Chemical and enzymatic treatment of endothelin

Endothelin-1 (ET), the most potent vasoconstrictor yet discovered, is a peptide containirig 21 amino acids with two intrachain disulfide bridges. With the aim of obtaining two-chain derivatives, Et was submitted to chemical and enzymatic treatments. Reaction of ET with CNBr in 70% HCOOH gave, in addition to the expected [Hse⁷ lactone]-7,8-seco-ET and unreacted material, a by-product whose molecular weight was 25 m.u. greater than that of ET. When the reaction mixture, after lyophilisation, was immediately quenched with NH3-saturated dry MeOH, two products could be recovered in a 5:1 ratio, both obtained by nucleophilic attack of the homoserine lactone: the expected [Hse⁷-NH₂]-7,8-seco-ET and [Hse⁷]ET, resulting from competitive intramolecular reaction of the deprotonated α-amino group of the Asp⁸ residue. The Lys⁹-Glu¹⁰ bond turned out to be very resistant to enzymatic attack both by Lys-C-endopeptidase and trypsin. The 9,10-seco-ET derivative could be obtained by treatment with Lys-C-endopeptidase only by using a high enzyme/ET ratio and after a prolonged incubation time. Cleavage of the Lys⁹-Glu¹⁰ bond could not be achieved by treatment with trypsin, even with a high enzyme/substrate ratio. The main product was 13, 14-seco-ET, deriving from the action of chymotripsin (present as an impurity in the trypsin preparation) on Tyr¹³. The structure of these peptides was confirmed by amino-acid sequence analysis and fast atom bombardment mass spectrometry (FAB-MS). Nicking of the ET structure at different positions had different impact on the biological properties of the resulting derivatives. © Munksgaard 1995.     

健康教育与大众媒体互动合作机制的定性研究

目的了解大众媒体报道艾滋病的现状，探索大众媒体与健康教育机构之间的互动合作模式。方法以艾滋病的宣传报道为切入点，对15名从事艾滋病宣传报道的负责人或记者进行个人深入访谈。结果影响大众媒体与健康教育机构之间合作的因素主要是资金、观念与机制。大众媒体与健康教育机构之间合作的最佳方式是相互理解、优势互补，建立健全双方长期、定时的信息交流机制和良好的互动合作机制，前者提供宣传平台，后者提供健康信息。结论大众媒体与健康教育机构之阃的合作既有基础，又有必要。加强两者的合作，将是一项双赢的策略。     

川芎挥发油化学成分研究

采取闪蒸气相毛细管色谱法和气相毛细管色谱—质谱法研究了宁夏六盘山区产川芎的挥发油化学成分,色谱分离出50多个峰,质谱鉴定了24个成分,主要是川芎酜内酯(46.37％)、丁基酞内酯(13.87％)、新蛇床内酯(6.98％)和丁烯基酜酯(4.8％)。红外光谱图中有较强的内酯特征吸收峰,为质谱所鉴定的以上主要成分提供了佐证。将闪蒸气相色谱法与蒸气蒸馏提取气相色谱法进行对照,二者的色谱图基本相符,前者是分析天然产物挥发性成分更加简便、迅速的微量方法。     

四逆汤煎煮过程中乌头类生物碱的溶出和水解平衡

目的 研究四逆汤中乌头类生物碱的溶出平衡和水解平衡。方法 利用电喷雾质谱分析，比较了制附子、四逆汤、四逆汤药渣和含有3种双酯型生物碱的混合对照品体系中的乌头碱类二萜生物碱。结果 在煎煮过程中双酯型生物碱溶解并发生水解反应，而脂类生物碱则难溶于水。乌头碱、中乌头碱、次乌头碱水溶性相近，但是次乌头碱在水中的热稳定性更高，C19二萜骨架上C3取代基(—OH或—H)的变化影响生物碱的稳定性。结论四逆汤中的乌头碱类生物碱的种类及含量由其溶解性和化学稳定性共同决定。     

血液透析中尿毒素两室模型实验验证的研究

为了揭示血液透析过程中溶质在体液中的传递规律，我们制做了尿毒症实验动物犬模型进行血液透析实验，采用肌肉活体组织活检测定组织细胞内尿素氮（BUN）和肌酐（Cr）的浓度，同时取血样测定其血浆水平，发现组织细胞内BUN和Cr的浓度与其血浆浓度随时间变化具有明显的差异。因此，从实验上直接证实了人体体液两室模型理论的假设，提示人体细胞内代谢物质的传递与排他是不均一的，细胞内的物质进入血液需要克服一定的传质阻力。实验结果为合理地评价透析的充分性提供了理论根据。     

Gadolinium ring enhancement and mass effect in acute disseminated encephalomyelitis

A 9-year-old boy presented with a subacute history of optic neuritis followed by brainstem involvement, with fever and a lymphocytic pleocytosis in the cerebrospinal fluid. Gadolinium-enhancing ring lesions were demonstrate in the white matter of the cerebrum, brainstem and cerebellum on day 17 of the illness, all appearing simultaneously as part of a monophasic illness. A parietal lesion exerted mass effect. Needling and biopsy yielded no evidence of a pyogenic lesion, tumour or tuberculosis and showed vasculitis. There was insufficient material for myelin staining. Dexamethasone therapy lead to rapid improvement of the radiological lesions: MRI and CT on day 34 of the illness showed complete clearing of the lesions except for residual abnormality at the biopsy site.     

一阶导数光谱法测定丙吡胺尿药浓度及其缓释片的相对生物利用度

本文报道了用导数光谱法测定磷酸丙吡胺的尿药浓度,本方法能消除尿中杂质干扰,测定结果准确。6名受试者交叉口服磷酸丙吡胺缓释片和普通片,测得尿药浓度计算消除速度常数K,排泄速率(Δx/Δt)_(max) 所需时间,证明缓稀片药物排泄慢,药效维持时间长,且缓释片的相对生物利用度与普通片基本相同。     

Orthogonal solid-phase synthesis of a monobiotinylated analog of Neuropeptide Y

Analogs of Neuropeptide Y (NPY) were synthesized with conventional Boc/benzyl protective group strategy. Instead of Asn⁷ in the native scquence, Boc-Lys(Alloc)-OH was incorporated. At the end of the synthesis the Alloc group was selectively removed by palladium-catalyzed hydrostannolysis and biotin coupled to the e-amino group of Lys⁷. After cleavage and characterization with plasma desorption mass spectrometry the N^e-7-biotinyl-[Lys⁷]-NPY and the nonbiotinylated analog [Lys⁷]-NPY were investigated as ligands to the NPY receptor from rat cerebral cortex. Both analogs were found to be high affinity ligands to the NPY receptor and bound with essentially the same affinity as unmodified NPY.     

易误诊为神经肿瘤的一种疾病——肿块型中枢神经系统原发性血管炎

背景与目的：由于缺乏特异性临床和影像表现，肿块型中枢神经系统原发性血管炎（primary angiitris of central nervous system，PACNS）常被误诊为胶质瘤．本文旨在探讨肿块型PACNS的诊断与鉴别诊断。方法：回顾性分析手术治疗的37例肿块型PACNS患者的临床及影像表现。结果：85．3％的患者出现局灶性神经功能减退，55．9％患者有不同程度皮层高级功能减退症状。70．6％的颅内病变累及脑皮层：73．5％患者的正常区域脑血管周围间隙增宽，其中76％出现血管强化；病变出现特征性的“C”形强化。结论：局灶性神经功能和高级功能减退、病变累及皮层和“C”形强化等特征．有助于诊断肿块型PACNS。     

城市污灌废水的致突变性检测及色谱/质谱分析

应用Ames致突变试验,对比研究了武汉市易家墩、黄孝河污灌区污灌废水与土壤的致突变性。同时应用色谱/质谱(GC/MS)分析技术。测定了主要污水中有机污染物的化学组成。结果表明:罗家渠废水的致突变活性最强;受各条污水灌溉的土壤的致突变活性顺序与相应废水的强弱顺序一致;罗家渠废水中致突变致癌物主要是萘、联苯等。