去氢甲基睾丸素的合成工艺研究

目的:研究蛋白同化激素去氢甲基睾丸素的合成工艺。方法:以去氢表雄酮醋酸酯为原料,经格氏反应,水解,沃氏氧化,DDQ脱氢等四步反应制得。结果:该合成路线不仅收率高,产品纯,而且无需过柱分离。结论:该工艺路线适合工业化生产。     

米非司酮联合甲基睾丸素治疗子宫肌瘤180例疗效观察

目的观察米非司酮联合甲基睾丸素治疗子宫肌瘤的临床效果。方法 180例子宫肌瘤患者每月月经第1～3天每晚睡前服用米非司酮12.5mg;甲基睾丸素5mg/次,每天1次,连服3个月。对比用药前后彩色B型超声下子宫及肌瘤大小变化情况,对比用药前后促卵泡生成激素（FSH）、黄体生成素（LH）、孕酮（P）、雌激素（E2）、雄激素（T）、催乳激素（PRL）等血清激素变化情况,并记录不良反应。结果 165例患者子宫及肌瘤体积均明显减小,与用药前比较差异有统计学意义（P〈0.05或P〈0.01）;15例患者无明显改变,改为手术治疗。FSH、LH、E2、P水平均较用药前明显降低（P〈0.05）,且肝肾功能无明显变化,不良反应轻微。结论 米非司酮联合甲基睾丸素可明显减轻子宫肌瘤患者症状,且无明显不良反应,值得临床推广应用。     

去氢罗默碱的电合成

去氢罗默碱的电合成１）伍家泉（彼迪药业有限公司，广洲开平５２９３３１）陈虹２）陈琪瑞３）庞开圻３）（武警医学院，天津３００１６２）关键词电解还原；去氢罗默碱；阿朴菲阿朴菲类生物碱存在于某些植物中，其中许多具有抗癌、抗菌、抗帕金森氏综合征等生理作用〔１...     

甲基睾丸素用于药物流产的临床研究

目的 探讨甲基睾丸素用于药物流产的临床效果。方法 将３００例观察对象随机分为两组；每日早晚各服米非司酮２５ｍｇ，连服３ｄ，观察组同时加服甲基睾丸素１０ｍｇ，每日３次，连服３ｄ，两组于第４ｄ早晨空腹服米索前列醇０．６ｍｇ。结果 观察组完全流产率９６％，姐９０％，具有显著差异；阴道流血量观察组比对照明显减少，两组有极显著差异；阴道流血时间观察组比对照组明显缩短，两组有极显著差异。结论药物流产同时加服甲     

O-去甲基文拉法辛琥珀酸盐的合成工艺研究

目的 优化O-去甲基文拉法辛的合成工艺.方法 以对羟基苯乙酸为原料,经苄基保护,依次经过酰化、缩合、还原、氢解脱苄、成盐反应成功合成了目标化合物.结果 反应条件得到了优化,避免了使用二甲胺气体、正丁基锂和四氢锂铝试剂,总收率为30％(以对羟基苯乙酸计).结论 该路线原料价廉易得,反应条件温和,操作简便,适合于工业化生产.目标化合物经1 H-NMR、MS结构确证.     

蛋白同化激素坦波龙的合成研究

报道了蛋白同化激素坦波龙的一种新合成方法，即采用国内易得的１９－羟基－雄甾－４－烯－３，１７－二酮为原料，经七步反应合成坦波龙，并对氧化、缩合和水解等反应条件进行了研究。     

去氢骆驼蓬碱衍生物的合成和抗肿瘤活性研究

目的 合成去氢骆驼蓬碱衍生物并研究其抗肿瘤活性。方法 以去氢骆驼蓬碱为原料,在NaH催化下先用卤代烷烃对9位氮原子进行烷基化,然后用溴化苄将2位氮原子进行季铵化,得到一系列去氢骆驼蓬碱衍生物,用 MTT 法考察其对肿瘤细胞的抑制作用。结果 合成了6个新的去氢骆驼蓬碱衍生物,结构经1H-NMR、MS和红外光谱确证。与去氢骆驼蓬碱相比,所合成的化合物均有明显的抗肿瘤活性。结论 初步药理实验结果表明去氢骆驼蓬碱9-苯丙基取代能够明显提高抗肿瘤效果。     

甲基睾丸素在药物流产中的应用

近年来米非司酮及米索前列醇联合应用终止早期妊娠因其痛苦小,损伤少,使用方便而广泛应用于临床。在获得满意的流产率同时,有相当部分患者在流产后有长时间的阴道淋漓出血,个别病人即使在诊刮后仍不能有效的止血。为提高药物流产成功率,解决药物流产后出血量多,持续时间长的问题。我院于1999年3月至12月给门诊自愿药物流产者早孕妇女50例服用甲基睾丸素,并与对照组50例对比,效果满意,现报道如下：     

甲基睾丸素及其它甾体的HPLC测定

以ＨＰＬＣ法测定甲基睾丸素及其它甾体，采用Ｓｈｉｍ－Ｐａｃｋ ＯＤＳ柱，甲醇－水（７２：２８）为流动相，炔诺酮为内标，检测波长为２４１或２５４ｎｍ。与ＴＬＣ、ＵＶ法相比，本法简便、准确、可靠、重现性好。     

6,7—去氢托品的一种新合成法

用６β－羟基托品酮为起始原料，经８步反应合成了东莨菪碱全合成关键中间体－－６，７－去氢托品，总产率达３５．８％。     

Synthesis and properties of human γ-lipotropin

The synthesis of human γ-lipotropin by the solid-phase method is described. The synthetic product was characterized by R_f in partition chromatography on Sephadex G-50, paper electrophoresis, polyacrylamide gel electrophoresis, thin-layer chromatography, HPLC, end group determination, peptide mapping of a tryptic digest, and amino acid analyses of acid and enzymic digests. The synthetic material is identical to natural human γ-lipotropin when assayed against natural human β-lipotropin for lipolytic activity.     

Age–Dependent Effects of Ethanol on Central Monoamine Synthesis in the Male Rat

Abstract: In the present study, the effect of ethanol on central monoamine synthesis in developing and adult male rats was studied by measuring the accumulation of DOPA and 5–hydrotryptophan after inhibition of aromatic amino acid decarboxylase. Before adolescence, ethanol caused a decrease of DOPA accumulation in the whole rat brain, while after adolescence ethanol increased the DOPA synthesis. Ethanol had no effect on the serotonin synthesis at any of the ages studied. It is suggested that hormonal events occuring during puberty may be of importance for the stimulatory properties of ethanol observed at adult age     

Synthesis of 17O isotope labeled Leu-enkephalin and 17O n.m.r.*

Oxygen-17 isotope was introduced into the α-carboxyl group of glycine, 1-phenylalanine, 1-leucine and 1-tyrosine by acid catalyzed exchange of ¹⁷O from H₂¹⁷O or by acid hydrolysis of respective amino acid methyl esters in H₂¹⁷O. Quantitative enrichment of glycine was achieved by acid hydrolysis of amino acetonitrile in H₂¹⁷O. For α-amino protection in amino acids t-butoxycarbonyl (Boc) group was employed for ¹⁷O labeled enkephalin synthesis. Five analogues of Leu-enkephalins (I–V) labeled with ¹⁷O at different amino acid residues were synthesized by solid phase method. ¹⁷O n.m.r. spectra were measured at 24.4 and 67.8 MHz for Leu-enkephalins ¹⁷O labeled at Gly² and Phe⁴ positions. A downfield shift was observed for ¹⁷O labeled Gly² Leu-enkephalin upon heating. This shift is indicative of the rupture of intramolecular hydrogen bonds. The preliminary results confirm the hypothesis that an intramolecular hydrogen bond exists between the carbonyl group of Gly² and NH group of Leu⁵.     

Qualitative and Semiquantitative Analysis of Doping Products Seized at the Swiss Border

Background: Substances developed for therapeutic use are also known to be misused by athletes as doping agents and, outside of regulated sport, for image-enhancement. This has generated a market for counterfeit doping substances. Counterfeit doping agents may be of poor pharmaceutical quality and therefore constitute health risks to consumers. Objectives: This study aims to investigate the pharmaceutical quality of 1,190 doping products seized at the Swiss border. Methods: Swiss customs authorities seize incoming shipments potentially containing doping agents. Qualitative and semiquantitative analyses were performed in order to test for prohibited doping substances. The main analytical methods utilized for characterizing confiscated compounds were liquid chromatography-high resolution mass spectrometry, polyacrylamide gel electrophoresis with subsequent in-gel tryptic digestion and identification of peptidic compounds using nanoliquid chromatography-tandem mass spectrometry, and electrochemiluminescence immuno assay. Results: For 889 (75%) of the analyzed products, the label suggested the content of anabolic agents, for 146 samples (12%) peptide hormones or growth factors, and for 113 items (9%) antiestrogens, aromatase inhibitors or other metabolic modulators. For the majority of the investigated products, the pharmaceutical quality was an unsatisfactory standard: nonapproved substances were detected and less than 20% of the products contained the claimed substance in the respective amount. Conclusion: A comprehensive sample of confiscated doping products was analyzed, allowing for monitoring of developments regarding the use of doping substances in Switzerland and for anticipating future trends and challenges in sports drug testing. An alarming number of tested products was of substandard pharmaceutical quality.     

度他雄胺的合成工艺

目的制备度他雄胺。方法孕烯酮醇经过酯化、氧化（沃氏反应）、水解得孕烯酮酸,再经过氧化开环、环合、还原、氧化、酰基化共八步制得目标产物。结果最终产物由核磁共振谱和元素分析进行结构鉴定。总收率为31.5%。结论探索了不同条件对各个合成中间体的产率的影响,找出合适的反应条件,使之更适于工业生产。     

6-去氢诺龙醋酸酯的合成

目的 以相对廉价的19-去甲-4-雄烯二酮为起始原料合成6-去氢诺龙醋酸酯。方法 经醚化、还原、双酯化和脱氢4个操作步骤合成目标化合物。结果 革除文献中用到的有毒溶剂苯，以硼氢化钾替代了价格贵且易潮解的硼氢化钠，降低了成本；用亚硫酸氢钠破坏反应中过剩的N-溴代丁二酰亚胺（NBs），从而提高了产品质量；总收率为51％。结论 用该方法合成6-去氢诺龙醋酸酯，收率高，成本低，适宜于工业化生产。     

正交试验设计在17α-羟基-21-碘黄体酮合成工艺改进中的应用

目的:以羟基黄体酮和一氯化碘为原料,合成17α-羟基-21-碘黄体酮。方法:设计正交试验考察溶剂体系、反应温度及原料配比对反应结果的影响,得到优化反应条件。结果:通过新的合成方法合成了目标产物。结论:最佳反应条件为:反应溶剂为水、反应温度为0~5℃、羟基黄体酮与一氯化碘摩尔比为1.0:1.0,粗品精制后收率98%以上。     

Effect of methandrostenolone on liver morphology and enzymatic activity

The action of different doses and time of metandrostenolone administration on liver morphology and activity of the enzymes of blood serum, liver and pancreatic tissue was studied in experiments on male rats. It was established that metandrostenolone regardless of its dose and time of administration produces changes in enzymatic activity and in morphological characteristics, manifesting in hypertrophy of hepatocytes in modification of the cell size of the reticuloendothelium as well as in the magnitude and amount of nucleoli in the nucleus. The changes also involve impaired rhythmicity of RNA and glycogen synthesis by the liver.     

吗氯贝胺的合成

以对氯苯甲酰氯为起始原料，与Ｎ－（２－氨乙基）吗啉综合制得吗氯贝胺，收率：７４．５％。