苦楝皮中5个柠檬苦素化合物的细胞毒活性以及构效关系

Cytotoxic activity of five limonoids from Meliae cortex and their structure-activity relationship

摘要: 目的:研究柠檬苦素化合物1-5的细胞毒活性以及阐明其构效关系。方法:从苦楝皮中分离获得化合物1-5,采用MTT法进行3种肿瘤细胞株的体外细胞毒活性实验。结果:化合物1-5均表现出潜在的抗肿瘤活性。尤其是化合物1对人肝癌BEL7402细胞的IC508.57gmL-1,对人肺癌H460细胞的IC506.29gmL-1,对人胃癌SGC-7901细胞的IC506.08gmL-1,较其他化合物表现出更强的细胞毒活性。结论:化合物1-5的构效关系研究显示16位羟基为柠檬苦素化合物具备细胞毒活性的重要基团。

Abstract: AIM: To investigate the cytotoxic activity of five limonoids (1-5) and illuminate their structure-activity relationship (SAR). METHODS: Compounds 1-5 isolated from Meliae cortex were examined for their cytotoxic activity against three cancer cell lines in vitro by MTT method. RESULTS: Among the tested compounds, all compounds possessed their potent antitumor activity. Especially compound 1 was the most active compound against human liver cancer BEL7402 cells (IC50 8.57 gmL-1), human lung cancer H460 cells (IC50 6.29 gmL-1), human stomach cancer SGC-7901 cells (IC50 6.08 gmL-1). CONCLUSION: The SAR of compounds 1-5 indicated that 16-OH was very important for keeping the cytotoxic activity of limonoids.