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The apoptotic activity of one VLC fraction of the sponge Petrosia tuberosa on human cervical cells and the subsequent isolation of a bioactive polyacetylene

机译:海绵Petro的一个VLC馏分对人宫颈细胞的凋亡活性以及随后的生物活性聚乙炔的分离

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As part of our ongoing studies on bioactive natural products from marine sponges, we investigated the cytotoxic potential of extracts from the new sponge Petrosia tuberosa sampled from Mauritius waters. Bioguided fractionation of the ethyl acetate extract by vacuum liquid chromatography (VLC) revealed two fractions, namely VLC (6-9) and (13-17) showing cell deaths of 86 ± 1% and 88 ± 4%, respectively, at 50 μg/mL on HeLa cells. At 10 μg/mL, only VLC (13-17) displayed a significant cell death (56 ± 7%) compared with VLC (6-9) (8 ± 1%). The cytotoxic activity of VLC (13-17) was also determined on nine other human cancer cell lines. Clonogenic assay, mitochondrial membrane potential change, DNA fragmentation and microscopic analysis of fraction VLC (13-17) revealed distinct features of apoptosis on HeLa cells. Further fractionation and purification of this fraction by chromatographic techniques resulted in isolation of one known secondary metabolite, petrosynol. Its structure was determined by ~1H and ~(13)C-NMR analyses.
机译:作为我们正在进行的有关海洋海绵生物活性天然产物研究的一部分,我们调查了从毛里求斯水域采样的新型海绵Petrosia tuberosa提取物的细胞毒性潜力。通过真空液相色谱法(VLC)对乙酸乙酯提取物进行生物引导分馏显示出两个馏分,即VLC(6-9)和(13-17)在50μg时分别显示出86±1%和88±4%的细胞死亡/ mL在HeLa细胞上。与VLC(6-9)(8±1%)相比,在10μg/ mL下,只有VLC(13-17)表现出显着的细胞死亡(56±7%)。 VLC(13-17)的细胞毒性活性也已在其他9种人类癌细胞系中确定。克隆分析,线粒体膜电位变化,DNA片段化和级分VLC(13-17)的显微镜分析揭示了HeLa细胞凋亡的明显特征。通过色谱技术进一步分级分离和纯化该级分,导致分离出一种已知的次级代谢产物,邻苯三酚。通过〜1H和〜(13)C-NMR分析确定其结构。

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