Positron emission tomographic investigations of central muscarinic cholinergic receptors with three isomers of [76Br]BrQNP

We studied the potential of three radiobrominated isomers of BrQNP, (Z(-,-)-[⁷⁶Br]BrQNP,E(-,-)-[⁷⁶Br]BrQNP andE(-,+)-[⁷⁶Br]BrQNP), as suitable radioligands for imaging of central muscarinic cholinergic receptors in the human brain. These radioligands were stereospecifically prepared by electrophilic radiobromodestannylation of the respective tributylstannyl precursors using no-carrier-added [⁷⁶Br]BrNH₄ and peracetic acid. Preliminary pharmacological characterizations were determined by biodistribution, autoradiography, competition, displacement and metabolite studies in rats. The (-,-)-configuration presented important specific uptakes in brain muscarinic cholinergic receptor (mAChR)-rich structures and in heart, low metabolization rates and an apparent M₂ selectivity. The (-,+)-configuration revealed more rapid clearance, lower uptake, a higher metabolization rate and an apparent M₁ selectivity. Reversibility of the binding was confirmed for the three radiotracers. Positron emission tomography in the living baboon brain revealed high and rapid uptake in the brain and accumulation in the mAChR-rich structures studied. At 30 min p.i., theE(-,-)-radiotracer reached a plateau in cortex, pons and thalamus with concentrations of 29%, 24% and 19% ID/l, respectively.Z(-,-)-[⁷⁶Br]BrQNP also accumulated in these structures, reaching a maximal uptake (27% ID/l) in the cortex 2 h p.i. At 5 min p.i. a plateau (17% ID/l) was only observed in the cortex for theE(-,+)-[⁷⁶Br]BrQNP; by contrast, the other structures showed slow washout. After 3 weeks, the (-,-)-radiotracers were studied in the same baboon pretreated with dexetimide (1 mg/kg), a well-known muscarinic antagonist. In all the mAChR structures, the highly reduced uptake observed after this preloading step indicates that these radiotracers specifically bind to muscarinic receptors.Z(-,-)-[⁷⁶Br]BrQNP, which is displaced in higher amounts from M₂ mAChR-enriched structures, reveals an M₂ affinity. The two isomers having the (-,-)-configuration are potential probes for investigating central muscarinic receptors. The absolute configuration on the acetate chiral centre influences their muscarinic subtype selectivity and thecis-trans isomerism of the vinyl moiety affects their specific fixation.     

Max Brödel (1870–1941): his life and his role in the development of surgery

Summary. Max Br?del (1870–1941), from Leipzig, Germany, is often referred to in the USA as the father of modern medical illustration and mentioned in the same breath as Leonardo da Vinci or Andreas Vesal. After a classical formal art education in Leipzig he worked in Carl Ludwig's laboratory of physiology and anatomy, where he came in contact with American physicians. In 1894, the anatomist F. P. Mall convinced him to work for the recently inaugurated Johns Hopkins School of Medicine in Baltimore, where he collaborated with world-famous surgeons such as H. A. Kelly, W. S. Halsted, and H. Cushing. His illustrations were characterized by meticulous observation, both realistic and explanatory intention, technical superiority, and artistic merit. In 1911 he established the first “Department of Art as applied to Medicine”. Here, he proved to be an innovative artist, a creative scientist, and an inspiring and skillful instructor. By the time of Br?del's retirement in 1939, 160 students had graduated as medical illustrators. His pupils spread his principles and style throughout the USA and Canada, and several similar academic programs for medical illustration have been founded in these countries.      

8-Br-cAMP对肺癌NSCLC-3细胞凋亡相关基因表达的影响

目的:观察8-Br-cAMP对人肺癌NSCLC-3细胞凋亡相关基因表达的影响.方法:将体外培育的NSCLC-3细胞分为实验组和对照组,采用原位杂交方法观察8-Br-cAMP对NSCLC-3细胞c-myc、bcl-2基因表达的影响.结果:8-Br-cAMP处理后的实验组较未加8-Br-cAMP的对照组c-myc、bcl-2基因表达降低(P＜0.01).结论:8-Br-cAMP可下调与NSCLC-3细胞凋亡相关的c-myc、bcl-2基因表达.     

5—Br—PADAP光度法测定粮食中微量铜

目的：建立简便、无毒、灵敏、准确地测定粮食中微量铜的方法。方法：２－ （５－ 溴－ ２－吡啶偶氮）－ ５－ 二乙氨基苯酚（５－ ＢｒＰＡＤＡＰ）光度法。结果：铜含量在０．００～１０．００μｇ 范围内符合比尔定律,Ｙ＝ ２．３４９×１０－ ３＋ ０．０５１４８Ｘ,ｒ＝ ０．９９９９;用本法测定了６ 个样品,回收率为９０．２％ ～１０６．０％ ,平均回收率为９７．８％ ;日间重复试验（７ 次）,标准差为０．０１０７～０．０２１５ｍ ｇ／ｋｇ,相对标准偏差为０．５９％ ～１．２９％ 。结论：本法无毒、简便、灵敏,适用于粮食中微量铜的测定。     

灯台树种子萌发特性的研究

目的 研究灯台树种子萌发的最适宜条件和储藏时间，为大量人工繁殖灯台树苗木提供借鉴。方法 不同温度，不同光照时间，不同光质及不同储藏时间，测量灯台树种子的萌发率。结果 灯台树种子萌发的适宜温度为30℃～40℃，适宜的光照时间为8h，适宜的光质为黄光和日光，储藏时间为5个月以内最好。结论 灯台树种子是高温萌发型。     

牧马豆生物碱成分研究

从豆科野决明属植物牧马豆ThermopsislanceolataR.Br.的全草中分得6个生物碱。经物理常数测定及光谱分析，分别鉴定为黄华碱（Ⅰ），13-羟基黄华碱（Ⅱ），金雀花碱（Ⅲ），N-甲基金雀花碱（Ⅳ），5，6－dehydrolupanine（Ⅴ）和N－（3－氧代丁基）金雀花碱（Ⅵ）。其中化合物Ⅱ和Ⅴ为首次从该植物中分得，化合物Ⅵ为首次从本属植物中分得。     

奥替溴铵、匹维溴铵、马来酸曲美布汀和酪酸茵治疗肠易激综合征药物经济学研究

目的 初步探讨奥替溴铵（斯巴敏）、匹维溴铵（得舒特）、马来酸曲美布汀（舒丽启能）和酪酸菌（米雅BM）治疗肠易激综合征的药物经济学。方法 从中国生物医学文献数据库和学术期刊检索相关文献，选择符合标准（随机、双盲、安慰剂对照）的临床试验论文，提取临床试验数据，进行药物经济学评价。结果 服用斯巴敏40mg,tid,2wk药费71.16元；服用得舒特50mg,tid,2wk药费120.12元；服用舒丽启能200mg,tid,2wk药费110.46元；服用米雅BM80mg,tid,2wk药费282.24元。产生单位效果所需的成本分别为斯巴敏80.86；得舒特143.17；舒丽启能135.37；米雅BM351.04。以斯巴敏治疗成本最低。结论 斯巴敏是治疗肠易激综合征最优的选择。     

山楂药材HPLC指纹图谱研究

目的建立山楂药材HPLC指纹图谱,为有效控制山楂药材的质量奠定基础。方法采用HPLC法,色谱柱为AgilentTC—C18柱（250mm×4．6mm,5μm）,乙腈-0．01％甲酸水梯度洗脱,检测波长为280nm,体积流量为1．0mL／min,分析时间为120min,分析了10批山楂药材的HPLC指纹图谱。结果在选定的色谱条件下,通过相似度分析确定23个色谱峰构成山楂药材指纹图谱的特征峰。结论采用HPLC方法建立的指纹图谱具有精密、稳定、重现性好的特点,可用于山楂药材的质量控制。     

A review of the taxonomy, ethnobotany, chemistry and pharmacology of Sutherlandia frutescens (Fabaceae)

Sutherlandia frutescens (tribe Galegeae, Fabaceae), a popular plant in traditional medicine, is indigenous to South Africa, Lesotho, southern Namibia and southeastern Botswana. It is chemically, genetically and geographically extremely variable and has been divided into three subspecies and several regional forms. A second species, Sutherlandia tomentosa, is localized along the Cape coast. Sutherlandia is sometimes treated as part of the genus Lessertia. There are numerous vernacular names and a wide diversity of uses, including poor appetite, indigestion, stomach complaints, dysentery, colds, influenza, kidney conditions, fever, diabetes, internal cancers, uterine troubles, liver conditions, backache, rheumatoid arthritis, urinary tract infections, stress and anxiety, dropsy and heart failure. Notable is the use as a bitter tonic ("blood purifier"), anti-stress medication ('musa-pelo) and, at least since 1895, specifically as a cancer tonic (both as treatment and as prophylaxis). Externally it is applied to haemorrhoids, inflamed wounds and eye infections. Recent in vitro and in vivo studies have shown antiproliferative, anti-HIV, anti-diabetic, anti-inflammatory, analgesic, antibacterial, anti-stress, anticonvulsant and antithrombotic activities. Aqueous extracts often differ in activity from organic solvent extracts. The presence of high levels of free amino acids, non-protein amino acids such as canavanine and GABA, the cyclitol pinitol, flavonols and triterpenes (including SU1, a cycloartane-type triterpene saponin) provide plausible hypotheses on how these compounds, individually or collectively, may be responsible for the reputed efficacy in a wide range of ailments. Results of animal studies, as well as a phase I clinical study, have shown no indications of toxicity. Sufficient preclinical data are now available to justify controlled clinical studies.     

蒙药鹅绒藤HPLC指纹图谱研究

目的：建立蒙药鹅绒藤的高效液相色谱指纹图谱,为鹅绒藤药材鉴定以及质量标准的建立积累资料。方法：采用HPLC法,Agilent C18（250 mm×4.6 mm,5μm）色谱柱,甲醇-0.2%磷酸水溶液梯度洗脱,检测波长345nm,流速为0.8 mL/min,分析10批鹅绒藤药材的HPLC指纹图谱。结果：在选定的色谱条件下,通过相似度分析软件确定了由11个色谱峰构成的鹅绒藤的高效液相指纹图谱。结论：该分析方法稳定可靠,为蒙药鹅绒藤的质量评价与控制提供了理论依据。