18种青黛7-氮杂靛玉红对6种肿瘤细胞增殖的影响

Effects of Eighteen 7-Nitrogen Substituted Indirubin Derivatives on the Proliferation of Six Cancer Cell Lines

本文阐述了利用MTT法测定青黛中18种7-氮杂靛玉红衍生物对6种肿瘤细胞增殖的抑制作用。化合物1~18（1.25~20μmol/L）处理肿瘤细胞72 h后,观测细胞生长抑制作用,分析其结构-疗效关系。结果发现具有相同结构特征即R位上的N-OH基团和R3′位上的B r（C l）基团的化合物10~15可显著抑制6种肿瘤细胞的增殖,与此相反,无此结构特征的化合物1~9的抑制作用大大降低。初步确定,R位上的N-OH基团和R3′位上的B r（C l）基团是7-氮杂靛玉红衍生物抗肿瘤作用的主要活性部位。

Indirubin is an active anticancer component isolated from Qingdai.In this study,effects of eighteen 7-nitrogen substituted derivatives of indirubin on the proliferation of six cancer cell lines were evaluated by MTT assay,and their structure-function relationship was analyzed.After treatment of the cancer cells with compounds 1-18 at concentration range from 1.25 to 20 μmol/L for 72 h,growth inhibitory effects were determined.Results showed that compounds 10-15 with two substitutions,i.e.a N-OH group at the R-position and a bromide or chloride atom replaced H at the R3′-position,could significantly inhibit the proliferation of six human cancer cell lines.However,compounds 1-9 without these substitutions showed relatively lower inhibitory effects.This study suggested that the N-OH group at the R-position and the bromide or chloride atom at the R3′-position might be important for the anti-tumor activities of 7-nitrogen substituted indirubin derivatives.