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Objectives Marine organisms have proven to be a rich source of potent pharmacologically active compounds. Three polyprenyl‐1,4‐hydroquinone derivates (hexaprenyl‐1,4‐hydroquinone, heptaprenyl‐1,4‐hydroquinone and nonaprenyl‐1,4‐hydroquinone) were isolated from the Zoobenthos‐inhabiting sponges Sarcotragus muscarum and Ircinia fasciculata from the Eastern Mediterranean Sea (phylum: Porifera; class: Demospongiae). Methods Hexa‐, hepta‐ and nonaprenylhydroquinone were identified by 1H‐NMR, H,H‐COSY, heteronuclear multiple bond correlation, FAB‐MS and UV spectroscopy. The effects of the compounds on cell viability was determined using the MTT assay; anti‐oxidative potential was measured using the Trolox equivalent antioxidative capacity assay. Inhibition of nuclear factor‐k B activity was detected by secreted alkaline phosphatase assay. Activity against an array of protein kinases was determined in 96‐well FlashPlates. Key findings All compounds had prominent antioxidative activity, comparable to that of the synthetic vitamin E derivate Trolox. Hexaprenylhydroquinone showed the greatest cytotoxicity in H4IIE hepatoma cells (EC50 2.5 μM). All three compounds inhibited NF‐k B signalling in this cell line, with heptaprenylhydroquinone being the most active. Screening of 23 kinases involved in signal transduction pathways (cell proliferation, survival, angiogenesis and metastasis) showed that hexaprenylhydroquinone and heptaprenylhydroquinone inhibited the activity of the epidermal growth factor receptor (IC50 1.6 and 1.4 μg/ml, respectively), and heptaprenylhydroquinone also inhibited the activity of other kinases (Src tyrosine kinase, vascular endothelial growth factor receptor 3 and insulin‐like growth factor 1 receptor). Conclusions The prenylated hydroquinones isolated from the marine sponges S. muscarum and I. fasciculata showed cytotoxic and antioxidative activities and inhibited NF‐k B signalling in H4IIE hepatoma cells and protein kinases. These findings may result in the generation of new lead substances in cancer therapy.  相似文献
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目的分离鉴定海绵Axinella verrucosa中的溴吡咯生物碱,并进行体外免疫活性评价。方法利用减压柱层析、Sephdex LH-20凝胶柱层析、半制备HPLC等色谱方法分离纯化,运用NMR、MS等波谱方法并结合文献鉴定化合物结构,采用体外脾淋巴细胞增殖实验评价化合物的免疫活性。结果分离得到5个溴吡咯生物碱,分别鉴定为hymenidin(1)、stevensine(2)、4-bromopyrrole-2-carboxylic acid(3)、4,5-dibromopyrrole-2-carboxylic acid(4)和3,5-dibromo-2-pyrrolecarboxylic acid(5)。化合物1能够增强ConA诱导的T淋巴细胞增殖,化合物2能够增强LPS诱导的B淋巴细胞增殖。结论化合物4为首次从该种中分到,5为首次从该属中鉴定。化合物1和2具有一定的增强免疫作用。  相似文献
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