摘要
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 。
Objective Searching more potent and less toxic HMBA\|derivative. Methods Human erythroleukemia cell line K562,murine erythroleukemia cell line (MEL) and its sub\|line MEL DS19 were chosen as target cells to select a cell line which is the most sensitive to HMBA,then analyzed the differentiation inducing capacity of two new HMBA derivatives:HMBPA [hexamethylenebi(3\|pyridin) amide] and Co\|HDTA(ethylenediaminetera aceticacid cobalt) using cytochemical,cell and molecular biology techniques. Results The MEL DS19 cells present most sensitive to HMBA (Benzidine positive,B\++76%).Co\|HDTA can inhibite the growth of MEL DS19,but induces differetiation just in a little population(B\++2%\|4 5%).Between 0\^02\|5?μmol/L HMBPA induces 3%\|8% cells committed to differentiation with little inhibition of cell proliferation.1?μmol/L HMBPA plus 2 mmol/L HMBA can increase the percentage of differentiated cells (B\++72%),inhibit DNA synthesis and accelerate β globin transcription. Conclusion The new HMBA derivatives could be used as potential cancer differentiation inducers.\;[
出处
《解剖学报》
CAS
CSCD
北大核心
2001年第3期246-250,共5页
Acta Anatomica Sinica
基金
国家自然科学基金资助项目 (3 9870 893 )
