山柰酚衍生物的合成和细胞毒性研究(英文)

Synthesis and cytotoxicity of kaempferol derivatives

本研究报道一个简单的山柰酚结构修饰方法, 该方法采用不同的条件最终得到1个新化合物3,5-dihydroxy-2-(4-hydroxyphenyl)-6,8,8-tris(3-methylbut-2-en-1-yl)-4H-chromene-4,7(8H)-dione (5)和3个已知化合物8-异戊烯基山柰酚(2)、6-异戊烯基山柰酚(3)、6,8-二异戊烯基山柰酚(4)。所有的衍生物均是首次合成, 根据它们的核磁和质谱数据进行了结构鉴定。化合物2、3和5对MDA-231 (IC_(50)值分别为9.45±0.20 μM、7.15±0.37 μM和6.92±0.30 μM和MCF-7 (IC_(50)值分别为10.08±0.57 μM、10.04±0.23 μM和2.15±0.20 μM)两种人乳腺癌细胞株表现出显著的细胞毒性。

Abstract： In the present study, we developed a simple approach for the structural modifications ofkaempferol （1）. A new compound, 3,5-dihydroxy-2-（4-hydroxyphenyl）-6,8,8-tris（3-methylbut-2-en-1-yl）-4H-chromene-4,7（SH）-dione （5） together with three known compounds, 8-prenylkaempferol （Z）, 6-prenylkaempferol （3） and 6,8-diprenylkaempferol （4）, were synthesized under different reaction conditions. All of derivatives were synthesized in a structural modification way for the first time. Their structures were primarily elucidated by NMR and MS analyses. Compounds 2, 3 and 5 exhibited prominent cytotoxic activity against MDA-231 （IC50 values were 9.45±0.20 μM, 7.15±0.37 μM and 6.92±0.30 μM, respectively） and MCF-7 （ICso values were 10.08±0.57 0M, 10.04±0.23 μM and 2.15±0.20 μM, respectively） breast cancer cells.