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天然生物碱
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  natural alkaloid
     Enantioselective Catalyzed Hydrogenation to Natural Alkaloid Isoanabasine with (S)-BINAP-Rh
     对映体选择性催化氢化合成天然生物碱异毒藜碱
短句来源
     The 10-hydroxycamptothecin(HCPT) demonstrates more significant antitumor activity and less toxicity than another natural alkaloid—the camptothecin, so it arrests more and more attention as an important intermediate in camptothecin derivatives.
     其中10—羟基喜树碱(HCPT)因为比另一种天然生物碱—喜树碱的抗肿瘤效果好,且毒性较低,因此越来越受到人们的重视,日益成为喜树碱类衍生物研究的重要中间体。 但是HCPT的水溶性极差,一般将其制成水溶性钠盐用于临床。
短句来源
  “天然生物碱”译为未确定词的双语例句
     Regioselective Friedel-Crafts alkylation at the 3-position of indoles represents one of the most straightforward methods for the synthesis of many naturally occurring alkaloids.
     在吲哚3位的区域选择性Friedel-Crafts烷基化代表了合成许多天然生物碱的最直接的方法之一。
短句来源
     In chapter 3, based on the work of our lab, 13 naturally occurring unsaturated amide alkaloids bearing pyrrolidine, isobutyl and piperidine moieties and one analogue were synthesized by Ramberg-Backlund reaction.
     第3章将本组在Ramberg-Backlund反应方面的研究拓展到共轭多烯酰胺生物碱的合成中。 以该反应为关键步骤合成了13个具有吡咯烷,异丁基或哌啶结构的天然生物碱和一个类似物。
短句来源
     The current applications and traits of supercritical fluid extraction technique in alkaloids' extraction were reviewed emphatically in this paper according to the classification of alkaloids' pharmacological action.
     以生物碱的生物活性分类,综述了超临界萃取技术在各种天然生物碱提取中的应用研究现况及其特点。
短句来源
  相似匹配句对
     THE NATURAL C_(20)-DITERPENOID ALKALOIDS
     天然C_(20)二萜生物碱
短句来源
     ADVANCNESIN CHEMISTER OF NORDITERPENOID ALKALOIDS
     天然去甲二萜生物碱的研究进展
短句来源
     Natural Seasoning
     天然调味料
短句来源
     Natural Slate
     天然板石
短句来源
     THIN LAYER CHROMATOGRAPHY OF ALKALOIDS
     生物碱的薄层层离
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  natural alkaloids
Actually total syntheses of natural alkaloids, (-)-antirhine, (+)-dihydroantirhine and (-) dihydrocorynantheol were accomplished.
      
Structures, origins, biosynthesis, photodimerization, and biological activities of a selection of cyclobutane-containing alkaloids and selected synthethic analogs of natural alkaloids are reviewed.
      
Information provided on the packings of the tablet only indicated the presence of natural alkaloids and vitamines.
      
Examples of the synthesis of physiologically active natural alkaloids with the structure of the above-mentioned condensed isoindoles are presented.
      
Examples of the synthesis of physiologically active natural alkaloids possessing the structure of these condensed isoindoles are presented.
      
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  natural alkaloid
The natural alkaloid boldine, added at 0.5 mg/g oil level, improved the oxidative stability by a factor ranging from 1.7 to 2.4, as assessed by the Oil Stability Index method between 90 and 110°C.
      
All synthetic isomers of (+)-muscarine, the racemic forms of epi-muscarine, allo-muscarine, and epiallo-muscarine are at least 100 times less potent on blood pressure of cats and isolated frog hearts than the natural alkaloid.
      
(-)-Emetine, as prepared by total synthesis, has the same antiamebic activity and toxicity as the natural alkaloid.
      
The latter salts by the action of ammonia are converted to the corresponding β-carbolines - derivatives of the natural alkaloid harman.
      
The brevicarine obtained by the cleavage of the pyrrolidine ring of brevicolline is identical with the natural alkaloid, which is an additional proof of its structure.
      
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The present paper deals with the results of hunting for new sources of five medi- cinal alkaloids. Reserpine:A study by means of paper chromatography and UV spectra indicat- ed that reserpine was present in all five species and three varieties of Chinese Rau- volfia,viz.R.serpentina,R.yunnanensis,R.latifrons,R.tiaolushanensis,R.verticil- lata,R.verticillata var.rubrocarpa,R.verticillata var.hainanensis,R.verticillata var. oblanceolata,the total alkaloid and the reserpine percentage of these plants are given...

The present paper deals with the results of hunting for new sources of five medi- cinal alkaloids. Reserpine:A study by means of paper chromatography and UV spectra indicat- ed that reserpine was present in all five species and three varieties of Chinese Rau- volfia,viz.R.serpentina,R.yunnanensis,R.latifrons,R.tiaolushanensis,R.verticil- lata,R.verticillata var.rubrocarpa,R.verticillata var.hainanensis,R.verticillata var. oblanceolata,the total alkaloid and the reserpine percentage of these plants are given in table 1. Atropine:Tested by the method of TLC of the Chinese solanaceous plants,hy- oscyamine has been shown to be present in Atropanthe sinensis,Mandrogora caules- cens,Hyoscyamus pusillus,Physochlaina infundibularis,Physochlaina physoides,Prze- walskia shebbearei,Przewalskia tangutica,Scopolia lurida,Scopolia tangutica.Further- more,the major alkaloid isolated from the roots of Przewalskia shebbearei was iden- tified as hyoscyamine based upon melting point,UV and IR spectra,the total alkaloid and hyoscyamine content was 1.89% and 1.65% respectively.Owing to the presence of tropane group alkaloids in the genus Przewalskia,it thus reveals the ubiquitous existence of these alkaloids in the whole genera of the Solanaceae-Solaneae-Hyoscya- minae(sensu Wettstein),which may be regarded as a high incidence of tropane-con- taining category. Strychnine:By means of an alkaloid screening method,three species of Strychnos appear to have a high alkaloid content,viz.S.pierriana,S.confertiflora and S.hainan- ensis.Strychnine is the princeple alkaloid identified in the seeds of S.pierriana and in the roots of S.confertiflora,while the seeds of S.hainanensis contains chiefly brucine.The total alkaloid content was 1.26% and 2.9% with strychnine content of 1.1% and 0.04% for the 2nd and 3rd plant respectively. Ephedrine:A study has been made on the total alkaloid content as well as ephe- drine and pseudo-ephedrine percentages of genus Ephedra,obtained from autonomous regions Sinkiang and Tibet,the results are recorded in table 2. Berberine:The amount of berberine in Tibetan Berberis has also been determined. Berberis jamesiana Forrest et W.W.Sm.has been found to contain a high content of this alkaloid(7.07%—7.73%). Finally,the present work reveals that the Plant Phylogeny-Phytochemistry rela- tionships can be satisfactorily used in the discovery of new sources of drugs.

本文报道了五种重要的药用生物碱资源植物的研究结果对于萝芙木总碱和利血平资源植物,分析了国产萝芙木属(Rauvolfia)五个种及三个变种根中总生物碱及利血平的含量;对于阿托品资源植物,重点研究了国产的茄科植物,发现有六个属九个种植物含有莨菪碱,并证明矮莨菪(Przewalskia shebbearei)根中的总生物碱高达1.89%,莨菪碱含量为1.65%;对于士的宁资源植物,研究了八种国产的马钱属(Strychnos)植物,有三种含生物碱量较高;对于麻黄碱资源植物,重点分析了产于西藏与新疆的麻黄属(Ephedra)的三个种及一变种;对于小檗碱资源植物,分析了采自西藏的四种小檗属(Berberis)植物,其中大刺黄柏小檗内皮的含量以小檗碱计算可达7.73%。本研究证明了利用植物亲缘关系相近,则其化学成分也近似的规律来寻找并扩大药物资源,是一种有效的途径。当某种天然生物碱通过大量的研究和临床验证,肯定其疗效,并确定其法定地位(收载入药典),投入生产时,对于这种药物资源的需求,就成为一个突出的问题。目前,除了根据其化学结构采用人工合成方法外,最常用的解决途径便是利用植物亲缘关系和化学成分间存在着密切联系...

本文报道了五种重要的药用生物碱资源植物的研究结果对于萝芙木总碱和利血平资源植物,分析了国产萝芙木属(Rauvolfia)五个种及三个变种根中总生物碱及利血平的含量;对于阿托品资源植物,重点研究了国产的茄科植物,发现有六个属九个种植物含有莨菪碱,并证明矮莨菪(Przewalskia shebbearei)根中的总生物碱高达1.89%,莨菪碱含量为1.65%;对于士的宁资源植物,研究了八种国产的马钱属(Strychnos)植物,有三种含生物碱量较高;对于麻黄碱资源植物,重点分析了产于西藏与新疆的麻黄属(Ephedra)的三个种及一变种;对于小檗碱资源植物,分析了采自西藏的四种小檗属(Berberis)植物,其中大刺黄柏小檗内皮的含量以小檗碱计算可达7.73%。本研究证明了利用植物亲缘关系相近,则其化学成分也近似的规律来寻找并扩大药物资源,是一种有效的途径。当某种天然生物碱通过大量的研究和临床验证,肯定其疗效,并确定其法定地位(收载入药典),投入生产时,对于这种药物资源的需求,就成为一个突出的问题。目前,除了根据其化学结构采用人工合成方法外,最常用的解决途径便是利用植物亲缘关系和化学成分间存在着密切联系这一规律,从已知含此类成分的植物类群中去寻找高含量的新资源。实践证明,这是一条行之有效的途径。以下便是我们对五种重要药用生物碱资源植物的部分研究报道。

Detailed procedures of the total synthesis of the less toxic, more effective antitumor camptothecinoid alkaloids, dl-10-hydroxycamptothecin and dl-10-methoxycamptothecin, are described.Based on the previous works on the total synthesis of dl-camptothecin (dl-1), the following procedures were devised. The acetal 4 which was prepared from 2-nitro-5-methoxybenzaldehyde with ethylene glycol followed by hydrogenation, was condensed with 1', 2', 3', 5'-tetrahydro-5'-oxo-6'-cyano-7'-(1-carbethoxy) propyl-spiro (1,...

Detailed procedures of the total synthesis of the less toxic, more effective antitumor camptothecinoid alkaloids, dl-10-hydroxycamptothecin and dl-10-methoxycamptothecin, are described.Based on the previous works on the total synthesis of dl-camptothecin (dl-1), the following procedures were devised. The acetal 4 which was prepared from 2-nitro-5-methoxybenzaldehyde with ethylene glycol followed by hydrogenation, was condensed with 1', 2', 3', 5'-tetrahydro-5'-oxo-6'-cyano-7'-(1-carbethoxy) propyl-spiro (1, 3-dioxolene-2, 1-indolizine) (5) to give 2-methoxy-7- (1-carbethoxy) propyl-8-cyano-9, 11-dihydro-9-oxo-indolizino (1, 2-b) quinoline (6)in 66 % yield. It was hydrogenated under atmospheric pressure in a mixture of glacial acetic acid and acetic anhydride with Raney Nickel as catalyst to give 2-methoxy-7-(1'-carbethoxy) propyl-8-acetamidomethyl-9, 11-dihydro-9-oxo-indolizino(1, 2-b)quinoline(7). Without purification, the crude 7 was treated directly with sodium nitrite to afford 2-methoxy-7-(1'-carbethoxy) propyl-8-acetoxy-9, 11-dihydro-9-oxo-indolizino (1, 2-b)quinoline (8). On hydrolysis of compound 8 with dilute sulphuric acid, 10-metboxy-20-deoxycamptothecin (9) was obtained in 62% overall yield based on compound 6. Compound 9 was then oxidized by air in dimethylformamide solution in the presence of cupric chloride and dimethylamine to give dl-10-methoxycamptothecin(dl-3)with a yield of 62%. dl-10-hydroxycamptothecin (dl-2)was obtained by hydrolysis of dl-3 with 48% hydrobromic acid, with a yield of 65%.In order to avoid using silicagel chromatography for the purification of dl-2 and dl-3, an alternative method of working up was developed. The crude dl-2 produced during the hydrolysis of crude dl-3 with hydrobromic acid may be directly acetylated with acetic anhydride-pyridine to give a diacetyl derivative(10) which was then purified by recrystallization. Sufficiently pure dl-2 was obtained upon hydrolysis of 10 with hydrochloric acid-acetic acid. However, this alternative method gave a lower yield.The synthetic dl-2 and dl-3 thus prepared were identical in the TLC R_f-value, UV, NMR and MS spectra with those of the natural alkaloids. Pharmacological tests revealed that the synthetic dl-2 and dl-3 showed similar activity as the natural alkaloids on Ehrlich ascites carcinoma, ascitic reticule-cell sarcoma or lymphosarcoma in mice at an equi-toxicity dosage level. One of the synthetic alkaloids dl-2, is subjected to clinical trials.

本文详细报道以1′,2′,3′,5′-四氢-5′-氧代-6′-氰基-7′(1-乙氧羰基)丙基-螺(1,3-二噁茂烷-2,1′- 吲嗪)为原料,经6步及5步反应合成dl-10-羟基喜树碱及dl-10-甲氧基喜树碱的方法。合成产品与天然生物碱的薄板层析、紫外光谱、核磁共振谱和质谱均一致。dl-10-羟基喜树碱正在临床试用中。

A human bladder tumor cell line resistant to adriamycin,BIU-87/ADM,has been established in vitro by the stepwise exposure of BIU-87 human bl adder cancer cell to increasing concentrations of the drug over a period of 8 months.BIU-87/ADM cell showed 6.3-fold higher resistance to adriamycin than BIU-87 parent cell.BIU-87/ADM cell line was shown to significantly cross-resistant to adriamycin derivatives(epirubicin,daunoubicin),vincristine and etoposide, but not to cisplatin and mitomycin C. Anti-p-glycoprotein...

A human bladder tumor cell line resistant to adriamycin,BIU-87/ADM,has been established in vitro by the stepwise exposure of BIU-87 human bl adder cancer cell to increasing concentrations of the drug over a period of 8 months.BIU-87/ADM cell showed 6.3-fold higher resistance to adriamycin than BIU-87 parent cell.BIU-87/ADM cell line was shown to significantly cross-resistant to adriamycin derivatives(epirubicin,daunoubicin),vincristine and etoposide, but not to cisplatin and mitomycin C. Anti-p-glycoprotein monoclonal antibody JSB-1 and labelled streptaoavidin biotin(LSAB )immunocytochemical staining technique were used to study the relation between p-gp expression and MDR in BIU-87/ADM cell line.Unlike BIU-87 parent cell, about 75%of the BIU-87/ADM cell showed a positive reaction. The result indicated that there was a close association between the p-gp expression and the resistance to chemotherapeutic drug in BIU 87/ADM cell line. BIU-87/ADM may be a useful model for the development of new chemotherapeutic strategies in covercoming drug resistance in the treatment of bladder cancer.

为探讨肿瘤细胞耐药性,以人膀胱癌细胞株BIU-87为亲本,以递增阿霉素剂量的方法,历时8个月,成功地诱导建立了一株耐药细胞亚株BIU-87/ADM。通过生物学鉴定发现此细胞对阿霉素的相对时受度较亲本细胞提高了6.3倍,对阿霉素类似物柔红霉素、表阿霉素及天然生物碱类抗癌药长春新碱、鬼臼乙叉甙有明显的交叉耐药性,对顺铂、丝裂霉素则无交叉耐药性。为进一步阐明其耐药机理,应用链霉亲和素-生物素免疫细胞化学技术对其耐药性进行研究发现,约75%的BIU-87/ADM细胞P-gp过表达,而亲本细胞均为阴性。由此结果表明,BIU-87/ADM耐药性的产生主要是由于P-gp膜泵功能增强介导产生细胞内药物外溢增多所致,是其产生耐药性的主要原因,BIU-87/ADM的建立为进一步针对P-gp药泵功能逆转其抗药性的研究奠定了实验基础。

 
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