采用活性追踪分离的方法,从鱼藤中分离鉴定出了2个抗肿瘤活性化合物,即羟基鱼藤素(1)和鱼藤酮(2).用丽丝胺罗丹明B(SRB)法评价其抗肿瘤活性,用紫外光谱和荧光光谱等方法探讨了化合物与DNA的相互作用.结果发现,羟基鱼藤素(1)与鱼藤酮(2)为鱼藤的抗肿瘤活性成分,对人大肠癌细胞HCT8、人肝癌细胞BEL7402、人胃癌细胞BGC823、人肺癌细胞A549和人卵巢癌细胞A2780的半数抑制浓度(IC50)在0.1~90.0μmol/L之间.这两种化合物的紫外吸收强度随着HS—DNA的加入均呈现减色效应,并使EB—HS—DNA复合体系荧光强度减弱,表明化合物的抗肿瘤活性与DNA以插入方式作用有关.
Two antitumor compounds, tephrosin(1) and rotenone(2), were acquied by bioassay-guided isolation from Derris trifoliate Lour. Compounds 1 and 2, assayed by SRB (Sulforhodamine B) methods, showed antitumor activities against cell lines of HCT8, BELT402, BGC823, A549 and A2780 in vitro with IC50 values from 0. 1 to 90. 0 μmol/L. The interaction of the compounds with HS-DNA was investigated using UV spectra and fluorescent spectra. The absorbance values at the UV max peaks of compounds 1 and 2 were reduced by adding HS-DNA while the intensity of fluorescent spectra of EB-HS-DNA were gradually weaken following the increased amounts of compounds 1 and 2. It indicated that the mode of antitumor activities of compounds 1 and 2 was relative to binding with DNA through intercalation mode.