Skalkos Dimitris, Stavropoulos Nikolaos E, Tsimaris Ioannis, Gioti Eleni, Stalikas Constantine D, Nseyo Unyime O, Ioachim Elli, Agnantis Niki J
Department of Material Sciences & Engineering, University of Ioannina, Greece.
Planta Med. 2005 Nov;71(11):1030-5. doi: 10.1055/s-2005-873127.
Hypericum perforatum L. (St. John's wort) is a medicinal plant used for many pathologies, especially for the treatment of mild to moderate depression. In the present study we have investigated the cytotoxic activity of the locally collected (Epirus region) Hypericum perforatum L. against cultured T24 and NBT-II bladder cancer cell lines. The lipophilic extract of the herb, prepared using petroleum ether, induced apoptosis displaying LC(50) values at concentrations as low as 4 and 5 microg/mL. A fraction of this extract displayed 60 % cell growth inhibition at a concentration of 0.95 microg/mL. Evaluating the importance of various biologically active components of the extract, it was found that hypericins (hypericin, pseudohypericin, etc.) were identified only in the methanolic (lipophobic) extract of the herb, and not in the active lipophilic extract. In addition, hyperforin concentrations in the lipophilic extract and its most active fraction, were 0.94 microg/mL, and 0.17 microg/mL, respectively, while the active cytotoxic concentration of pure hyperforin appeared in the range of 1.8 microg/mL - 5.0 microg/mL. Therefore, pure hyperforin does not seem to contribute significantly to the cytotoxicity activity. Chlorophylls were identified in low, not significantly different, concentrations in all extracts and fractions and were not correlated to the biological activity. Owing to the combination of significant cytotoxic activity, natural abundance and low toxicity, the lipophilic extract of Hypericum perforatum holds the promise of being an interesting, new, antiproliferative agent against bladder cancer that deserves further investigation.
贯叶连翘是一种用于多种病症治疗的药用植物，尤其用于治疗轻至中度抑郁症。在本研究中，我们调查了当地采集（伊庇鲁斯地区）的贯叶连翘对培养的T24和NBT-II膀胱癌细胞系的细胞毒性活性。用石油醚制备的该草药亲脂性提取物在低至4和5微克/毫升的浓度下诱导细胞凋亡，显示出半数致死浓度（LC50）值。该提取物的一部分在浓度为0.95微克/毫升时显示出60%的细胞生长抑制率。在评估提取物中各种生物活性成分的重要性时，发现金丝桃素（金丝桃素、假金丝桃素等）仅在该草药的甲醇（疏脂性）提取物中被鉴定出来，而在活性亲脂性提取物中未被鉴定出来。此外，亲脂性提取物及其最具活性部分中的金丝桃素浓度分别为0.94微克/毫升和0.17微克/毫升，而纯金丝桃素的活性细胞毒性浓度出现在1.8微克/毫升至5.0微克/毫升的范围内。因此，纯金丝桃素似乎对细胞毒性活性没有显著贡献。在所有提取物和部分中均鉴定出低浓度的叶绿素，且浓度差异不显著，并且与生物活性无关。由于具有显著的细胞毒性活性、天然存在且低毒性的综合特性，贯叶连翘的亲脂性提取物有望成为一种有趣的新型抗膀胱癌增殖剂，值得进一步研究。
