刺果甘草化学成分的研究

从刺果甘草(Glycyrrhiza pallidiflora Maxim)的根和根茎中分离到五种化合物,经理化性质和光谱方法鉴定,化合物P-2为4-羟基-2,4’-二甲氧基查尔酮,为一新的化合物,命名为刺果甘草查尔酮(glypallichalcone,P-2)。其它分别为4'-O-methyl-coumestrol(P-1),谷氨酸乙酰化物(N-acetylglutamicacid,P-3)和芒柄花素(formononetin,P-4),均为首次从该植物中获得。此外还得到β-谷甾醇(β-sitos-terol,P-5)     

朝藿素D的分离和结构

从朝鲜淫羊藿(Epimedium koreanum)地上部分分离得到一新黄酮成分(I)和一已知化合物(II)。经光谱解析,证明I的结构为5,7,3',4'-tetrahydroxy-5'-prenylflavone,命名为朝藿素D(epimedokoreanin D);II为2-hydroxy-3,4,6,7-tetramethoxy-9,10-dihydrophenanthren。     

Tryptophan reduction and histidine racemization during deprotection by catalytic transfer hydrogenation of an analog of the luteinizing hormone releasing factor

(d -Trp)⁶-LHRH:pGlu-His-Trp-Ser-Tyr-d -Trp-Leu-Arg-Pro-GlyNH₂ was prepared by solid-phase peptide synthesis using the nitro group to protect the guanidine side chain of the arginyl residue. Removal of the side-chain protecting groups was carried out by catalytic transfer hydrogenation (CTH) using palladium acetate/ammonium formate or palladium on charcoal/formic acid. We show in this paper that this deprotection method induces i) reduction of the tryptophan residue and ii) epimerization at the histidine level (with palladium acetate/ammonium formate). Despite the formation of significant amounts of reduced peptide. CTH enabled us to obtain (d -Trp)⁶-LHRH in relatively good yield.     

URINARY EXCRETION OF TITRATABLE ACID AND ITS RELATIONSHIP TO URINARY pH AND INORGANIC PHOSPHORUS EXCRETION

The relationship between urinary pH, titratable acid (T.A.) and inorganic phosphorus (I.P.) excretion was examined in a group of 81 hospital out-patients and some normal volunteers, who presented for one-day renal function testing. Although the patients had a variety of renal diseases, with glomerular filtration rates ranging from 7 to 146 ml. per minute per 1·73 sq. m., a strictly linear relationship was found between the “ratio of urinary T.A. over urinary I.P.” and urinary pH, expressed by the following equation: urinary T.A./urinary I.P. = 4·2409-0·5678 × urinary pH. From this relationship it was deduced that abnormalities of urinary T.A. excretion in these patients were mainly dependent on abnormalities of either urinary I.P. excretion, or urinary pH, or both. For any given level of urinary pH, variations in urinary T.A. excretion were caused mainly by variations in urinary I.P. excretion. The theoretically derived sigmoid titration curve of a buffer with a pK′ of 7·20 most closely fitted the experimentally determined regression line, especially between urinary pH values of 6·0 and 8·0 units ; this was consistent with the behaviour of phosphoric acid at 25° C., the temperature of titration. The standard error of the method for deriving urinary I.P. excretion from urinary pH and urinary T.A. excretion measured titrimetrically was 5% ; and this was considered sufficient to allow its use in clinical biochemistry as a screening procedure for urinary I.P. excretion, as part of a one-day renal function testing system.     

3-甲基芬太尼立体异构体的合成、绝对构型和镇痛活性

报道3-甲基芬太尼(2)四个光学异构体的合成及其绝对构型的确定,并测定了各异构体的镇痛活性(小鼠,ip,热板法)。结果表明,cis-(+)-(3R,4S)-2的镇痛作用最强,ED_(50)0.00767 mg/kg,镇痛效能是吗啡的2600倍,比其对映体cis-(-)-(3S,4R)-2以及混旋的cis-(±)-2分别强119和1.5倍;trans-(+)-(3S,4S)-2的镇痛效能是吗啡的450倍、trans-(-)-(3R,4R)-2的4倍。     

佳贝和欧可芬滴眼液在白内障手术中应用的研究

目的：评价佳贝和欧可芬滴眼液在白内障术中维持瞳孔散大及术后抗炎作用疗效。胡机分组（佳贝组、欧可芬组和对照组）研究８６名白内障患者术前应用两种药物后,白内障术中瞳孔大小的改变以及对卡米可林（氨甲酰胆碱,Ｃａｒｂａｃｏｌ）缩瞳作用的影响;以地塞米松滴眼液为对照,研究应用两种滴眼液对术后角膜后ＫＰ和房水混浊度的影响,以及对术眼眼压的影响。结果：与对照组相比,佳贝和欧可芬都能有效抑制术中的瞳孔缩小（Ｐ〈０     

卡托普利对大鼠t-PA和PAI-1活性的作用

目的评价卡托普利对大鼠血浆t-PA和PAI-1活性水平的影响。方法给大鼠应用三种剂量的卡托普利,观察其对大鼠血浆t-PA和PAI-1活性水平的作用。结果卡托普利治疗后使大鼠血浆t-PA活性升高,PAI-1活性及PAI-1/t-PA活性比值显著降低,这种作用呈某种程度的剂量依赖性。结论卡托普利能增强大鼠纤溶系统的活性,这种作用呈某种程度的剂量依赖性。