摘要
（Ｓｐ）－８－氯腺苷－３＇，５＇－环磷酸辛酯（Ｓｐ－ｏｃｔｙｌ８－ｃｈｌｏｒｏａｄｅｎｏｓｉｎｅ３＇，５＇－ｃｙｃｌｏｐｈｏｓｐｈａｔｅ，ＯＣＣ）对人白血病ＨＬ－６０细胞有生长抑制和分化诱导作用，该作用与ＯＣＣ浓度和处理时间呈正相关，为不可逆性。流式细胞光度术发现，ＯＣＣ阻断ＨＬ－６０细胞周期于Ｇ１期。参入实验证实，ＯＣＣ对ＨＬ－６０细胞ＤＮＡ合成有显著抑制作用，但不影响ＲＮＡ和蛋白质合成。ＯＣＣ能直接激活ＨＬ－６０细胞浆中提取的蛋白激酶Ａ（ＰＫＡ），并抑制它与ｃＡＭＰ的结合。经ＯＣＣ处理的ＨＬ－６０细胞浆中ＰＫＡ活性明显升高，说明ＯＣＣ能与ｃＡＭＰ竞争ＰＫＡ的结合并激活ＰＫＡ。
Sp)- octyl 8-chloroadenosine 3',5'-cyclophosphate(OCC),a newly synthesizedcAMP analog,strongly induced growth inhibition and differentiation in human leukemia HL-60 cells。The effects were dose and time-dependent and irreversible,In flow cytometry,OCC brought about ablock at the Gl phase of HL-60 cell cycle,Determined by incorporation assay,OCC was shown tostrongly inhibit DNA synthesis without affecting the synthesis of RNA and protein in HL-60 cells.OCC activated the protein kinase A(PKA)in the cytosol of HL-60 cells and inhibited its binding tocAMP,The activities of PKA in the cytosol of HL-60 cells treated with OCC were more significantlyincreased than those in control cells.It can be concluded that OCC binds itself to PKA in competitionwith cAMP and,as a result,activates PKA。
出处
《药学学报》
CAS
CSCD
北大核心
1996年第9期641-646,共6页
Acta Pharmaceutica Sinica
关键词
环磷酸辛酯
OCC
白血病
cAMP类似物
诱导分化
Sp)- Octyl 8-chloroadenosine 3',5'-cyclophosphate,Induced differentiation
Proteinkinase A
HL-60 cells
cAMP analogues
