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目的:对红藻刺状鱼栖苔Acanthophora spicifera中的甾体类化学成分进行研究,寻找具有生物活性的先导化合物。方法:利用正相和反相柱色谱、Sephadex LH-20柱色谱、反相HPLC以及重结晶等手段进行分离纯化,借助MS,IR,1D和2D NMR等方法鉴定结构;通过MTT法对分离鉴定的单体化合物在HCT-8,Bel-7402,BGC-823,A549和HELA细胞株上进行细胞毒活性测试;通过MTT法对单体化合物在犬血管平滑肌细胞模型上进行增殖抑制活性测试。结果:从刺状鱼栖苔中分离得到6个甾体类化合物,分别鉴定为6-羟基-胆甾-4-烯-3-酮(1)、胆甾-4-烯-3,6-二酮(2)、胆甾-5-烯-3β-醇(3)、5α-胆甾-3,6-二酮(4)、β-谷甾醇(5)和24-羟基-24-乙烯基-胆甾醇(6)。结论:其中化合物1,2,3,5为首次从该海藻中分离鉴定;化合物1,2,4表现出一定细胞毒活性。
OBJECTIVE: To study the steroid chemical constituents of Acanthophora spicifera, aiming to find the bioactive lead compounds. Methods: The compounds were isolated and purified by normal and reversed-phase column chromatography, Sephadex LH-20 column chromatography, reverse phase HPLC and recrystallization. The structures were identified by MS, IR, 1D and 2D NMR. Cytotoxicity test was carried out on HCT-8, Bel-7402, BGC-823, A549 and HELA cell lines. The inhibitory activity of monomeric compounds on the proliferation inhibition of canine vascular smooth muscle cells was tested by MTT assay. Results: Six steroidal compounds were isolated from the prickly habitat, and were identified as 6-hydroxy-cholest-4-en-3-one (4), β-sitosterol (5) and 24-hydroxy-24-ethylene Cholesterol (6). Conclusion: Compounds 1, 2, 3 and 5 were isolated and identified from this seaweed for the first time. Compounds 1, 2 and 4 showed certain cytotoxic activity.