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生物活性导向法从矢车菊中分离具有抗增殖活性的化合物

Bioactivity-guided isolation of antiproliferative compounds from Centaurea jacea L.

机构信息

Department of Pharmacognosy, University of Szeged, Szeged, Hungary.

出版信息

Fitoterapia. 2012 Jul;83(5):921-5. doi: 10.1016/j.fitote.2012.04.006. Epub 2012 Apr 17.

DOI:10.1016/j.fitote.2012.04.006
PMID:22537643
Abstract

Bioassay-guided fractionation of the chloroform extract of Centaurea jacea L. afforded the isolation of cirsiliol, apigenin, hispidulin, eupatorin, isokaempferide, axillarin, centaureidin, 6-methoxykaempferol 3-methyl ether, trachelogenin, cnicin, 4'-acetylcnicin and three aliphatic glucose diesters, including the new natural product 1β-isobutanoyl-2-angeloyl-glucose. The structures of the compounds were established on the basis of spectroscopic analyses (UV, MS and NMR). All compounds were isolated for the first time from this species. The compounds were evaluated for their tumour cell growth inhibitory activities on HeLa, MCF-7 and A431 cells. Different types of secondary metabolites (flavonoids, sesquiterpenes) were found to be responsible for the antitumour effects of the extracts; the highest activity was exerted by centaureidin, in addition to moderately active compounds (cirsiliol, isokaempferide, apigenin, hispidulin, cnicin and 4'-acetylcnicin).

摘要

生物测定导向的矢车菊属植物氯仿提取物的分段分离得到了泽兰内酯、芹菜素、木犀草素、大波斯菊苷、异泽兰黄素、紫菀酮、矢车菊苷、6-甲氧基山奈酚 3-甲基醚、千里光萜醇、山奈酚、4'-乙酰山奈酚和三种脂肪葡萄糖二酯,包括新的天然产物 1β-异丁酰基-2-当归酰基葡萄糖。根据光谱分析(UV、MS 和 NMR)确定了化合物的结构。所有化合物均首次从该种中分离得到。评估了这些化合物对 HeLa、MCF-7 和 A431 细胞的肿瘤细胞生长抑制活性。不同类型的次生代谢产物(类黄酮、倍半萜)被认为是提取物具有抗肿瘤作用的原因;除了具有中等活性的化合物(泽兰内酯、异泽兰黄素、芹菜素、木犀草素、山奈酚和 4'-乙酰山奈酚)外,矢车菊苷的活性最高。

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