Hu Hao-Bin, Liang Hai-Peng, Li Hai-Ming, Yuan Ru-Nan, Sun Jiao, Zhang La-La, Han Ming-Hu, Wu Yun
College of Chemistry & Chemical Engineering, Longdong University, Qingyang 745000, PR China.
Department of Oncology, Qingyang First People's Hospital, Qingyang 745000, PR China.
Fitoterapia. 2018 Jan;124:167-176. doi: 10.1016/j.fitote.2017.11.007. Epub 2017 Nov 8.
Twenty natural stilbenoids (1-20), including seven new stilbenoids (2, 4-7, 19, 20) and thirteen known stilbenoids (1, 3, 8-18), were isolated from the stem barks of Acanthopanax leucorrhizus, and six modified stilbenoid derivatives (1a, 2a, 4a, 4b, 7a and 17a) were obtained via methylation, demethylation and isopentenylation of the corresponding isolates (1, 2, 4, 7 and 17). These stilbenoids were structurally characterized by comprehensive analysis of their spectroscopic data and comparison with literature information, and evaluated for their cytotoxic activities against three human tumor cell lines (leukemia HL-60, hepatoma SMMC-7721 and breast carcinoma MCF-7) in vitro by MTT assay. The results showed that compounds 1a, 4a and 4b showed potent selective cytotoxicity against SMMC-7721 (IC=10.16±1.95μM and 9.76±1.32μM) and MCF-7 (IC=10.72±2.78μM) cell lines. The cytotoxic evaluation of these structurally modified stilbenoid derivatives have led to the establishment of a structure-activity relationship.
从五加科植物白簕的茎皮中分离得到20种天然芪类化合物（1-20），包括7种新的芪类化合物（2、4-7、19、20）和13种已知的芪类化合物（1、3、8-18），并通过对相应分离物（1、2、4、7和17）进行甲基化、去甲基化和异戊烯基化反应得到6种修饰的芪类衍生物（1a、2a、4a、4b、7a和17a）。通过对这些芪类化合物的光谱数据进行综合分析并与文献信息进行比较，对其结构进行了表征，并采用MTT法在体外评估了它们对三种人类肿瘤细胞系（白血病HL-60、肝癌SMMC-7721和乳腺癌MCF-7）的细胞毒性活性。结果表明，化合物1a、4a和4b对SMMC-7721细胞系（IC=10.16±1.95μM和9.76±1.32μM）和MCF-7细胞系（IC=10.72±2.78μM）显示出强效的选择性细胞毒性。对这些结构修饰的芪类衍生物的细胞毒性评估建立了构效关系。
