消炎痛对癫痫保护作用的免疫学研究

目的　评价消炎痛在癫痫神经细胞退行性变中的作用。方法　免疫组化染色。结果　海仁酸诱导的实验性癫痫大鼠海马小胶质细胞表达 MHC- 、MHC- 类分子和 C3 b受体。用消炎痛处理后 ,其表达可明显降低。同时消炎痛还可阻止部分神经元退行性变。结论　消炎痛通过抑制免疫应答对实验性癫痫大鼠海马退行性变具有保护作用。     

复方吲哚美辛栓对取环镇痛及宫口松弛的作用

[目的]比较三种不同药物肛门内置入后对取环手术镇痛及宫口松弛的作用.[方法]将90例择期行取环手术的妇女随机分为三组,分别于肛门内置入复方吲哚美辛栓1粒(A组),或0.4 mg米索前列醇(B组),或者安慰荆甲硝唑片200 mg(C组),1 h后行取环手术.术中判断宫颈软化程度及阴道出血量,记录手术时间和各种副反应以及最终能否取出宫内节育器,术毕患者评价术中疼痛视觉模拟评分(VAS).[结果]三组一般资料差异无显著性,宫颈软化程度C组显著低于A、B两组,C组较其他两组手术时间显著为长、手术成功率显著为低,术中疼痛VAS评分A组＜B组＜C组.[结论]复方吲哚美辛栓在取环手术前直肠内应用,可在一定程度上软化宫颈、缩短手术时间、提高手术成功率,并且可以减轻术中疼痛.     

Androgen metabolic response to indomethacin and the alkaline phosphatase inhibitor levamisole in fibroblasts

OBJECTIVES: The aim of this investigation is to study the effects of indomethacin (I) and the alkaline phosphatase (ALP) inhibitor levamisole (L) on androgen 5alpha-reductase expression in gingival and periosteal fibroblasts, in the context of repair in the periodontium. Chronically inflamed human gingival fibroblasts (HGF) were used to demonstrate the comparative effects of L on HGF and human oral periosteal fibroblasts (HPF). MATERIAL AND METHODS: Monolayer cultures of six cell lines of HPF of the fifth to ninth passage were incubated in duplicate with 14C-testosterone/14C-4-androstenedione as substrates in Eagle's MEM; I was added at concentrations of 1 and 3 microg/ml in the presence or absence of the established inhibitory concentration of 30 microg/ml L and incubated for 24 h. The medium was solvent extracted for radioactive metabolites, separated by thin layer chromatography and quantified. RESULTS: L caused 50% inhibition of 5alpha-reductase and 17beta-hydroxysteroid dehydrogenase activity in HGF. In HPF, 5alpha-reductase expression was enhanced by I with both substrates, by 65-76% (n = 6; p<0.01), inhibited by 30-50% (n = 6; p<0.01) with L and restored to control values in combination. CONCLUSION: Yields of androgen metabolites may be linked to ALP activity, with implications on healing, during adjunctive treatment of inflammatory periodontal disease with I.     

建立具有药物代谢酶CYP2C9活性的微生物模型

 目的研究短刺小克银汉霉AS 3.910体外模拟人体细胞色素P450(CYP)2C9的能力,建立具有CYP2C9活性的微生物模型。方法选用3种人体CYP2C9代谢的药物格列本脲、双氯芬酸和吲哚美辛为底物,利用液相色谱-质谱联用技术检测药物代谢产物的种类和转化率。结果通过调节转化培养基的种类和初始pH,使转化系统在较高底物浓度下具有良好的转化效果,格列本脲、双氯芬酸和吲哚美辛总转化率分别为90%,100%和83%,而且形成的主要转化产物与人体CYP2C9产生的主要代谢产物相同。结论短刺小克银汉霉AS 3.910具有CYP2C9代谢酶活性,是研究人体CYP2C9药物代谢适宜的体外模型。     

环氧合酶-2抑制剂对大鼠骨关节炎模型软骨中血管内皮生长因子表达的影响

目的研究环氧合酶-2抑制剂(吲哚美辛)对大鼠骨关节炎模型关节软骨中血管内皮生长因子(VEGF)表达的影响。方法健康雄性wistar大鼠30只,随机均分为对照组、骨性关节炎组(OA组)和吲哚美辛处理组。利用膝关节注射4%的木瓜蛋白酶溶液的方法制作骨关节炎模型。采用关节炎评分法评定各组大鼠平均关节炎指数(MAI),免疫组化方法与Western blot方法检测关节软骨中VEGF蛋白的表达变化。结果 OA模型组随着造模的时间延长,关节出现了重度红肿现象,对照组关节无任何异常变化;与OA模型组比较,吲哚美辛组的关节炎症反应呈现消退现象。VEGF蛋白在对照组大鼠关节软骨仅有微量表达,而在术后8周OA组大鼠关节软骨表达则显著升高(P0.01);与OA组相比,吲哚美辛组大鼠关节软骨中VEGF蛋白表达显著降低(P0.01)。结论吲哚美辛对骨关节炎的抑制作用可能与下调VEGF蛋白的表达相关。     

Possible mechanism underlying the effect of Semax on the formation of indomethacin-induced ulcers in rats

Intraperitoneal injection of Semax (synthetic analogue of ACTH4-7, MEHFPGP) in a dose of 50 mg/kg produced a protective effect on rats with experimental indomethacin-induced ulcers. Experiments on narcotized rats showed that Semax in the studied dose had no effect on basal blood flow in the stomach, but prevented reduction of blood flow induced by indomethacin. The antiulcer effect of Semax is probably related to improvement of blood flow in the gastric wall disturbed by indomethacin.     

Mixed Hyperbranched/Triblock Copolymer Micelle Assemblies: Physicochemical Properties and Potential for Drug Encapsulation

Mixed micelles have numerous advantages while requiring little to no effort in preparation. This study aims to produce mixed micelle nanostructures from a linear triblock copolymer and a hyperbranched random copolymer, and is able to be loaded with the weakly water-soluble drugs curcumin and indomethacin. Different preparation techniques are employed to produce mixed micelles comprised of Pluronic F127 block copolymer, and hyperbranched poly[(ethylene glycol) methyl ether methacrylate-co-lauryl methacrylate], H-[P(OEGMA-co-LMA)], copolymer. Few studies have dabbled in these types of coassemblies, which provides insight into how structural differences of each copolymer can affect the formation of micelles. To determine the properties of the emerging nanostructures in aqueous environments, including their size, homogeneity, and surface charge, different physicochemical techniques are used, such as light scattering and spectroscopic methods. The results reveal that the copolymers combine, and spontaneously self-assemble into mixed micelle-like nanostructures in aqueous environments, whereas both systems of neat and drug-loaded nanostructures exhibit desirable properties such as small average micelle hydrodynamic radii and low size polydispersity indices. The nanostructures that result from the effective encapsulation of curcumin exhibit outstanding stability over 169 days. The fluorescent qualities of curcumin persist after encapsulation, making the novel nanostructures excellent candidates for bioimaging applications.     

Caspases在消炎痛所致胃黏膜细胞凋亡中的作用

目的　研究大鼠在体情况下消炎痛(IND) 所致胃黏膜细胞凋亡过程中caspase 3、8基因及蛋白表达的变化,以探讨其黏膜损伤机制。方法　SD大鼠以不同剂量IND(30、60、90、120mg/kg)灌胃后3h处死,另设对照组。采用TUNEL标记技术检测黏膜细胞凋亡;分别采用原位分子杂交和RT PCR检测caspase 3基因表达的变化,应用免疫组化方法同步检测caspase 3、8蛋白表达的变化。结果　TUNEL标记显示对照组大鼠胃黏膜仅见少量凋亡细胞,IND组凋亡细胞数明显增加,计算机图像分析显示阳性细胞平均像素点在IND 30、60、90、120mg/kg组分别为对照组的6 3、8 0、12 6和17 1倍(P<0 01);原位分子杂交显示,caspase 3 mRNA在对照组胃黏膜呈弱阳性表达,IND 30~90mg/kg组呈中等至强阳性,120mg/kg组呈强阳性表达,与对照组相比均有显著差异(P<0 01), caspase 3 mRNA表达变化同细胞凋亡之间呈明显正相关(r=0 9642,P<0 01);RT PCR显示对照组胃黏膜中caspase 3 mR NA表达量极少,IND各剂量组的caspase 3/βactin吸光度比值较对照组明显升高(P<0 01);免疫组化染色显示对照组胃黏膜caspase 3、8蛋白均呈弱阳性表达,caspase 3表达水平强于caspase 8(P<0 05),IND使caspase 3、8蛋白表达呈中等至强阳性,明显高于对照组(P<0 05),IND各剂量组caspase 3     

"Hemicrania continua": The first bilateral case?

The patient reported had had a continuous headache involving the whole skull for 7 years. Many drugs had failed to relieve the pain, but with indomethacin the headache completely disappeared within 3 days. Nine months later the treatment was discontinued without any relapse. This variety of headache, not previously reported, was quite similar to the "hemicrania continua" except for its localization.