Abstract
Context: 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. Objective: To determine the anti-proliferative activity of isolates from the chloroform extract of C. kilaea Boiss. Materials and methods: 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, lH-NMR and 13C-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 IC50 values. Results: 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 IC50 values of 3.25 and 4.3 μg/mL, respectively. Discussion and conclusion: This is the first report on cirsimaritin. Cirsimaritin and cnicin could serve as potential anti-cancer drug candidates against breast and prostate cancer, respectively.
Highlights
Cancer is a complicated genetic disease defined as uncontrolled growth, invasion, angiogenesis and metastasis, and one of the main causes of death in the world (Moura et al 2016)
We previously reported anti-proliferative activity of heptane (H), chloroform (C) and methanol extracts endemic C. kilaea against three human cancer cell lines (Hela; cervix adenocarcinoma, MCF-7; breast adenocarcinoma, PC-3; prostate adenocarcinoma) using MTT assay and C exhibited the greatest anti-proliferative activity against Hela and MCF-7 cells while C and M showed the highest activity against PC-3 cell
Total 11 compounds from the active extract of the plant consisting of seven flavonoids (30-O-methyl eupatorin, apigenin, cirsimaritin, eupatorin, jaseosidin, pectolinarigenin, salvigenin), two sesquiterpene lactones and two triterpene are isolated and the structures of compounds are elucidated using spectroscopic methods
Summary
Cancer is a complicated genetic disease defined as uncontrolled growth, invasion, angiogenesis and metastasis, and one of the main causes of death in the world (Moura et al 2016). In Turkey, the age-standardized rate of cancer among males in 2013 was 267.9 per 100,000; for female, the rate is 186.5 per 100,000. Total cancer incidence is 227.2 per 100,000, and 174,000 new cancer cases in Turkey have been diagnosed in 2013 (TPHI 2016). Chemotherapy is the most common cancer treatment, due to its side effects, it needs to be improved (Ummavathy et al 2015; Zheng et al 2016). Complementary and alternative medicine is the most noticeable approach in cancer management. Most of the anti-tumour drugs are generally developed from efficient herbal phytochemicals. Medicinal plants could be a good source of anti-tumour agents. Herbal-based drugs might be developed after systematic assessment and chemical modification (Zheng et al 2016)
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