Aspirin-like drugs may block pain independently of prostaglandin synthesis inhibition

Summary Using flurbiprofen, a chiral anti-inflammatory and analgesic 2-arylpropionic acid derivative, the enantiomers of which are not converted to each other (less than 5%) in rats or man, we obtained evidence that prostaglandin synthesis inhibition is primarily mediating the anti-inflammatory activity but prostaglandin synthesis independent mechanisms contribute to the analgesic effects. Thus, the S-form inhibited prostaglandin synthesis, inflammation and nociception in rats. The R-form had much less effect on prostaglandin synthesis and did not affect inflammation. It did, however, block nociception in rats almost as potently as the S-form. S-flurbiprofen, in contrast to the R-form, was clearly ulcerogenic in the gastrointestinal mucosa. These results indicate additional molecular mechanisms of analgesia and suggest the use of R-arylpropionic acids as analgesics.     

以环糊精为手性添加剂对药物对映体的毛细管电泳手性拆分

在40 mmol/L,PH值为2.5的磷酸二氢钠缓冲液中,分别以β-环糊精和HP-β-环糊精(取代度为5.5)及二者的混合物为手性添加剂对10种市售药物作了毛细管电泳分离,探讨了手性药物在环糊精中的嵌入型"包合络合作用",以及环糊精第二面上的羟基群在药物分离过程中的"边缘作用".     

Chiral influence of sex pheromonal substances on responses of the male American cockroach

Summary In order to elucidate the roles of optical enantiomers of sex pheromonal substances of the American cockroach, behavioral assays with a single enantiomer and with mixtures of enantiomers of sex pheromone mimics were carried out. Inactive enantiomers [(–)-enantiomers] had no influence on the potency of enantiomers active as sex pheromones [(+)-enantiomers]. By analysis of the results from EAG recordings with single and mixed sample of the enantiomers, it was confirmed that (–)-enantiomers did not react with the sex pheromone receptors which are responsive to (+)-enantiomers.We acknowledge technical assistance from Miss R. Kimura.     

[Co(2，6-二胺基甲基吡啶)(1，2-二胺基丙烷)Cl]ZnCl4体系配合物的合成及一异构体的晶体结构

用过氧化物法合成了 [Co(bamp) (cmen)Cl]ZnCl4(bamp =2 ,6 -二胺基甲基吡啶 ;cmen =1 ,2 -二胺基丙烷 ) ]中的两个经式异构体 ,解析了其中一个异构体阳离子的晶体结构为m1 .晶体学参数 :单斜晶系 ,空间群C2 /c,a =2 .0 1 2 0(6 )nm ,b =0 .940 8(3)nm ,c =2 .0 5 2 1 (6 )nm ,β =92 .0 45 (6 )° ,V =3.882 2(1 9)nm3,Dc =1 .786 g/cm3,Z =8,F0 0 0 =2 1 0 4,μ(MoKα) =2 7.83cm-1,R =0 .0 42 6 ,RW=0 .1 0 38.配合物离子中Co3 为六配位 .晶胞中含 4个配合物离子 ,对映体的比例为 1 :1     

HPLC法测定兔血浆中SFZ-47对映异构体浓度

建立家兔血浆中新抗炎镇痛剂 SFZ- 47[(± ) - 3H - 1 ,2 -二氢 - 2 - ( 4 -甲基苯胺基 ) -甲基 - 1 -吡咯里嗪酮 ]对映异构体浓度测定的高效液相色谱 ( HPL C)测定法 .采用反相 HPLC测定服药后血浆中 (± ) - SFZ- 47,同时收集其流出组分 .经浓缩后 ,再用 Chiral- AGP手性色谱柱进行对映异构体的直接分离 ,达到了良好的分离效果 .实验表明 ,动物体内药物动力学过程具有明显的立体选择性     

两种药物光学对映体的毛细管电泳分离研究

报道了手性药物氧氟沙星和Ｎ－异丁基－１－苯基氨基乙醇光学对映体的毛细管电泳拆分，在毛细管区带电泳模式下，采用２，６－二甲基－β－五糊精作为手性选择剂，通过考究手性选择剂浓度和背影电解质溶液ＰＨ对对映体表观工差的影响优化了分离条件，使氧氟沙星和Ｎ－异丁基－１－苯基氨基乙醇对映体成功达到基线分离。     

氟比洛芬脂质体的制备及其载药性能研究

利用薄膜蒸发-超声分散法制备氟比洛芬脂质体,通过鱼精蛋白凝聚法测定脂质体对氟比洛芬的包封率和载药率,研究了氟比洛芬脂质体载药性能的影响因素.结果表明,制得的氟比洛芬脂质体的粒径为100～250 nm,具有良好的分散性;氟比洛芬定位于脂质体的疏水基团区域,它在卵磷脂相和水相中的分配系数KD为815.6.当卵磷脂浓度为5.4×10-4mol.L-1时,所得脂质体对氟比洛芬的包封率和载药率比较理想;随着氟比洛芬与卵磷脂的质量比的增加,脂质体对氟比洛芬的载药率增大,包封率降低;胆固醇可以调节脂质体膜的稳定性,胆固醇与卵磷脂的质量比应该控制在0.3以下,过高浓度的胆固醇会大量插入膜内使得膜的刚性增强,导致脂质体对氟比洛芬的载药率和包封率降低.     

牛血清白蛋白亲和毛细管整体柱的制备及色氨酸对映体的分离

利用亲和毛细管电色谱整体柱对色氨酸对映体进行了手性拆分研究.利用溶胶-凝胶法制备了壳聚糖/硅胶复合基质毛细管整体柱,然后采用戊二醛交联柱上键合牛血清白蛋白(BSA)得到亲和毛细管整体柱,以毛细管电色谱(CEC)模式分离色氨酸对映体,考察了缓冲液pH、浓度及有机修饰剂含量对分离过程的影响.在缓冲液的浓度为20 mmol/L,pH 7.5时,色氨酸对映体分离效果良好,分离度为2.44.     

Enantioselectivity of the Musk Odor Sensation

1 Introduction Chiral recognition of substrates is one of the most characteristic phenomena of biological activity. And one of the most fundamental biological activities of chemical substances is their smell. In 1991, Linda Buck and Richard Axel~([1]) discovered a large multigene family that en codes odorant receptors, for which they were awarded the 2004 Nobel Prize in Medicine and Physiology. These odorant receptors are highly homologous, consist of ca. 320 amino acids, and show a heptah…     

铀酰-(6′-(1H-吡唑-1-硫代羰基)-[2,2′-联吡啶]-6-基)(5-甲氧基-1H-吡唑-1-基)甲硫酮对手性丙溴磷络合分离的理论研究

本文设计了一个新颖的配体:(6′-(1H-吡唑-1-硫代羰基)-[2,2′-联吡啶]-6-基)(5-甲氧基-1H-吡唑-1-基)甲硫酮,将这个配体与铀酰离子络合,构建了一个新的铀酰不对称受体。基于密度泛函理论系统研究了受体对客体R/S-丙溴磷对映体络合能力和配位选择性。结果表明铀酰受体在水和多种有机溶剂中对R/S-丙溴磷具有很好的分子识别能力和配位选择性,其对映选择性系数均超过90%。