共查询到17条相似文献,搜索用时 109 毫秒
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目的: 研究药物米非司酮中的杂质。方法: 运用硅胶柱层析和半制备高效液相进行分离和纯化,其结构通过NMR和HREIMS等技术进行鉴定。结果: 从母液中分离得到3个化合物,其结构分别鉴定为17β-羟基-17α-(1-丙炔基)-雌甾-5, 9-二烯-3-酮环缩乙二醇(Ⅰ),11-[4-(二甲基氨基)苯基]-17β-羟基-17α-(1-丙炔基)-雌甾-5, 9-二烯-3-酮环缩乙二醇(Ⅱ),11-[4-(二甲基氨基)苯基]-17β-羟基-17α-(1-丙炔基)-雌甾-4, 10, 11-三烯-3-酮(Ⅲ)。结论: 3个杂质均为首次从药物米非司酮中确定,其中Ⅱ为新化合物。 相似文献
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以19-羟基雄甾-4-烯-3,17-二酮(1)为先导物,经4β,5β-环氧化得8,然后4-位,引入取代基如羟基、氯、溴及乙酰硫基(2、3、4及5)。并用HPLC法测定其对人胎盘微粒体睾丸素A环芳香化酶的相对抑制活性,结果表明3活性较强。 相似文献
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仙人掌中一个新α-吡喃酮成分的分离与结构鉴定 总被引:2,自引:0,他引:2
目的 研究仙人掌的化学成分。方法 应用多种柱色谱方法进行分离和纯化 ,NMR和MS等波谱解析化学结构。结果 从仙人掌肉质茎的乙醇提取物中分离出 6个化合物 ,其结构分别鉴定为 :3 O 甲基异鼠李黄素 (1)、4 乙氧基 6 羟甲基 α 吡喃酮 (2 )、正十七醇 (3)、香草酸 (4)、异鼠李黄素 3 O 鼠李糖苷 (5 )和芦丁 (6 )。结论 化合物2为新化合物 ,化合物 1、3、4、5均为首次从本属植物中分离得到 ,化合物 6为本植物首次分离得到。 相似文献
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米非司酮(mifepristone,RU486),是八十年代初法国Roussel-Uclaf公司首次合成的甾体化合物,“七·五”期间我国亦成功地合成了,它具有抗孕激素和抗肾上腺皮质激素的作用,在靶细胞上竞争性地抑制孕激素、黄体期和妊娠期的激素,目前主要作为避孕药物进行研究。 近来报告早孕时如以米非司酮与前列腺素类似物联合使用,可使流产成功率达90%以上,且作用专一、使用方便、副作用小,该药的研制成功是抗生育药物研究领域的显著进展之一。 相似文献
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孕烯醇酮乙酸酯经溴仿反应、酯化、沃氏氧化得到非那雄胺的关键中间体3-酮基-4-雄甾烯-17β-羧酸甲酯,其中沃氏氧化用邻硝基苯甲醛为氧化剂,使用催化量异丙醇铝在甲苯中于95℃反应2h即可完成,收率85%.总收率71%. 相似文献
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仙人掌中一个新α-吡喃酮成分的分离与结构鉴定 总被引:1,自引:0,他引:1
目的研究仙人掌的化学成分。方法应用多种柱色谱方法进行分离和纯化,NMR和MS等波谱解析化学结构。结果从仙人掌肉质茎的乙醇提取物中分离出6个化合物,其结构分别鉴定为:3-O-甲基异鼠李黄素(1)、4-乙氧基-6-羟甲基-α-吡喃酮(2)、正十七醇(3)、香草酸(4)、异鼠李黄素-3-O-鼠李糖苷(5)和芦丁(6)。结论化合物2为新化合物,化合物1、3、4、5均为首次从本属植物中分离得到,化合物6为本植物首次分离得到。 相似文献
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7α-和7β-甲基-10β,17β-二乙酰氧基-△~4-雌甾烯-3酮(简称7α-和7β-甲-乙氧雌酮)对小鼠抗早孕ED_(50)分别为1.6和5.5 mg/kg。7α-甲-乙氧雌酮在大鼠也有抗早孕作用并使血浆孕酮浓度降低,应用10 μg/ml浓度能抑制离体妊娠大鼠卵巢孕酮合成。7α-和7β-甲-乙氧雌酮与兔子宫胞浆雌二醇受体的相对结合亲和力(RBA)分别为10.8和1.5,与孕酮受体的RBA均<1.7α-和7β-甲-乙氧雌酮都有较弱的雌激素和抗雌激素活性。 相似文献
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A novel gymnomitrane-type alcohol was identified from the liverwort Cylindrocolea recurvifolia. The structure of this new compound was confirmed by X-ray analysis. This is the first report on the chemical constituents of this genus. 相似文献
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Hua Guo Jing Si Zheng-Hui Li Tao Feng Ze-Jun Dong Yu-Cheng Dai 《Journal of Asian natural products research》2013,15(3):253-257
Two new triterpenoids, 3β-(2-methoxy-oxalyloxy)-24-methylene-lanost-8-en-21-oic acid (1) and 3β-(2-methoxy-oxalyloxy)-15α-hydroxy-24-methylene-lanost-8-en-21-oic acid (2), were isolated from cultures of the fungus Perenniporia maackiae, together with two previously known triterpenoids (3 and 4). Their structures were determined by spectroscopic methods, including 1D and 2D NMR, and MS analyses. All compounds were evaluated for their cytotoxic activities on five tumor cell lines. 相似文献
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A novel gymnomitrane-type alcohol was identified from the liverwort Cylindrocolea recurvifolia. The structure of this new compound was confirmed by X-ray analysis. This is the first report on the chemical constituents of this genus. 相似文献
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Application of endogenous anabolic steroids to meat producing animals is not allowed in the EU. In other countries application is practised due to a low oral activity based on an efficient first liver passage. This contrasts with pharmacological investigations where steroids were readily absorbed by the buccal and sublingual mucosa using absorption enhancers. An in vivo study was performed to clarify possible absorption after sublingual applications of one milligram portions of either testosterone (T), 17beta-estradiol (E), or nortestosterone (NT) in sesame oil to castrated male pigs (n=5) without specific delivery systems during anaesthesia. Blood samples were drawn using jugular vein catheters for 15 min before and 3h after application. Hormone concentrations were determined by Radioimmunoassay for T and E or Enzymeimmunoassay for NT. For all steroids a slight increase was measurable one minute after application. Maximal values for T, E, and NT were 2.5 ng/ml, 1.5 ng/ml and 4.2 ng/ml, respectively, and were observed after 10 min. The concentrations of the three steroids decreased slowly thereafter but were still significantly elevated 1-3h after application. Oral absorption of steroids without enhancers should be considered in risk analysis. 相似文献
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Repeated chromatography of the n-hexane-soluble fraction of the MeOH extract of the rhizomes of Zingiber zerumbet led to the isolation of two isomers of 6-methoxy-2E,9E-humuladien-8-one (1 and 2) and stigmast-4-en-3-one. The structures of 1 and 2 were determined by spectroscopic methods including 1 D and 2D-NMR elucidated by analysis of spectroscopic data as well as by comparison with published values. This is the first report on the isolation of compounds 1 and 2 from the nature. Stigmast-4-en-3-one was first isolated from this plant. 相似文献