东北淫羊藿活性成分研究

自东北淫羊藿（ＥｐｉｍｅｄｉｕｍｋｏｒｅａｎｕｍＭａｋａｉ）的地上部分，分离得到４个单体化合物，根据理化数据和光谱分析鉴定为：金丝桃甙（ｈｙｐｅｒｉｎ）（１），淫羊藿甙－Ⅱ（ｉｃａｒｉｓｉｄⅡ）（２）．淫羊藿甙－Ⅰ（ｉｃａｒｉｓｉｄⅠ）（３）和淫羊藿甙（ｉｃａｒｉｉｎ）（４）．其中，金丝桃甙在本种植物中首次分离得到，同时，我们又利用１Ｈ－１Ｈｃｏｓｙ和１３Ｃ－１Ｈｃｏｓｙ谱，对原文献中化合物２部分Ｃ信号的归属进行了修正，另外，药理实验结果表明：淫羊藿甙（ｉｃａｒｒｉｎ）对氢化可的松造成的小鼠阳虚有一定的拮抗作用．     

异叶败酱黄酮类成分的研究

从异叶败酱（ＰａｔｒｉｎｉａｈｅｔｅｒｏｐｈｙｌｌａＢｇｅ．）地上部分甲醇提取物中分得２个黄酮类化合物，经光谱分析与化学方法鉴定为：金丝桃甙（Ⅰ），异槲皮甙（Ⅱ），这２个化合物在败酱科植物中均是首次报道。     

金丝桃甙(hyperin)药理作用研究进展

金丝桃甙系锦葵科植物黄蜀葵中提取的有效单体，属黄酮醇甙化合物，临床上对很多疾病有很好疗效。具有镇痛，保护脑缺血损伤等作用，并对钙离子内流有影响。本文综述近年来金丝桃甙的临床应用及药理研究的概况。     

金丝桃甙中枢镇痛作用及其机制的研究

金丝桃甙5μg/只(20g)侧脑室注射,经小鼠甩尾试验,热板法测痛,证实其有显著的中枢镇痛作用,其作用效价强度约等吗啡的1/20;相当于外周给药(腹腔给药)的100倍。用放射免疫法测得各脑区亮氨酸脑啡肽与金丝桃甙镇痛作用无关,纳络酮亦未能拮抗金丝桃甙的镇痛作用,但侧脑室注射CaCl_2和EGTA可分别拮抗和增强金丝桃甙的镇痛作用,并用原子吸收光谱法测得金丝桃甙产生镇痛作用时,小鼠脑内Ca~(2+)含量显著地减少。提示金丝桃甙中枢镇痛作用可能与降低脑内Ca~(2+)含量有密切关系。     

罗布麻中金丝桃甙的脉冲极谱测定

本文报道了罗布麻中金丝桃甙的提取、分离和脉冲极谱测定条件。罗布麻中含有较大量的金丝桃甙,生药用甲醇提取后用聚酰胺板分离,展开剂为氯仿—甲醇—水(4:1.5:0.1),用5 ml混合溶剂浸泡、洗脱,金丝桃甙在0.1 M硫酸铵底液中于—1.45V(vs SCE)有很好的峰形。     

秦岭三种金丝桃属植物药中金丝桃甙的含量测定

用薄层一紫外分光光度法测定了秦岭地区三种金丝桃属植物药贯叶连翘、红旱莲、大对经草中金丝桃甙的含量。结果以红旱莲含金丝桃甙为最高，达１．１７２％。     

万山淫羊藿的化学成分(Ⅱ)

从万山淫羊藿（EpimediumwanshanenseS.ZHeetGuo）全草中分离得到6个成分，经化学与光谱方法鉴定为胡萝卜甙（daucosterol）、宝藿甙-I（baohuoside-I）、淫羊藿次甙-I（karisid-I）、槲皮素（quercetin）、淫羊藿次甙-C（epimedoside－C）和淫羊藿甙（icariin），均为首次从该植物中获得。     

三氟拉嗪对金丝桃甙镇痛作用的影响及机制的分析

以前工作表明金丝桃甙的镇痛作用与减少神经末梢钙内流有密切关系.本文在小鼠热板模型及痛介质诱发的神经放电模型上.发现预处理5mg·kg~(-1)的三氟拉嗪可显著减弱金丝桃甙的镇痛作用;并不被多巴胺受体激动剂及侧脑室注射多巴胺所逆转;在小鼠扭体上.利血平及酸妥拉明Sc后.金丝桃甙镇痛作用未见有显著变化。实验结果提示金丝桃甙镇痛作用与去甲肾上腺素能系统无关,而与钙调蛋白活性有关。     

西陵知母中新芒果甙的分离与结构鉴定

西陵知母中新芒果甙的分离与结构鉴定洪永福韩公羽郭学敏（第二军医大学药学院中西药研究室，上海２００４３３）知母（ＡｎｅｍａｒｈｅｎａａｓｐｈｏｄｅｌｏｉｄｅｓＢｇｅ．）为常用中药，以根茎入药。文献［１］记载，我国河北易县西陵出产的为最佳品，以“西陵知母...     

木根黄芩地上部分成分研究

首次从木根黄芩地上部分分离出13个化合物，经理化常数和光谱分析分别鉴定为异甘草甙元（isoliquiritigenin），蓟黄素(cirsimaritin），汉黄芩素（wogonin），芹菜素（apigenin），粘毛黄芩素Ⅲ(viscidulin Ⅲ），紫丁香甙（syringin），白杨素－6－C-β－D－葡萄糖－8－C－α－L－阿拉伯糖甙（6－C－β－D－glucosyl-8-C-α-L-arabinosylchry-sin），白杨素－6－C－α-L－阿拉伯糖－8－C－β－D－葡萄糖甙（6－C－α－L－arabinosy1-8-C-β-D-glucosylchryin），黄芩甙（baicalin），汉黄芩甙（acteoside和martynoside）。其中异甘草甙元，蓟黄素和紫丁香甙均为首次从黄芩属植物中分离得到。     

Effect of alkali treatment on properties of native shellac and stability of hydrolyzed shellac

The objective of this study was to investigate the effect of alkali treatment on properties of shellac. The native shellac was treated with sodium hydroxide for 15, 30, and 60 min to obtain hydrolyzed shellac. All types of shellac, namely native and hydrolyzed shellac at various times of treatment, were then prepared in films as free acid and ammonium salt forms by using ethanol and ammonium hydroxide solution, respectively. The results showed that alkali treatment caused an increase in acid value and a decrease in ester value. This is due to higher free carboxylic and hydroxyl groups caused by ester bond breaking. The longer the alkali treatment the higher impact of bond breaking, therefore, causing an increase in acid value, solubility at pH 7, strain, a decrease in ester value, water vapor permeability coefficient, and stress. The films were then kept at 40 degrees C, 75% RH for a period of three months. The aging effect led to an esterification of free carboxylic and hydroxyl groups, resulting in the significant change of acid value, ester value, and insoluble solid for both native and hydrolyzed shellac films in acid form. On the other hand, all types of shellac films in ammonium salt form exhibited a reasonable stability in physicochemical and mechanical properties as all films were protected from the esterification due to the formation of ammonium salt at the carboxylic binding site. It could be concluded that alkali treatment could produce hydrolyzed shellac with higher solubility in the intestine, the stability was yet in dilemma unless the shellac was in an ammonium salt form. The result obtained could, thus, provide a guideline in the use of shellac.     

A fluorometric method for the determination of praziquantel in blood-plasma and urine

Some physicochemical data of praziquantel which may have analytical relevance are reported. For the quantitative determination praziquantel is extracted from plasma or urine by means of organic solvents and then hydrolyzed in an aqueous alkaline solution. The hydrolyzed product is reacted with dansyl-chloride (5-dimethylaminonaphthalene-sulfonylchloride). The dansylated compound is separated and quantified fluorometrically. The limit of determination is 3 micrograms/l in blood plasma and 30 micrograms/d in urine. For both fluids, the imprecision is approximately 7.5%. The method is suitable for the determination of praziquantel in patients or healthy volunteers treated with therapeutic doses.     

2，4-噻唑二酮的合成

以硫脲和氯乙酸忆酯为原料,经环合、中和,得到2-亚胺基-4-噻唑酮,然后用20%盐酸水解,合成了目标物2,4-噻唑二酮,总收率为61%,该方法未见文献报道。     

The synthesis of 7-substituted-3-dinitrostyryl cephalosporins and their ability for detecting extended spectrum beta-lactamases (ESBLs)

We synthesized 7-substituted-3-(2,4-dinitrostyryl)cephalosporin derivatives which were Nitrocefin analogs, for detecting extended spectrum beta-lactamase (ESBL) specifically. HMRZ-86 which has carboxypropyloxyimino group on 7-aminothiazolacetamide substituent were not hydrolyzed by class A, C and D beta-lactamases, but it was hydrolyzed by ESBL and metallo beta-lactamase (class B), then its color changed from yellow to red. The hydrolysis of metallo beta-lactamase was inhibited by adding sodium mercapto acetic acid (SMA). Therefore HMRZ-86 is a useful chromogenic agent to detect ESBL specifically.     

促神经生长因子生长剂Neotrofin的合成

对氨基苯甲酸乙酯用丙烯酰氯酰化，在碱催化下对腺嘌呤9-位N进行烷基化，随后经重氮化、水解得促神经生长因子生长剂Neotrofin，总收率为55％。     

木糖的制备研究

将蔗糖与１％的硫酸混合，加压水解后用碳酸锶除去溶液中的硫酸，滤液经脱色、离子交换净化、浓缩结晶得含量在９７％以上的结晶木糖，一次结晶收率大于１２％（不包括母液中残留木糖）。     

头孢呋辛酸反应体系的优化

以7-ACA为原料,通过与N-甲氧亚氨基呋喃乙酰氯缩合、3位水解、然后与氯磺酰异氰酸酯缩合水解得头孢呋辛酸,在与氯磺酰异氰酸酯的缩合反应过程中,用乙酸丁酯作为反应媒介具有操作简单、产品收率高等特点,适合于工业化生产。     

Carboxylesterases in the respiratory tracts of rabbits, rats and Syrian hamsters

Esters are a widespread class of organic compounds found both in industry and the environment. Because esters are often volatile and, therefore, readily inhaled, the capacity of respiratory tract tissues as well as liver S-9 homogenates from rats, rabbits, and Syrian hamsters to hydrolyze a variety of esters was investigated. A new technique to determine hydrolysis rates by measuring carboxylic acid residues using ion chromatography was proven effective. The results indicated that esters, including potentially carcinogenic beta-lactones, are readily hydrolyzed by respiratory tract enzymes. Species and tissue differences were apparent. The nasal ethmoturbinates had especially high levels of esterase activity with tissue weight-normalized activities from rabbits and hamsters for most substrates exceeding all other tissues tested, including liver. Phenyl acetate was the most rapidly hydrolyzed by ethmoturbinate tissue of the esters tested. Among straight chain aliphatic alcohol acetates, hydrolysis rates increased with carbon number up to pentyl alcohol and then decreased. Branched 4-carbon alcohol acetates were less rapidly hydrolyzed than n-butyl acetate. Correlation of hydrophobicity constants with hydrolysis rates indicated that, for the straight chain aliphatic acetates, a bilinear model best fit the data.     

盐酸头孢他美酯的合成

盐酸头孢他美酯是一口服前体药,口服后在体内迅速水解为具有抗菌活性的头孢他美。本文报道了盐酸头孢他美酯的制备方法,其生产工艺简单,成本低廉:以3-去乙酰氧基-7-氨基头孢烷酸(7-ADCA)为起始物与活性酯反应,先制备头孢他美(酸),然后和特戊酸卤甲酯反应生成头孢他美酯,最后头孢他美酯成盐得盐酸头孢他美酯。     

Metabolism of glycyrrhizin by human intestinal flora.

During the course of experiments on the metabolism of Chinese crude drugs by human intestinal flora, glycyrrhizin, an active component of liquorice, was shown to be hydrolyzed to the aglycone, 18-beta-glycyrrhetic acid, which was then transformed to a new compound, 3-epi-18beta-glycyrrhetic acid. The epimerization of 18beta-glycyrrhetic acid to 3-epi-18beta-glycyrrhetic acid was also shown to be reversible VIA a metabolic intermediate, 3-dehydro-18beta-glycyrrhetic acid.