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(英文)

Cytotoxic activity of five limonoids from Meliae cortexand their structure-activity relationship

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IC508.57μg·mL-1,对人肺癌H460细胞的IC506.29μg·mL-1,对人胃癌SGC-7901细胞的IC506.08μg·mL-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。

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 celllines 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 μg·mL-1）,human lungcancer H460 cells（IC50 6.29 μg·mL-1）,human stomach cancer SGC-7901 cells（IC50 6.08 μg·mL-1）.CONCLUSION：The SAR ofcompounds 1-5 indicated that 16-OH was very important for keeping the cytotoxic activity of limonoids.