马蔺子甲素体外抗癌及其诱导白血病细胞K562凋亡的作用  

In Vitro Anticancer Effects of Pallasone A and Its Induced Apoptosis on Leukemic K562 Cells

作　　者：张富赓[1,2] 李德华[3] 齐静[4] 刘昌孝[5] 

机构地区：[1]天津中医药大学,天津300193 [2]天津市环湖医院药剂科,天津300060 [3]天津市医药科学研究所,天津300020 [4]中国医学科学院血液病研究所,天津300020 [5]释药技术与药代动力学国家重点实验室,天津药物研究院,天津300193

出　　处：《中国药学杂志》2010年第22期1716-1719,共4页Chinese Pharmaceutical Journal

基　　金：科技部重大新药创制专项基金(2009ZX09304)

摘　　要：目的研究马蔺子甲素体外抗癌及其诱导白血病细胞K562凋亡的作用。方法采用四氮唑蓝(MTT)法检测马蔺子甲素对白血病K562和阿霉素耐药株K562/AO2、白血病HL-60、肺癌GLC-82、肝癌BEL-7402、胃腺癌BGC-823、神经母细胞瘤LA-N-5、星型胶质瘤TJ-905、骨肉瘤MG-639种人癌细胞株的IC50;应用荧光显微镜、电镜和流式细胞术的方法检测马蔺子甲素诱导K562细胞凋亡的作用,并采用流式细胞仪检测其凋亡百分率和细胞周期。结果马蔺子甲素对9种人癌细胞株作用72h,IC50均在26.70nmol.mL-1(10.0μg.mL-1)以下;马蔺子甲素终浓度8.01nmol.mL-1(3.0μg.mL-1)与K562细胞共培养72h,电镜和荧光镜下明显可见细胞形态学呈凋亡特征样改变,流式细胞仪检测其凋亡率为(20.36±1.41)%,与对照组比较统计学差异有显著性;马蔺子甲素终浓度2.67nmol.mL-1(1.0μg.mL-1)也具有诱导K562细胞凋亡的作用。马蔺子甲素作用后,K562细胞G0/G1期显著升高,S期细胞则显著降低,细胞周期被阻断在G0/G1期。结论马蔺子甲素对多种人癌细胞株具有显著的体外抗癌活性,并能诱导白血病细胞K562凋亡。OBJECTIVE To investigate the in vitro anticancer effects of pallasone A and its induction on apoptosis of leukemic K562 cells.METHODS Nine kinds of human cancer cells,including leukemic K562,adriamycin resistance K562/AO2,leukemia HL-60,pulmonary cancer GLC-82,hepatocarcinoma BEL-7402,gastric adenocarcinoma BCG-823,neuroblastoma LA-N-5,astroglioma TJ-905 and osteosarcoma MG-63,were used in cytotoxicity tests with MTT method.The apoptosis and cell cycles of K562 cells were assessed by flow cytometry,and cell morphology was observed with fluorescent and electron microscopes.RESULTS The IC50 of pallasone A（72 h exposure）on nine cancer cell lines was less than 26.70 nmol·mL-1（10.0 μg·mL-1）.The apoptosis of K562 cells induced by pallasone A was proved on the methods of fluorescent and electron microscopes and flow cytometry.The apoptotic percentage of K562 exposed with pallasone A 8.01 nmol·mL-1（3.0 μg·mL-1）for 72 h was（20.36±1.41）%,which was significantly different with that of control,the pallasone A 2.67 nmol·mL-1（1.0 μg·mL-1）group also statistically different from the control group.Pallasone A influenced the cell cycle of K562,and the proportion of cells with pallasone A in G0/G1 phase was more than that of control cells,but less in S phase significantly.CONCLUSION Pallasone A has anticancer activity in vitro broadly and be able to induce apoptosis of leukemic cell K562.

关 键 词：抗癌 细胞凋亡 马蔺子甲素 

分 类 号：R965[医药卫生—药理学]