三尖杉碱吲哚类似物的全合成

目的 合成三尖杉碱吲哚类似物。方法 以色胺为原料经缩合、环合、水解与脱羧反应得吲哚哌啶酮化合物,经Ｂｉｓｃｈｌｅｒ－Ｎａｐｉｅｒａｌｓｋｉ反应得烯胺。通过烯胺的化与氧化－重排反应得到吲哚氮杂Ｚｈｕｏ化合物。用溴苄与吲哚氮杂Ｚｈｕｏ反应在吲哚环上引入苄基保护基,经还原、环合反应合成了三尖杉碱吲哚类似物。结果 经１０步反应合成了三尖杉碱吲哚类似物。总收率１４．３％。结论 合成得三尖杉碱吲哚类似物,并对     

大花千里光中吡咯里西啶生物碱的分离与鉴定

从菊科植物大花千里光Senecioambraceus全草的甲醇提取物中首次分离并鉴定了5种吡咯里西啶生物碱，它们是千里光碱（senecionine，Ⅰ）、全缘千里光碱（integerrimine，Ⅱ）、千里光菲灵碱（seneciphylline，Ⅲ）、克氏千里光碱（senkirkine，Ⅳ）和倒千里光碱（retrorsine，v）。     

钩藤中不同成分降压作用的差异

目的：比较钩藤中提取的异钩藤碱、钩藤碱、钩藤总碱及非生物碱部分的降压作用。方法：大鼠麻醉后经颈总动脉插管记录外周血压和经股静脉微量输注实验用药。结果：实验表明钩藤中４种成分的降压强度为异钩藤碱（４２．０％）〉钩藤碱（３２．１％）〉钩藤总碱（２１．３％）〉钩藤非生物碱（１２．４％）。结论：提示钩藤中主要降压成分为异钩藤碱的钩藤碱。     

三尖杉碱吲哚类似物的全合成

目的合成三尖杉碱吲哚类似物。方法以色胺为原料经缩合、环合、水解与脱羧反应得吲哚哌啶酮化合物,经Bischler-Napieralski反应得烯胺。通过烯胺的溴化与氧化-重排反应得到吲哚氮杂     

青藤生物碱成分的研究

目的: 研究青藤 (sinomenium actum(thumb) Rehd.et wils)中具有纳洛酮戒断作用的生物碱类化学成分.方法: 采用硅胶柱层析进行分离纯化,通过理化和波谱分析鉴定其化学结构.结果: 从青藤的氯仿部分分离得到3个生物碱,经理化和波谱分析鉴定为青藤碱1 (sinomenine)、青风藤碱2(sinoacutine)和木兰碱3 (magnoflorine).结论: 青藤中可分离到3种生物碱.     

HPLC法测定糖渴清片中小檗碱,掌叶防己碱和药根碱的含量

本研究建立了反相高效液相法测定新药糖清片中小檗碱、掌叶防己碱和药根碱含量的方法。固定相为ＹＷＧ Ｃ１８，１０μｍ，４．６（ｉ．ｄ．）×２５０ｍｍ柱；流动相为乙腈－水（１：１，每１０００ｍｌ含磷酸二氢钾３．４ｇ及十二烷基硫酸钠１．７ｇ）；检测波长为３４５ｎｍ；小檗碱、掌叶防己碱和药根碱的加样回收率分别为９６．００±１．９９％，９８．９２±１．６２％，９７．２８±１．６２％。     

L-半胱氨酸修饰电极在高浓度抗坏血酸共存下测定多巴胺

目的为了研究多巴胺的测定,并有效排除抗坏血酸的干扰,制备了聚L-半胱氨酸修饰电极。方法通过电化学方法将L-半胱氨酸修饰到玻碳电极表面,采用线性扫描溶出伏安法对多巴胺进行定量分析。结果实验表明,该修饰电极对神经递质多巴胺的电化学氧化有显著的催化作用,峰电流明显增大,线性范围为2.0×10-7～1.0×10-4mol/L,检出限为2.0×10-8mol/L。结论该聚合物修饰电极具有良好的选择性,用于多巴胺的测定,能有效地排除抗坏血酸的干扰,结果令人满意。     

聚脯氨酸修饰电极循环伏安法选择性测定去甲肾上腺素

目的 建立聚脯氨酸修饰电极测定去甲肾上腺素的新方法,并有效排除肾上腺素与抗坏血酸干扰.方法 在pH 9.0的磷酸盐缓冲溶液中.用循环伏安法制备了聚脯氨酸修饰电极,研究去甲肾上腺索在聚合物薄膜上的电化学行为,建立测定去甲肾上腺素的电化学分析新方法.结果 在pH 7.0的磷酸盐缓冲溶液中,去甲肾上腺素在修饰电极上呈现一对灵敏的氧化还原峰,利用循环伏安法测定其还原峰电流可排除肾上腺素与抗坏血酸干扰.去甲肾上腺素检测的线性范围是7.0×10-7～1.1×10-4mol/L:检出限为6.0×10-8mol/L.结论 该修饰电极具有良好的灵敏度、选择性和稳定性,用于药剂样品分析,结果满意.     

阿托品敏感场效应传感器的研制和应用

Atropine-H2SO4 is widely used in clinic. The atropine sensitive electrode has been prepared, but Atropine field-effect transistor (Atropine-FET) has not been reported. In this communication, electro-active material is atropine tetraphenylboron. The sensor was fabricated by coating solution composed of electro-active material, dibutyl phthalate (DBP) and 5% PVC in tetrahydrofuran (THF) on Pt wire of gate electrode of MOSFET. The sensor showed linear response to atropine within concentration range 2.0 x 10(-2)-6.3 x 10(-5) mol/L. The slope of the sensor was 55 mV/decade and the limit of detection was 1.6 x 10(-5) mol/L. The sensor response was not affected by pH in the range 3.2-8.2, and the sensor can be used for the determination of atropine sulphate in drug-substances by direct potentiometry. The results of determination were in agreement with the data obtained by the official method in Chinese Pharmacopoeia. The method appears to be a rapid, simple and precise one.     

乌头碱对胎鼠中脑多巴胺能神经元细胞的神经毒性作用

目的: 观察乌头碱对中脑多巴胺能神经元细胞的毒理作用,以了解和预防乌头碱及其衍生物产生的神经毒性作用。方法: 从孕14 d的小鼠中取出胎鼠中脑,并分离出多巴胺能神经元细胞,于5％CO2,37 ℃和100％湿度条件培养,培养第10天加入不同浓度的乌头碱(0.1,0.5,1,5,10,50 和100 μmol/L)作用48 h,于第12天免疫组化染色。选取神经元细胞数、神经元树突的长度和数量作为观察指标,并进行分析。结果: 乌头碱作用48 h后,不同浓度的乌头碱(0.5～100 μmol/L)对神经细胞生长均有明显的抑制作用,并表现出浓度依赖性神经毒性作用,高浓度乌头碱(10～100 μmol/L)的抑制强度高于低浓度组(0.5～5 μmol/L)。结论: 体外实验证实了乌头碱对中脑多巴胺能神经元有神经毒性作用。     

一氧化氮光纤传感技术的初步研究

根据ＮＯ与过氧化氢反应生成过氧亚硝酸（ＯＮＯＯＨ）,ＯＮＯＯＨ极易氧化鲁米诺产生化学发光的原理,我们初步建立了一种行传感技术,并对该传感系统的最佳实验条件进行了研究。     

锌离子对牙各矿化成份破骨细胞性吸收的体外调控

目的:研究锌离子对破骨细胞体外吸收牙片功能的影响.方法:体外分离、培养新生乳兔破骨细胞,与玻片和灭活牙片共同培养,加入不同浓度锌离子.抗酒石酸酸性磷酸酶(TRAP)染色鉴定玻片上的破骨细胞,显微摄影分析破骨细胞吸收造成的牙片上的吸收陷窝,原子吸收分光光度法测定溶出的钙,并将实验组与对照组上清液钙离子浓度的比值定义为骨吸收指数,以评价破骨细胞的功能.结果:体外成功分离培养出多核的、TRAP(+)的破骨细胞.破骨细胞吸收牙片时,首先在接近牙根牙骨质或牙本质部位开始形成吸收陷窝,这与这些部位的矿化程度相对较低有关;破骨细胞在牙片上形成的吸收陷窝与骨片相比,吸收陷窝数量较少,体积较小,多为正圆形;吸收深度较浅,常为大面积的浅吸收.用原子吸收分光光度法测定不同浓度的锌离子对溶出的钙和骨吸收指数的影响,初步结果表明,培养第3天,1×10^-4～1×10^-14 mol/L锌离子刺激破骨细胞吸收牙片,其中1×10^-8 mol/L,1×10^-10 mol/L和1×10^-14 mol/L锌离子能够显著刺激吸收(P＜0.05);但是到了培养第7天,各浓度组除了对照组和1×10-14 mol/L锌离子还进一步有吸收外,其余浓度锌离子组的上清液钙离子浓度与自身第3天相比都有降低,但与同时期的对照组相比差异无统计学意义.在培养末期(第7天)1×10^-4～1×10^-7 mol/L,1×10^-9 mol/L,1×10^-12 mol/L和1×10^-13 mol/L浓度组的骨吸收指数小于1,而1×10^-8 mol/L,1×10^-10 mol/L,1×10^-11 mol/L和1×10^-14 mol/L浓度组骨吸收指数都大于1.结论:锌离子对破骨细胞吸收功能的作用与浓度和时程有关.     

Insulin sensitivity and the diffuseness of coronary artery disease in humans

Objective To study the relationship between insulin sensitivity and diffuse coronary artery disease.Methods Ninety-two consecutive patients underwent coronary angiography were enrolled in the study. Relationships between the results of angiograms and both glucose tolerance and blood lipids were analyzed.Results The mean age of the 92 patients (70 males, 22 females) was 65.4±6.3 y. In the 78 patients diagnosed by angiography as coronary artery disease, diffuse lesion was more common in diabetic patients than in those without a diabetes history (12/13 vs 24/65, P=0.00026). Fasting glucose ［(6.06±2.43)×10(-3) mol/L vs (4.80±1.47)×10(-3) mol/L, P=0.009］, glucose levels at one hour ?(12.37±4.38)×10(-3) mol/L vs (9.10±3.97)×10(-3) mol/L, P=0.001］, two hours ［(11.12±5.64)×10(-3) mol/L vs (7.49±4.29)×10(-3) mol/L, P=0.003］ and three hours ［(8.11±5.51)×10(-3) mol/L vs (5.56±3.46)×10(-3) mol/L, P=0.020］ after food were higher in patients with diffuse coronary disease than in those with non-diffuse coronary disease. Differences in the insulin sensitivity index (ISI) between the two groups was statistically significant (-4.36±0.52 vs -3.89±0.69, P=0.003). The incidence of multiple-vessel disease in diabetic patients was higher than that in non-diabetic patients (12/13 vs 33/65, P=0.00565). Glucose levels at two hours ［(10.22±5.57)×10(-3) mol/L vs (7.67±4.43)×10(-3) mol/L, P=0.034］ and three hours ［(7.90±5.47)×10(-3) mol/L vs (5.22±2.79)×10(-3) mol/L, P=0.007］ after food were higher in patients with multiple-vessel disease than in those with single-vessel disease. Impaired insulin sensitivity without a history of diabetes mellitus was commonly seen in patients with coronary artery disease.Conclusions The diffuseness of coronary artery disease is associated with insulin sensitivity and blood glucose levels. Insulin resistance is a common phenomenon in non-diabetic patients.     

羧基化多壁碳纳米管修饰电极对秦皮中秦皮乙素的灵敏测定

目的研究秦皮乙素在羧基化多壁碳纳米管(c-MWCNTs)修饰电极上的电化学行为及其测定方法。方法利用交流阻抗法(EIS)和循环伏安法(CV)表征修饰电极,用CV研究秦皮乙素在电极上的电化学行为,以差示脉冲伏安(DPV)对其含量进行测定。结果 c-MWCNTs修饰电极对秦皮乙素有明显的电催化作用,在pH4.5磷酸缓冲液(PBS)中,氧化峰电流与秦皮乙素浓度在6.0×10-2～8.0μmol/L范围内呈良好的线性关系,检测限为5.0×10-3μmol/L。结论 c-MWCNTs修饰电极与裸玻碳电极(GCE)相比,提高了秦皮乙素的检测灵敏度,可用于实际样品中秦皮乙素含量的测定。     

Preparation of a new tissue-based biosensor]

A new adenosine electrode using rabbit thymus tissue as catalyst is described. The tissue membrane was immobilized at the surface of an ammonia gassensing electrode for determination of adenosine in body fluid or tissue samples. This tissue-based biosensor showed excellent selectivity, and sensitivity, with a response slope of 51.2mV/decade, linear range of 3.16 x 10(-5)-5.62 x 10(-3) mol/L, coefficients of variation ranging from 1% to 5.72% (n = 7, m = 5), recoveries of adenosine in rabbit blood from 94.9% to 108.4% (n = 5, m = 5), and response time of 7 min. The life-time of the electrode was 25 days and 14 analogous compounds showed no significant interference.     

钙通道、钙调蛋白拮抗剂对内皮素—1分泌的影响

OBJECTIVE: The study is to investigate the effects of calcium channel blockers and calmodulin inhibitors on the secretion of endothelin-1 (ET-1) in cultured endothelial cells from human umbilical veins. RESULTS: Results showed that calcium channel blockers verapamil (5.5 x 10(-6) mol/L, 5.5 x 10(-5) mol/L), diltiazen (2.4 x 10(-4) mol/L) and calmodulin inhibitors chlorpromazine (3.1 x 10(-5) mol/L, 3.1 x 10(-4) mol/L), berbamine (1.6 x 10(-5) mol/L, 1.6 x 10(-4) mol/L) significantly decreased medium ET-1 levels in cultured endothelial cells. CONCLUSION: It was also indicated that extracellular calcium influx and calmodulin activity were necessary to the secretion of ET-1. In addition, nitroglycerine (2.2 x 10(-3) mol/L) remarkably reduced medium ET-1 levels in cultured endothelial cells, which suggested that nitric oxide might inhibit the secretion of ET-1.