Sen Ali, Ozbas Turan Suna, Bitis Leyla
a Department of Pharmacognosy, Faculty of Pharmacy , Marmara University , Istanbul , Turkey.
b Department of Pharmaceutical Biotechnology, Faculty of Pharmacy , Marmara University , Istanbul , Turkey.
Pharm Biol. 2017 Dec;55(1):541-546. doi: 10.1080/13880209.2016.1255980.
The genus Centaurea L. (Asteraceae) is one of the largest genera in Turkey. Compounds and extracts obtained from different Centaurea species have significant anti-cancer activity against various cancer cell lines.
To determine the anti-proliferative activity of isolates from the chloroform extract of C. kilaea Boiss.
Eleven compounds were isolated using column chromatography and preparative TLC from the chloroform extract of aerial parts of endemic C. kilaea. The structures of the isolated compounds were elucidated by various spectroscopic methods, including UV, H-NMR and C-NMR. Anti-proliferative activity of compounds (0.5-50 μg/mL) were measured against one normal cell line (L-929, mouse fibroblast) and three human cancer cell lines (Hela, cervix carcinoma; MCF-7, breast carcinoma; PC-3, prostate carcinoma) using MTT assay. Results were expressed as IC values.
None of the 11 compounds displayed activity against L-929 and HeLa. Two of these compounds, cnicin and cirsimaritin, showed fairly strong activity against MCF-7 and PC-3 with IC values of 3.25 and 4.3 μg/mL, respectively.
This is the first report on cirsimaritin. Cirsimaritin and cnicin could serve as potential anti-cancer drug candidates against breast and prostate cancer, respectively.
矢车菊属（菊科）是土耳其最大的属之一。从不同矢车菊物种中获得的化合物和提取物对多种癌细胞系具有显著的抗癌活性。
确定基拉伊矢车菊氯仿提取物中分离物的抗增殖活性。
采用柱色谱法和制备薄层层析法从基拉伊矢车菊地上部分的氯仿提取物中分离出11种化合物。通过紫外光谱、氢核磁共振光谱和碳核磁共振光谱等多种光谱方法阐明了分离化合物的结构。使用MTT法测定化合物（0.5 - 50μg/mL）对一种正常细胞系（L - 929，小鼠成纤维细胞）和三种人类癌细胞系（Hela，子宫颈癌；MCF - 7，乳腺癌；PC - 3，前列腺癌）的抗增殖活性。结果以IC值表示。
11种化合物中没有一种对L - 929和Hela显示出活性。其中两种化合物，蓟苦素和cirsimaritin，对MCF - 7和PC - 3显示出相当强的活性，IC值分别为3.25和4.3μg/mL。
这是关于cirsimaritin的首次报道。Cirsimaritin和蓟苦素可能分别作为抗乳腺癌和抗前列腺癌的潜在抗癌药物候选物。
