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。     

Pentasomy X: Report of patient and studies of X-inactivation

A five-year-old girl presented with mental retardation (MR), microcephaly, short stature, ptosis, malocclusion, abnormal elbows, fifth finger clinodactyly, joint hyperextensibility in hands and feet, renal hypoplasia, nonobstructive ureteral stasis, pyelonephritis, and renal failure. Five X chromosomes (49,XXXXX) were found in all peripheral blood lymphocytes and skin fibroblasts examined. X^a RBC typing, utilizing serial dilutions of antiserum, gave agglutination at a higher titer than in either Xg(a+) positive parent; the patient's serum IgM was also elevated. These immunological findings imply a lack of dosage compensation and incomplete inactivation of some X-linked loci.     

Effects of fenfluramine on sleep-wakefulness in cats

Five cats were prepared with chronically implanted electrodes for recording sleep-wakefulness patterns. Four of these animals received fenfluramine at each of three dose levels and data was recorded for the following 12 hours. Percent of time in paradoxical sleep was significantly reduced by 2.5 and 7.5 mg/kg, but not by 0.5 mg/kg, of fenfluramine. The higher doses also increased slow-wave sleep and, at 7.5 mg/kg (an anorexigenic dose), total sleep time was significantly increased. Under similar conditions amphetamine, at an anorexigenic dose of 1 mg/kg, significantly suppressed both paradoxical sleep and slow-wave sleep in three cats.Rebound of paradoxical sleep after suppression induced by 2.5 mg/kg of fenfluramine was not seen in either of two cats studied when sleep patterns were recorded for 48 hours. After 7.5 mg/kg of the drug, however, rebound was seen on days 3 and 4 after suppression of paradoxical sleep which lasted for over 26 hours. In two animals, daily administration of 2.5 mg/kg of fenfluramine for 16 consecutive days, followed by saline administration for three days, indicated that tolerance was developing to the suppression of paradoxical sleep produced by the drug.     

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.