柚皮素衍生物的合成及抗肿瘤活性

Synthesis and anti-tumor activity of naringenin derivatives

目的:合成甲基化柚皮素和乙酰化柚皮素,并测定其抗肿瘤活性。方法:以柚皮素为原料,碘甲烷为甲基化试剂,乙酸酐为酰化试剂,制备目标物;IR、ESI-MS1、H-NMR确证目标物结构;噻唑蓝(MTT)法测定抗肿瘤活性。结果:目标物确证为7,4′-二甲基柚皮素和5,7,4′-三乙酰柚皮素,其对人源肝肿瘤细胞SMMC-CTT 21的抑制率分别为7.60%和4.10%。结论:7,4′-二甲基柚皮素和5,7,4′-三乙酰柚皮素无抑制肿瘤细胞生长的作用。

Objective：To synthesize methylnaringenin,acetylnaringenin and study their anti-tumor activities.Methods： The target compounds were synthesized by methylation and acetylation,iodomethane as methylated reagent,acetic anhydride as acylated reagent.The structure were confirmed through IR,ESI-MS and 1H-NMR;their anti-tumor activities were determined by the method of MTT.Results： 7,4′-dimethylnaringenin and 5,7,4′-tri-acetyl naringenin were identified and their inhibition rate to SMMC-CTT21is7.60% and 4.10% respectively.Conclusion： 7,4′-dimethylnaringenin and 5,7,4′-tri-acetyl naringenin have no anti-tumor activity.