Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Brno, Palackeho 1-3, CZ-612 42, Czech Republic.
J Nat Prod. 2010 Apr 23;73(4):568-72. doi: 10.1021/np900681y.
Nine geranylated flavanones isolated from the fruits of Paulownia tomentosa (4-12) and two from the roots of Morus alba (13 and 14) were examined for cytotoxicity to selected human cancer cell lines and normal human fibroblasts. Cytotoxicity was determined in vitro using a calcein AM cytotoxicity assay. Cytotoxicity for the THP-1 monocytic leukemia cell line was tested using erythrosin B cell staining. The geranylated compounds tested were compared with the known simple flavanone standards taxifolin (1), naringenin (2), and hesperetin (3) and with the standard anticancer drugs olomoucine II, diaziquone, and oxaliplatin and the antineoplastic compound camptothecin, and showed different levels of cytotoxicity. The effects of structural changes on cytotoxic activity, including geranyl substitution of the flavanone skeleton and the oxidation pattern of ring B of the flavanones, are discussed.
从泡桐果实（4-12）中分离得到的 9 种香叶基黄酮和从桑树根中分离得到的 2 种香叶基黄酮（13 和 14）被检测对选定的人类癌细胞系和正常人类成纤维细胞的细胞毒性。使用 calcein AM 细胞毒性测定法在体外测定细胞毒性。使用曙红 B 细胞染色法测试对 THP-1 单核白血病细胞系的细胞毒性。测试的香叶基化合物与已知的简单黄烷酮标准taxifolin（1）、柚皮素（2）和橙皮素（3）以及标准抗癌药物olomoucine II、diaziquone 和 oxaliplatin 和抗肿瘤化合物喜树碱进行了比较，并显示出不同程度的细胞毒性。讨论了结构变化对细胞毒性活性的影响，包括黄烷酮骨架的香叶基取代和黄烷酮 B 环的氧化模式。
