧＹｕ－Ｚｈｉａ（Ｄｅｐｔ．Ｃｈ...     

含杂环的β－锗代α－氨基酸倍半化合物的合成及抗肿瘤活性测定

含杂环的β－锗代α－氨基酸倍半化合物的合成及抗肿瘤活性测定姜凤超，刘敏，赵智（武汉同济医科大学药学院，武汉４３００３０）某些含有吲哚３－取代及呋喃２－取代基的衍生物具有抑制谷胱甘肽－Ｓ－转移酶（ＧＳＴｓ）的活性，从而可逆转肿瘤耐药性而使某些具有细胞毒...     

以L-半胱氨酸和吲哚为底物酶法合成L-色氨酸(英文)

以Ｌ－半胱氨酸和吲哚为底物,利用色氨酸酶基因工程菌ＷＷ－１１酶法合成Ｌ－色氨酸。方法：以ＩＰＴＧ诱导基因工程菌色氨酸酶表达,将酶活最高时的工程菌游离细胞作为转化反应的酶源,通过纸层析和氨基酸自动分析仪分析并测定转化液中Ｌ－色氨酸的含量。结果：８０ｍＬ反应液（Ｌ－半胱氨酸０.７５ｇ,吲哚０.７５ｇ）３７℃反应４８ｈ,可积累Ｌ－色氨酸１.１８ｇ,Ｌ－半胱氨酸转化率为９３．２％,吲哚转化率为９０.１％。经分离纯化所得的Ｌ-色氨酸晶体,在熔点、旋光性和红外吸收光谱等方面与标准品完全一致。结论：色氨酸酶基因工程菌能有效地催化Ｌ－半胱氨酸和吲哚合成Ｌ－色氨酸,这种酶合成法是工业化生产Ｌ－色氨酸较为有效的方法之一。     

氮唑取代苯基醚类衍生物的合成及其抗真菌活性

通过取代溴苄与１－（２，４－二取代苯基）－２－（１Ｈ－吲哚和苯并咪唑－１－基）乙醇反应，合成了一系列１－｛２－「（取代苯基）甲基」－２－（取代苯基）乙基－１－吲哚和苯并咪唑类新化合物，并用二倍体稀释法对化合物进行了体外抗真菌试验。     

褪黑素对大鼠松果腺细胞产生前列腺素E_2的影响

采用松果腺细胞培养、前列腺素Ｅ２（ＰＧＥ２）放射免疫测定等方法，研究了松果除分泌的褪黑素（ＭＴ）对松果腺细胞产生ＰＧＥ２的影响。结果表明：ＭＴ０．１～１０μｍｏｌ·Ｌ－１抑制松果腺细胞产生ＰＧＥ２，０．０１～１０μｍｏｌ·Ｌ－１对抗去甲肾上腺素刺激松果腺细胞产生ＰＧＥ２，且以１μｍｏｌ·Ｌ－１的作用最为明显。提示ＭＴ对松果腺细胞功能有负性调节作用。Ｐ＜０．０１图２ＭＴ对去甲肾上腺素刺激松果腺细胞（１０５ｃｅｌｌｓ）转引产生ＰＧＥ２的影响●－●：ＮＥ；○－○：ＮＥ＋ＭＴ；ｎ＝４与对照组比较，Ｐ＜０．０５，Ｐ＜０．０１；与对应的去甲肾上腺素比较，△Ｐ＜０．０５，△△Ｐ＜０．０１３讨论支配松果腺细胞的交感神经纤维在暗相时产生与释放大量去甲肾上腺素，作用于松果腺细胞膜上的β１、α１受体，双重受体激动后通过Ｇ蛋白使蛋白激酶Ｃ激活，Ｃａ２＋、Ｋ＋、花生四烯酸增多，继而使ｃＡＭＰ、ｃＧＭＰ产生明显增加，松果腺细胞内特有的合成ＭＴ的限速酶Ｎ－乙酰转移酶和羟基吲哚－０－甲基转移酶被激活，从血液中摄取的色氨酸迅速转化为ＭＴ。在ＭＴ合成过程中，ＰＧ起很重要作用，因α１受体激动可使ＰＧ产生增多，ＰＧ进而促进ｃＧＭＰ生成和ＭＴ的合成?     

紫外分光光度法测定吲哚拉辛胶囊的含量

紫外分光光度法测定吲哚拉辛胶囊的含量鞍山市药品检验所１１４００２郭伟，高铁勇吲哚拉辛（ｃｉｎｍｅｔａｃｉｕｍ）为２－甲基－１－肉桂酰基－５－甲氧基吲哚－３－醋酸。具有消炎、镇痛、解热作用，临床用于风湿性病症的治疗。对吲哚拉辛及胶囊含量的测定，标准中采...     

抗心律失常药物的研究Ⅰ2－乙基－3－［4－（2－羟基－3－胺丙氧基）苯酰］吲哚嗪类化合物的合成及活性测定

以吲哚嗪类化合物Ｂｕｔｏｐｒｉｚｉｎｅ为先导物，结合β－受体阻断剂的结构特点，设计合成了９个吲哚嗪类化合物，均未见文献报道，其化学结构经红外光谱、核磁共振、质谱和元素分析确证。抗氯仿诱发小鼠室颤结果表明，化合物(２)，(６)具有明显的抗心律失常活性。     

以L—半胱氨酸和吲哚为底物酶合成L—色氨酸

目的：以L－半胱氨酸和吲哚为底物,利用色氨酸酶基因工程菌WW－11酶法合成L－色氨酸。方法：以IPTG诱导基因工程菌色氨酸酶表达,将酶活最高时的工程菌游离细胞作为转化反应的酶源,通过纸层析和氨基酸自动分析仪分析并测定转化液中L－色氨酸的含量,结果：80mL反应液（L－半胱氨酸0．75g,吲哚75g)37℃反应48h,可积累L－色氨酸1．18g,L-半腕氨酸转化率为93．2％,吲哚转化率为90．1％,经分离纯化所得的L－色氨酸晶体,在熔点,旋光性和红外吸收光谱等方面与标准品完全一致,结论：色氨酸酶基因工程菌能有效地催化L－半胱氨酸和吲哚合成L－色氨酸,这种酶合成法是工业化生产L－色氨酸较为有效的方法之一。     

Valproate-dependent changes in the spectrum of free amino acids in rats: l-carnitine effects

The effect of L-camitine (LC) in a dose of 100 mg/kg on the spectrum of free amino acids in the tissues and blood plasma was studied in rats pretreated for 8 days with valproic acid (VA) in a dose of 200 mg/kg. The VA treatment led to a decrease in the concentration of Ser, Gln, and Ala in the blood plasma and of Gln, Cys, Phe, and His in the liver, and to an increase in the level of Tau, Thr, Gly, alpha-Aba, Ile, and Tyr in the liver. In the rat brain, the concentration of PEA, urea, Ile, Val, Tyr, Phe, and alpha-Aba increased, while the Orn level decreased. The introduction of LC led to correction of the dysbalance of free amino acids, whereby the levels of Asp, Ctn, and Orn in the blood plasma and the levels of Cys and Tyr in the liver were increased, while the levels of Thr, Cly, alpha-Aba, and Ile in the liver and the levels of alpha-Aba, Val, and Phe in the brain were decreased. The character of variation of the spectrum of free amino acids and their derivatives in the tissues and blood plasma of rats confirms the toxicity of VA and shows the ability of LC to normalize (to a certain extent) the balance violated by the VA-induced LC insufficiency.     

中药苍术炮制方法及理论研究进展

目的 通过查阅相关文献,梳理并总结中药苍术的古今炮制方法沿革及理论研究进展,为苍术的炮制规范化研究提供文献依据和思路.方法 对近20年来国内外发表的相关文献进行分析、整理和归纳.结果古代本草中记载苍术的炮制方法主要有醋制、泔制、药汁制、蒸制、土制、童便制、盐制、焙制、酒制、火炮、姜制、油制、大茴香制、桑椹制、乳制、蜜制、烘制等19类,现代主要的炮制方法有炒焦、麦炒、米泔水制.苍术通过炮制可降低其挥发油、微量元素的含量,以达到制其燥性、缓和药性、增强疗效的作用,但临床上使用的苍术炮制品种较多且较混乱,品种质量差异较大,缺乏统一的炮制工艺和质量标准.结论 应坚持传统炮制方法与现代科学方法相结合的原则,进行苍术炮制工艺的优化研究和质量标准规范化研究,保证临床用药质量,以期为临床安全合理用药提供依据.     

应用体外反搏对结核性包裹性胸腔积液的临床研究

目的 研究应用体外反搏技术,观察对结核性包裹性胸腔积液患者包裹范围大小、积液的体积以及胸膜肥厚程度的影响。方法 选择包裹性胸腔积液患者200例,随机分为对照组及应用组,对照组给予正规抗结核治疗。应用组在正规抗结核治疗基础上加用体外反搏。两组患者均在体外反搏治疗前,疗程结束时及结束后30d,分别行胸部平片、B型超声及胸部CT检查,观察包裹积液范围大小、积液的体积以及胸膜肥厚程度的变化,计数资料用χ2检验,计量资料用t检验,对结果 进行统计学分析。结果 应用组：治愈19例,有效65例,总有效率84%。对照组：治愈7例,有效59例,总有效率66%。两组间有高度显著性差异P〈0.01。结论 体外反搏通过提高舒张期主动脉内舒张压,提高对多脏器的血液灌注,加快肺部及胸膜的血液循环。对结核性包裹性胸腔积液患者,能有效促进包裹中的液体吸收,减少其胸膜的肥厚、粘连、钙化,有肯定的效果。     

无痛可视人工流产术有效性安全性相关因素研究

目的：研究探索无痛可视人工流产术有效性与安全性之间的相关因素。方法：比较五组麻醉药（瑞芬太尼、瑞芬太尼＋丙泊酚、瑞芬太尼＋咪唑安定、丙泊酚、丙泊酚＋芬太尼）作用时间、止痛效果、副反应及对体温、呼吸、脉搏、血压及血氧饱和度的影响等,严格操作规范,完善各环节工作,总结有效性与安全性之间的相关因素。结果：五组麻醉药中对诱导、手术、苏醒时间和定向力恢复时间以瑞芬太尼＋丙泊酚组最佳,镇痛效果显著,差异具有统计学意义,P〈0．05：对生命指征的影响以瑞芬太尼＋丙泊酚组最小,安全系数最高,经统计学处理．P〈0．05。瑞芬太尼＋丙泊酚最佳用药量分别为0．9-1．4ug／kg、1．9—2．2mg／kg。无痛可视人工流产术有效性与安全性之间的相关因素有：手术适应证、全麻药组合及剂量的选择、施术环境及设备的配置、受术者知情同意、手术医生、护士和麻醉医师的责任心及技术水平、术后指导及随访等。结论：无痛可视人工流产术有效性安全性与手术适应证、全麻药组合及剂量的选择、施术环境及设备的配置、受术者知情同意、手术医生、护士和麻醉医师的责任心及技术水平、术后指导及随访等因素有关。     

人性化管理模式在护理管理中的运用

目的探讨人性化管理模式在医院护理管理中应用情况。方法采取前后对照的临床试验,设计调查问卷对148例护理人员在人性化管理模式实施前后满意程度及患者在人性化管理模式实施前后满意程度,总结人性化管理模式经验。结果 148例护理人员在人性化护理管理实施前满意人数有15例,占10.13%,一般人数有86例,占58.11%,不满意人数有47例,占31.76%,实施后满意人数有65例,占43.92%,一般人数有69例,占46.64%,不满意人数有14例,占9.46%;患者中实施前满意人数有9例,占6.08%,一般人数有54例,占36.49%,不满意人数有85例,占57.43%,实施后满意人数有32例,占21.62%,一般人数有81例,占54.73%,不满意人数有35例占23.65%。结论护理人员及患者在人性化管理模式实施前后对于医院护理管理的满意程度均有明显的提高,人性化管理模式适合临床护理管理。     

Antiarrhythmic action of 3-carbethoxyamino-5-dimethylaminoacetyl-iminodibenzyl hydrochloride (Bonnecor, AWD 19-166, GS -15) on experimental arrhythmia induced by aconitin, ouabain, calcium chloride and barium chloride

In comparison with detajmium, prajmalium, ajmaline, quinidine, lidocaine, disopyramide, propranolol, and Ethmozin the substance GS 015 is tested on the aconitin-induced arrhythmia of the rat, the auricular fibrillation by aconitin of the dog, the ventricular arrhythmia induced by ouabaine of the dog, the arrhythmia caused by calcium chloride of the rat, and the arrhythmia induced by barium chloride of the rabbit. The particular qualities of effect in the special forms of arrhythmia are discussed in connection with the study of the antiarrhythmic action in case of coronary occlusion, with the increase of the electric fibrillatory threshold, and with the electrophysiologic tests.     

Autoradiographic localization of high-affinity [3H]kainic acid binding sites in the rat forebrain

Utilizing in vitro autoradiographic techniques, we have studied the distribution of high affinity [3H]kainic acid ([3H]KA) binding sites in intact sections of the rat forebrain. These sites have the same kinetic and pharmacological characteristics as the [3H]KA site described in tissue homogenates. Moderate to high levels of specific binding were observed in several discrete brain regions. These include lamina I, V and VI of the neo- and cingulate cortex, superficial layers of the pyriform cortex, striatum, external plexiform and granule cell layers of the olfactory bulb, olfactory tubercle, the stratum lucidum of CA3 of the hippocampus, molecular layer of the dentate gyrus, reticular nucleus of the thalamus, the hypothalamic median eminence, and the granule cell layer of the cerebellum. Low levels of specific binding were associated with other discrete regions such as the lateral septum, bed nucleus of the stria terminalis, medial geniculate, superficial layers of the superior colliculus, nuclei of the central grey, interpeduncular nucleus and the molecular layer of the cerebellum. Moderate uniform levels of specific binding were observed over the hypothalamus, zona incerta and the amygdala. One of the important factors in KA neurotoxicity seems to be the presence of KA receptors, and regions that are susceptible to the toxic effects of KA after local administration, such as the striatum, hippocampus, amygdala and pyriform cortex, have moderate to high levels of binding. Thus, these data provide a useful map for studying the relationship between receptor-mediated and seizure-induced neuronal damage following KA administration.     

Hypervitaminosis A induced teratogenesis.

In the past decade, the toxicology of reproduction has become increasingly important. This branch of toxicology focuses on mutagenic and embryotoxic effects. The study of embryotoxicity requires an extensive knowledge of the interaction of drugs and embryonic tissues, normal and abnormal developmental processes, and the susceptible stages during prenatal development. Hypervitaminosis A is one of the most extensively studied teratogens. It produces defects in almost all organ systems. Therefore, this article will first of all review the vitamin A-induced malformations in several organ systems. Moreover, it will discuss their morphogenesis and the susceptible developmental stages. Thus, the first ten chapters will cover the following subjects: malformations of the nervous system, ocular malformations, malformations of the ear, craniofacial malformations, cleft palate, defects of the circulatory system, defects of the respiratory systems, defects of the digestive tract, urogenital defects, skeletal malformations, and abnormal postnatal development. Since in general little is known about the mechanisms involved in the induction of congenital defects, we think it is of great value to review the knowledge and experience that have been gathered by the experimental work with hypervitaminosis A. Therefore, the next chapters will discuss the following subjects: teratogenic effects in different species, minimum effective dose, interaction with other agents, influence of chemical form, solvent, and route of administration, pathophysiology of vitamin A embryotoxicity, and hypervitaminosis A and human pregnancy.     

网络模式在病历归档规范化管理中的应用

目的通过百泰网络探讨病历归档规范化管理的模式。方法通过网络对归档的病历进行快速、便捷的核查病历、化验单等页数,然后提交病案室,病案室及时记录科室病历归档的时限、病历的页数同时进行优化病历统计工作。结果规范了医院工作中病历归档便捷管理的工作流程,形成了医疗部门对归档病历质量实时的监控、检查、评价的基础依据,充分发挥了网络化管理的优势,加大了质量监管力度,全面提升了医院病案质量,缩短了医护工作量。结论通过网络进行病历归档,保证了病历的完整性、真实性、归档的及时性、规范性,方便了病历管理者的质控性,提升了全院医务人员病历书写的整体素质,提高了归档管理的现代化水平。     

认知行为干预模式对孕妇心理保健作用的实证研究

目的构建提高孕妇心理健康水平的认知行为干预模式并实证其有效性。方法以认知行为干预模式对实验组进行干预;并采用组内与组间比较的方式,对相关有效性指标进行考察,判断出干预的有效性。结果实验组与对照组干预前的年龄、孕次、产次、孕产知识水平、焦虑、抑郁、一般自我效能感、自尊方面的差异均无统计学意义（P〉0．O5）;干预后,组间比较在出生方式、顺产出血量、非顺产出血量、顺产产程1、顺产产程2、Apgar评分、孕产知识水平、焦虑、抑郁、一般自我效能感、自尊的2或t值分另1是3．978、一5．364、一3．724、一4．371、一2．179、3．200、98．346、一3．821、一3．186、3．151、5．556,差异均有统计学意义（P〈0．05或0．01、0．001）;实验组组内前后比较在孕产知识水平、焦虑、抑郁、一般自我效能感、自尊的t值分别是一97．703、4．89、4．O88、一10．10、一4．016,差异均有统计学意义（P〈0．001）。结论实验组实验后的有效性指标显著优于实验前,且显著优于对照组;因此,采用认知行为干预模式来提高孕妇心理健康水平是极其有效的。