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M Ando K Isogai H Azami N Hirata H Yamazaki Y Yanagi 《Journal of natural products》1992,55(11):1620-1625
Efficient syntheses of (-)-arbusclin D and (+)-4-epi-arbusclin D are reported. By these syntheses the C-4 stereochemistry of arbusclin D and the absolute configuration of (-)-arbusclin D have been determined to be a s shown in structure 1. The biological activities, such as cytotoxic activity toward P-388 lymphocytic leukemia, plant growth regulating activity, and antimicrobial activity of compounds 1, 3, 7, 9, 12, and 14 were also studied. 相似文献
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N Kaneda I S Lee M P Gupta D D Soejarto A D Kinghorn 《Journal of natural products》1992,55(8):1136-1141
From the leaves and flowers of Lippia dulcis collected in Panama, a new sweet sesquiterpene identified as (+)-4 beta-hydroxyhernandulcin [2] was isolated, accompanied by (+)-hernandulcin [1], (-)-epihernandulcin [3] (a novel natural product), and 6-methyl-5-hepten-2-one [4]. Acteoside (verbascoside) [5], a known bitter phenylpropanoid glycoside, was isolated from the flowers of L. dulcis. The structure of (+)-4 beta-hydroxyhernandulcin was established by interpretation of its spectral data. 相似文献
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结合国内外文献综述了缬草属植物化学成分的研究进展,并对该属药用植物的药理活性进行了总结。缬草属植物除含有一定的挥发油外,化学成分主要集中于单萜类、倍半萜类、木脂素类、黄酮类、生物碱类等。其中单萜类成分主要以环烯醚萜类化合物为主,根据其结构是否裂环分为环戊烷环环烯醚萜和裂环环烯醚萜。药理研究表明该属植物具镇静、解痉、抗抑郁、抗肿瘤、抗A1阿糖腺苷受体性和细胞毒性,并对心血管有一定作用。鉴于目前缺少对缬草属研究的系统回顾和综述,该文对近年来发表的缬草属研究文献进行整理和分析,为其进一步开发利用提供依据。 相似文献
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目的合成氟哌啶醇季铵盐衍生物及其还原物并研究它们的扩血管活性。方法以氟哌啶醇、氟哌啶醇经四氢硼钠还原后得到的氢化氟哌啶醇为反应物,分别与取代氯苄回流下反应得到相应的氟哌啶醇季铵盐衍生物和氢化氟哌啶醇季铵盐衍生物;所有目的化合物结构均经IR,1H-NMR,MS和元素分析确证,并测定其对KCI诱导鼠、兔胸主动脉条收缩的抑制作用。结果合成了2个系列11个新化合物(ⅠF8~13,ⅡFB8~11和FB13)。初步生物活性实验表明,多数化合物具有不同程度的扩张血管作用,其中化合物F11的血管收缩抑制活性最强。结论F11扩张血管活性明显强于先导化合物,初步构效关系表明,N-取代苄基氟哌啶醇季铵盐衍生物中苄基苯环上取代基的电性效应和取代位置可能为影响扩血管活性的重要因素。氟哌啶醇母体上羰基被还原为羟基一般对其扩血管活性影响不大。 相似文献
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Several rare phenylpropanoids of the genus Pimpinella were tested for biological activity. Compounds with epoxy groups have a negative effect on the growth of plants, and they also show insecticidal and acaricidal activities. 相似文献
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4-色酮类和4-色满酮类化合物生物活性研究概况 总被引:2,自引:0,他引:2
目的 综述4-色酮类和 4-色满酮类化合物生物活性的研究概况。方法 以国内外有代表性的论文为依据 ,进行分析、整理和归纳。结果与结论 4-色酮类和4-色满酮类化合物具有抗炎和抗变态反应、抗血小板聚集、抗癌和抗精神病等生物活性 ,随着人们对这两类化合物研究的深入 ,将会有更多的有关新药被开发。 相似文献
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目的 寻找由抗菌氟喹诺酮向抗肿瘤氟喹诺酮转化的有效结构修饰途径。方法 以抗菌氟喹诺酮药物氧氟沙星1为原料,其相应的酰肼2与二硫化碳缩环合得C-3NFDE6二唑硫醇3中间体,然后分别与5-取代苯基-2-氯甲基-1,3,4-NFDE6二唑4a~4g缩合得含氟喹诺酮骨架的双NFDE6二唑甲硫醚5a~5g,接着用碘甲烷进行季铵化反应得相应的季铵盐6a~6g。用MTT方法评价了目标化合物5a~5g和6a~6g体外对肿瘤细胞的生长抑制活性。结果 合成了14个新的目标化合物,体外均显示潜在的抗癌活性(IC50<25 μmol·L),其中季铵盐6a~6g的活性高于相应游离碱5a~5g的活性。结论 基于抗菌氟喹诺酮C-3杂环的抗肿瘤氟喹诺酮的设计值得进一步研究。 相似文献
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Ki Hyun Kim Eunjung Moon Sun Yeou Kim Sang Un Choi Jei Hyun Lee Kang Ro Lee 《Journal of ethnopharmacology》2014
Ethnopharmacological relevance
Raphanus sativus seeds (Brassicaceae) known as Raphani Semen have long been used as anti-cancer and/or anti-inflammatory agents in Korean traditional medicine. This study was designed to isolate the bioactive constituents from the seed extracts of Raphanus sativus and evaluate their anti-inflammatory and antitumor activities.Material and methods
Bioassay-guided fractionation and chemical investigation of a methanolic extract of the seeds of Raphanus sativus led to the isolation and identification of seven 4-methylthio-butanyl derivatives. Structural elucidation of the isolated compounds was carried out using 1D and 2D nuclear magnetic resonance (NMR) spectroscopy techniques (1H, 13C, COSY, HMQC and HMBC experiments) and mass spectrometry.Results
The isolated compounds were characterized as in the following: three new 4-methylthio-butanyl derivatives, sinapoyl desulfoglucoraphenin (1), (E)-5-(methylsulfinyl)pent-4-enoxylimidic acid methyl ester (2), and (S)-5-((methylsulfinyl)methyl)pyrrolidine-2-thione (3), together with four known compounds, 5-(methylsulfinyl)-4-pentenenitrile (4), 5-(methylsulfinyl)-pentanenitrile (5), sulforaphene (6), and sulforaphane (7). Full NMR data assignments of the three known compounds 4–6 were also reported for the first time. We evaluated the anti-neuroinflammatory effect of 1–7 in lipopolysaccharide-stimulated murine microglia BV2 cells. Compound 1 significantly inhibited nitrite oxide production with IC50 values of 45.36 μM. Moreover, it also reduced the protein expression of inducible nitric oxide synthase. All isolates were also evaluated for their antiproliferative activities against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15), and all of them showed antiproliferative activity against the HCT-15 cell, with IC50 values of 8.49–23.97 μM.Conclusions
4-Methylthio-butanyl derivatives were one of the main compositions of Raphanus sativus seeds, and activities demonstrated by the isolated compounds support the ethnopharmacological use of Raphanus sativus seeds (Brassicaceae) as anti-cancer and/or anti-inflammatory agents. 相似文献12.
Soriano-Agatón F Lagoutte D Poupon E Roblot F Fournet A Gantier JC Hocquemiller R 《Journal of natural products》2005,68(11):1581-1587
Zanthoxylum chiloperone var. angustifolium was investigated. Alkaloids 1-3 from the canthin-6-one series were characterized. Derivatives 7-28 were prepared by hemisynthesis or total synthesis. All compounds were tested for in vitro antifungal activities against five pathogenic fungal strains. Analogues of canthin-6-one did not show better antifungal activities. 相似文献
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Modified taxols, 4. Synthesis and biological activity of taxols modified in the side chain 总被引:1,自引:0,他引:1
A number of taxol derivatives substituted at the 2' position of the side chain have been prepared and their biological activities determined in KB cell culture and/or the P-388 in vivo assay. The 2'-(t-butyldimethylsilyl)taxol 5 is essentially inactive, indicating the need for a free hydroxyl group at the 2' position for activity. Epimerization of the 2' position occurred on treatment of 2'-acetyltaxol derivatives with 1,5-diazabicyclo[5.4.0]undec-7-ene, but treatment of 2'-(2,2,2-trichloroethyloxycarbonyl) taxol derivatives with DBU yielded the novel cyclization products 11 and 12 and, after deprotection at the 7 position, 13. The derivative 13 is also essentially inactive in the KB test system. Two taxols with increased H2O solubility were prepared, the 2'-(beta-alanyl) derivative 15 and the 2'-succinyl derivative 16. Although both these derivatives were active in vivo and in vitro, the former was too unstable and the latter not active enough to make suitable H2O-soluble derivatives of taxol. 相似文献
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《中成药》2019,(4)
目的研究薰衣草Lavandula angustifolia Mill.残渣的化学成分及其生物活性。方法薰衣草残渣的正丁醇部位采用硅胶、Sephadex LH-20、ODS、半制备高效液相进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。检测抗氧化、降糖活性。结果从中分离得到10个化合物,分别鉴定为木樨草素-4′-O-β-D-葡萄糖醛酸苷(1)、木樨草素-3′-O-β-D-(6″-甲基)-葡萄糖醛酸苷(2)、木樨草素-7-O-β-D-葡萄糖醛酸苷(3)、木樨草素-7-O-β-(6″-甲基)-葡萄糖醛酸苷(4)、芹菜素-7-O-β-D-葡萄糖醛酸苷(5)、芹菜素-7-O-β-D-(6″-甲基)-葡萄糖醛酸苷(6)、芹菜素-7-O-β-D-(6″-乙基)-葡萄糖醛酸苷(7)、芹菜素-7-O-β-D-(6″-丁基)-葡萄糖醛酸苷(8)、(7S, 8R)-二氢去氢二愈创木基醇葡萄糖苷(9)、木樨草素(10)。化合物1、3~4对DPPH表现出较强的抗氧化活性,化合物3、7~8对PTP1B表现出较好的抑制作用。结论化合物1、2、5、7~10为首次从该植物中分离得到,化合物1、3、4、7~8有较强的生物活性。 相似文献
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白桦酯酸是一种天然存在的五环戊烷型三萜类物质,通常是从白桦Betula platyphylla树皮中分离出来,在其他植物中也有发现,以游离糖苷和糖基衍生物的形式存在于不同植物中。通过对其化学结构的修饰可以得到多种多样的衍生物,研究表明白桦酯酸及其衍生物在抗肿瘤、抗病毒、消炎止痛、抑制脑神经及血管损伤和对其他常见疾病的治疗作用等方面具有积极的作用。综述了白桦酯酸及其衍生物的种类、生物活性及作用机制,以期为今后对其进一步的研究与应用提供理论参考。 相似文献