Department of Pharmacognosy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Phytother Res. 2010 Nov;24(11):1664-9. doi: 10.1002/ptr.3187.
The antiproliferative effects of n-hexane, chloroform and aqueous methanol extracts prepared from the whole plant of Centaurea arenaria M.B. ex Willd. were investigated against cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF7) and skin epidermoid carcinoma (A431) cells, using the MTT assay. The chloroform extract displayed high tumour cell proliferation inhibitory activity (higher than 85% at 10 μg/mL concentration), and was therefore subjected to a bioassay-guided multistep separation procedure. Flavonoids (eupatilin, eupatorin, 3'-methyleupatorin, apigenin and isokaempferid), lignans (arctigenin, arctiin and matairesinol), the sesquiterpene cnicin, serotonin conjugates (moschamine and cis-moschamine), β-amyrin and β-sitosterin-β-D-glycopyranoside, identified by means of UV, MS and NMR spectroscopy, were obtained for the first time from this species. The isolated compounds were also evaluated for their tumour cell growth inhibitory activities on HeLa, MCF7 and A431 cells, and different types of secondary metabolites were found to be responsible for the antitumour effects of the extracts; in addition to moderately active compounds (isokaempferid and moschamine), especially apigenin, eupatorin, arctigenin, arctiin, matairesinol and cnicin exert marked antitumour effects against these cell lines.
采用 MTT 法，研究了来自滨藜 Centaurea arenaria M.B. ex Willd. 全草的正己烷、氯仿和水甲醇提取物对宫颈腺癌（HeLa）、乳腺腺癌（MCF7）和皮肤表皮样癌细胞的增殖抑制作用。氯仿提取物显示出高的肿瘤细胞增殖抑制活性（在 10μg/mL 浓度下高于 85%），因此进行了基于生物测定的多步分离程序。首次从该物种中分离得到了黄酮类化合物（艾黄素、艾皮素、3'-甲氧基艾皮素、芹菜素和异坎皮定）、木脂素（牛蒡子素、牛蒡子苷元和马泰瑞宁）、倍半萜 cnicin、血清素缀合物（木香素和顺式木香素）、β-香树脂醇和β-谷甾醇-β-D-吡喃糖苷。通过 UV、MS 和 NMR 光谱鉴定了这些化合物。分离得到的化合物也对 HeLa、MCF7 和 A431 细胞的肿瘤细胞生长抑制活性进行了评价，不同类型的次生代谢产物被认为是提取物抗肿瘤作用的原因；除了中等活性的化合物（异坎皮定和木香素）外，特别是芹菜素、艾皮素、牛蒡子素、牛蒡子苷元、马泰瑞宁和 cnicin 对这些细胞系表现出显著的抗肿瘤作用。
