X-Ray Structure and Crystal Lattice Interactions of the Taxol Side-Chain Methyl Ester

A colorless, parallelepiped crystal of methyl (2R,3S)-N-benzoyl-3-phenylisoserinate belonging to the space group P2_l with a = 5.414(4), b = 7.813(1), c = 17.802(7) , = 90.87(4)°, Z = 2, V = 752.9 ³, D _calc = 1.32 g cm^–3, and µ_calc = 1.02 cm^–1 was selected and the structure solved using direct methods. Refinement led to a final R = 0.079 for 819 [F _o 5(F_o)] reflections. Intermolecular hydrogen-bonding interactions are prevalent in the crystal lattice of this compound.     

Study of the substructure of the Morgagni and Brunescens cataract with the TAO non-coating technique

Lens tissue from a Morgagni cataract was examined by SEM and TEM. For SEM, after prefixation with glutaraldehyde and postfixation with the tannic acid/arginine/OsO₄ non-coating (TAO) technique, and for TEM, after prefixation with glutaraldehyde, postfixation with OsO₄/K₄Fe(CN)₆ and poststaining with uranyl acetate/lead citrate. The TAO technique seems to be a particularly suitable postfixation method for the SEM investigation of cararact tissue because of the presence of the protein structures present. The cortical region showed areas of radially, instead of concentrically, arranged lens fibres, degenerated lens fibres with holes (vacuoles), broken ball and socket connections between the lens fibres, and oval or spherical structures varying in size from 0.5–20 m, the largest resembling a golfball, arising from the cytoplasm of degenerating lens fibres. The smallest, 0.2–0.5 m, appear to have been expelled from the furrowed lens epithelium.     

The Structure of Celiprolol

The crystal structure and nuclear magnetic resonance (NMR) spectra and assignments of celiprolol, N-[3-acetyl-4[3-[N-t-butylamino-2-hydroxypropoxy]phenyl]-N, N-diethylurea, are reported. Celiprolol crystallizes in the monoclinic space group, P2_l/a, with a = 9.081(2), b = 13.800(4), and c = 17.471(5) Å and = 95.04(2)°. Structure was solved by direct methods; structure refinement to R of 0.058. Intermolecular hydrogen-bonding in the crystal is discussed. The ¹H, ¹³C, and two-dimensional (2D) NMR spectra of the hydrochloride have been obtained and definitive signal assignments made.     

Quantified ultrastructural study of spermatozoa in unexplained failure of in vitro fertilization

Failure of in vitro fertilization or very low cleavage rates may occur even though oocyte and semen parameters seem satisfactory. Quantified ultrastructural study of spermatozoa was performed in such cases of failure (n =6) or low cleavage rate (<20%; n =4). Through 1 to 11 retrievals, the number of inseminated oocytes ranged from 14 to 145. The results were compared to those of six fertile men. Quantification was achieved by cataloguing cell defects of the spermatozoon heads and mid-/principal pieces of the flagella. Using the data from each specimen, the percentages of total cellular abnormalities in the head/mid-/principal pieces were established. At the level of the head overall percentages for six groups of defects were determined. The overall percentage of combined head abnormalities, defined as the presence of at least three of these six defects on the same spermatozoon head, was established. Statistical differences among control and patient groups were analyzed by nonparametric Mann—Whitney Utest. The percentages of anomalies of the midpiece and of the principal piece were not significantly different between patients and controls. Motility assessed by spermogram was considered functionally uncompromised. In eight patients the percentage of cell alterations of the head (93–100 vs 77.3 ± 6.4%) and the percentage of combined anomalies of the head (78.1–100 vs 60.8 ± 8.5%) were significantly different between patients and controls. In two cases, the percentages established for all head parameters considered were not globally different from those observed in controls. Thus in 8 cases of 10, electron microscopy with quantified analysis supplied valuable evidence about the poor quality of these sperm samples judged as normal under light microscopy and may provide an explanation for their impaired fertilizability. In the two other cases the fact that the sperm appeared to be ultrastructurally normal does not rule out functional sperm pathology. Alternatively, defects in the oocyte may also account for unexplained failures of in vitro fertilization.     

藏药花锚中新化学成分的鉴定

目的 分离并鉴定高原植物椭圆叶花锚Halenia elliptica全草中的化学成分。方法 采用元素分析（EA），核磁共振波谱（NMR），质谱（MS），红外光谱（IR），紫外光谱（UV），差示扫描量热（DSC）等分析方法，测定其理化常数和波谱数据，鉴定其化学结构，结果 确证从椭圆叶花锚中所得到的两种针状结晶化合物，分别为1-羟基-3，7，8-三甲氧基Shan酮（1-hydroxy-3,7,8-trimethoxyxanthone)和1，7-二羟基-3，8-二甲氧基Shan酮（1，7-dihydroxy-3,8-dimethoxyxanthone)。结论 上述两种Shan酮衍生物为首次从藏药花锚中分离得到。     

甘肃产香青挥发油成分分析

香青 Anaphalis sinica Hance是菊科香青属中的一种 ,主产于我国北部、中部、东部及南部 ,生长于低山或高山灌丛、草地、山坡和溪岸 ,朝鲜和日本也有分布[1] 。全草入药 ,具有平喘、镇咳、祛痰、消炎等作用 [2 ] ,但对其化学成分及挥发油成分的研究未见报道。本研究采用水蒸汽蒸馏法提取香青挥发油并通过气相色谱 /质谱联用技术对其成分进行分析鉴定。1　仪器与材料HP6890 / 5 973GC- MS仪 ,HP- 5 MS( 30 m×0 .2 5 mm× 0 .2 5μm) (美国 HP公司 ) ,香青于 2 0 0 0年 9月采自甘肃省兰州地区石佛沟 ,由张永红博士鉴定为香青属植物香青…     

活血益气药不同剂量配伍对心梗后心衰大鼠心脏系数及功能的影响

目的 :观察相同种类活血益气药的不同剂量配伍对心梗后心衰大鼠心脏系数、功能的影响。方法 :采用左冠脉结扎术致心梗后心衰大鼠模型 ,分别用活血益气方 (全方活血药量占全方 75% )、益气活血方 (活血药量占全方25% )、气血方 (活血药量占全方 50%)于术后 4周给药至 8周 ,每日灌胃 ,以卡托普利作为阳性药。用阻抗法观察给药前后大鼠心脏功能、心脏系数的变化。结果 :心梗后心衰大鼠经 4周给药治疗后 ,心功能每搏输出量 (SV)、心输出量 (CO)、心脏指数 (CI)值都明显升高 (P<0.01) ;同时 ,活血益气方 (活血药量占全方 75 % )、气血方 (活血药量占全方50% )对模型动物治疗后心脏系数改善与假手术组相似 (P>0.05) ,而益气活血方 (活血药量占全方 25% )、卡托普利与假手术组比较 ,对其无改善 (P<0.01)。结论 :活血益气药通过改善心梗后心衰模型大鼠心脏系数及功能 ,达到治疗心衰作用 ;同时 ,方剂配伍中多量活血药的应用 (活血药 /益气药为 75%和 50%)可以较明显改善心衰大鼠的组织学指标心脏系数。     

重组人甲状旁腺激素1-34的氨基酸组成分析

分析重组人甲状旁腺激素 1-3 4的氨基酸组成 ,为该品种的结构鉴定提供依据。水解条件含 1%苯酚的6mol L盐酸 ,10 5℃水解 2 4h ;衍生方法异硫氰酸苯酯 (PITC)柱前衍生法 ;氨基酸测定色谱条件色谱柱为PhenomenexprodigyODS 10 0A。 (4 .6mm× 2 5cm ,5 μm) ;流动相A为 0 .1mol L醋酸钠 (pH6.5 ) -乙腈 (93 :7) ,B为水 -乙腈 (1:4) ;二元梯度洗脱 ;检测波长为 2 5 4nm ;流速为 1ml min ;柱温为 40℃。结果 :实验值与理论值一致 ,偏差小于 10 %。本法准确、可靠、重现性好 ,可用于该产品的质量控制。     

阳离子抗菌肽研究进展

阳离子抗菌肽广泛分布于多种生物 ,越来越多的证据表明它们在机体天然免疫中有着重要的作用。广谱抗菌、抗病毒、抗肿瘤细胞及其它特性也使得其具有潜在的医药价值。对抗菌肽的研究正不断深入。该文从一般性质、作用机制、构效关系、重组表达、应用价值、存在的问题与发展方向等方面 ,对阳离子抗菌肽的最新研究进展进行综述     

多肽药物分析方法研究进展

介绍多肽药物的生物活性分析、结构分析、纯度分析的发展状况。