苦木双碱甲和苦木双碱乙的结构

自苦木科(Simaroubaceae)植物苦木(Picrasma quassioides(D.Don.)Benn.)的木质部的乙醇提取物中经硅胶和氧化铝柱层析分离得到两个新β-咔巴啉二聚体生物碱,分别命名为苦木双碱甲(kumujansine)和苦木双碱乙(kumujantine),经光谱(UV,IR,~1H-NMR,~(13)C-NMR,2D-NMR和MS)分析确定结构分别为式Ⅰ和Ⅱ。     

化学模式识别评价中药威灵仙质量的研究

本文按威灵仙所含化学成分对6个种、16个产地的21个样品进行了气相色谱分析;以抗炎药理活性作为评价质量的指标,将样品分为有抗炎作用和无抗炎作用两大类,一部分作训练集,一部分作试验集;用SIMCA选择特征并分类,再用PCA将选择的特征数据在二维平面上显示;根据分类和显示的结果,可以区分威灵仙样品有无抗炎作用即质量的优劣。     

化学—酶法立体控制合成光学纯3-(2-吡啶基)丙氨酸的新方法

A new chemoenzymatic synthesis of optically pure 3-(2-pyridyl)alanine (IV)was established ,which comprised the stereocontrolled amination of olefinic bond in compound 3-(2pyridyl)acrylic acid(III)catalyzed by L-phenylalanine ammonialyase(PAL, EC 4.3.1.5)con-tained in Rhodotorula rubra mycelium. Compound III was prepared chemically from 1,1,1-trichloro-2hydroxy-3-(2-pyrdyl)propane(II) which was formed by addition of chloral to α-picoline(I).Theenzymatic amination of compound IIl was completed in aqueous ammonia solution(6.4 mol/L,pH10.5, 30℃)with the conversion of 60%,The preduct IV was separated ftom the unconverted III bysilica gel dry column chromatography and further purified by non-polar resin(CGA-688 )columnchromatography.The specific rotation [α]_D²⁴=36.25°(c 0.250, H₂O).     

催醒安在大鼠尿内代谢产物的研究

催醒安是一种新的中枢性抗胆碱酯酶药。给大鼠灌胃后,用HPLC分离纯化尿提取液中的代谢产物,得到四个组分。经MS鉴定分别为原形药物,N-羟甲基,N-甲基氨基甲酸-[间-(2-二甲氨基)]乙氧基苯酯(简称羟基化催醒安),N-甲基氨基甲酸-[间-(2-二甲氨基)乙氧基]苯酯(去甲基催醒安)及间-(2-二甲氨基)乙氧基苯酚(催醒安水解物)。原药及产物对电鳐乙酰胆碱酯酶抑制率的实验表明,去甲基催醒安抑酶活性与原药相近,羟基化催醒安活性比原药低,水解物无抑酶活性。     

Percutaneous excimer-laser and excimer-laser-assisted angioplasty of the lower extremities: results of initial clinical trial

Percutaneous peripheral excimer-laser angioplasty at 308 nm was used for treatment of 30 patients with peripheral vascular disease. Twenty-eight patients underwent laser-assisted balloon angioplasty, and two patients underwent laser angioplasty alone. Acute angiographic and clinical success was achieved in 24 of 31 (77%) femoropopliteal stenoses and occlusions. Seven of nine (78%) stenoses, six of seven (86%) short (0-5 cm) occlusions, seven of eight (88%) medium-length (6-10 cm) occlusions, three of four (75%) long (11-15 cm) occlusions, and one of three (33%) extreme (greater than 15 cm) occlusions were successfully treated. Inability to treat total occlusions was in each case related to a failure to maintain coaxial position and subintimal passage of the fiber. These cases demonstrate the feasibility of safely performing percutaneous peripheral excimer-laser or excimer-laser-assisted angioplasty. The overall frequency of restenosis after a mean follow-up period of 9.1 months was 29%. The data suggest that these procedures may be useful for the treatment of peripheral vascular disease in selected patients.