大黄素衍生物的合成及细胞毒性研究

Synthesis and Cytotoxicity of Emodin Derivatives

以天然大黄素为母体,经化学修饰得到一系列新的含氮衍生物6～14.通过1HNMR,IR,MS和元素分析确定了结构.选择口腔底癌(KB)和乳腺癌(MFC-7)两种人癌细胞株,采用标准MTT法测定了这类大黄素衍生物的细胞毒性.研究表明大多数衍生物都有较强的抗癌活性,其中位置异构体7a和7b的混合物表现出最强的活性,与母体大黄素相比较,活性分别提高了174倍(KB)和133倍(MFC-7).

A series of new emodin derivatives 6-14 containing nitrogen atoms have been synthesized.Their structures were established by IH NMR, IR, MS spectra and elemental analyses. The cytotoxicity bioassays of these new emodin derivatives were carried out using the standard MTT method, and most of emodin derivatives showed potent cytotoxicity. The mixture of positional isomers 7a and 7b demonstrated the strongest cytotoxicity activity against the cell line of KB and MCF-7.