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目的 寻找新的、更有效、低毒的六亚甲基双乙酰胺 (HMBA)衍生物。 方法 以人红白血病细胞(K5 6 2 ) ,小鼠红白血病细胞 (MEL)及其亚株MELDS19为靶细胞 ,筛选并比较新合成的HMBA衍生物———HMBPA[N ,N’六亚甲基双 (3吡啶 )酰胺 ]与 1,6乙二胺四乙酸钴 (Co HDTA)的诱导分化活性。 结果 MELDS19细胞株对HMBA最敏感 ,联苯胺染色阳性率 (B+ )可达 76 %。Co HDTA有一定的抑制细胞增殖作用及微弱的诱导分化活性(B+ 2 %～ 4 5 % ) ,有效浓度为 0 5mmol L ,HMBPA在 0 0 2～ 5 μmol L的浓度范围内也有较低的诱导活性 (B+ 3%～8% ) ,低浓度HMBPA与HMBA(2mmol L)联合应用 ,则可明显提高诱导分化活性 (B+ 72 % ) ,其诱导活性与 5mmol LHMBA及 1 6 %DMSO接近。 结论 HMBPA与Co HDTA对MEL细胞具有诱导分化活性 ,HMBPA与HMBA有协同诱导分化作用
Aim To find new, more effective and less toxic hexamethylene bisacetamide (HMBA) derivatives. Methods Human erythroleukemia cells (K5 6 2), mouse erythroleukemia cells (MEL) and their subline MELDS19 were selected as target cells. The new synthesized HMBA derivatives, HMBPA [N, N ’ (3-pyridyl) amide] and 1,6-ethylenediaminetetraacetic acid (Co HDTA). Results The MELDS19 cell line was the most sensitive to HMBA, and the positive rate of benzidine staining (B +) was 76%. Co HDTA had a certain inhibitory effect on cell proliferation and weak differentiation (B + 2% ~ 45%) with an effective concentration of 0 5 mmol L, and HMBPA also had lower induction at a concentration range of 0 0 2 ~ 5 μmol L (B + 3% ~ 8%), low concentration HMBPA combined with 2 mmol L HMBA could significantly enhance the differentiation activity (B + 72%), and its induction activity was close to that of 5mmol LHMBA and 16% DMSO. Conclusion HMBPA and Co HDTA can induce differentiation of MEL cells and HMBPA and HMBA can induce differentiation