雷公藤红素对人肺癌A549细胞增殖活性及能量代谢的影响  

Effect of celastrol on proliferation and energy metabolism of human lung cancer A549 cell line

作　　者：王淑静[1] 訾庆雪 付玉 刘琳[1] 张文君[1] 张家宁[1] WANG Shujing;ZI Qingxue;FU Yu;LIU Lin;ZHANG Wenjun;ZHANG Jianing(College of Pharmacy,Harbin University of Commerce,Harbin,150076,China)

机构地区：[1]哈尔滨商业大学药学院,黑龙江哈尔滨150076

出　　处：《药学研究》2020年第5期266-268,298,共4页Journal of Pharmaceutical Research

基　　金：哈尔滨商业大学研究专项基金资助(No.18XN049)。

摘　　要：目的探究雷公藤红素对人肺癌细胞(A549)的增殖活性以及能量代谢的影响。方法噻唑蓝(MTT)法和生长曲线检测雷公藤红素对细胞的增殖抑制情况;HE染色观察细胞形态变化;分光光度法测定糖酵解途径中己糖激酶(HK)、丙酮酸激酶(PK)、乳酸脱氢酶(LDH)活力和三羧酸循环中琥珀酸脱氢酶(SDH)活力及能量代谢终产物ATP的含量。结果雷公藤红素对A549细胞有增殖抑制作用,浓度在2μg·mL-1时,对A549细胞的抑制率达到62.71%,远远大于阳性药组5-FU的抑制率;生长曲线结果显示,雷公藤红素作用第4天细胞浓度最低,第6天细胞抑制程度最明显;HE结果表明雷公藤红素处理48 h后,细胞形态变圆,体积缩小,核深染且颜色变深;试剂盒检测结果显示,雷公藤红素非常显著的降低乳酸脱氢酶酶活力(P<0.01),显著降低琥珀酸脱氢酶活力和ATP含量均显著降低(P<0.05),但对己糖激酶和丙酮酸激酶无明显作用。结论雷公藤红素能够显著降低人肺癌A549细胞中乳酸脱氢酶和琥珀酸脱氢酶的活力,干扰能量代谢,抑制能量ATP生成,达到抑制A549细胞增殖的作用。Objective To investigate the effects of celastrol on proliferation and energy metabolism of human lung cancer cells( A549).Methods In the current study,growth curves and MTT assays were performed to determine the effects of celastrol in human lung adenocarcinoma cells( A549);Changes in morphology were observed using hematoxylin and eosin( HE) staining.The activities of HK,PK and LDH enzymes in the glycolysis.The activities of key enzymes tricarboxylic acid cycle were measured using spectrophotometry.The content of ATP was measured using spectrophotometry.Results Celastro inhibited cell proliferation in A549 cells. At a concentration of 2 μg · m L-1,the inhibition rate of A549 cells reached62.71%,which was more effective than the 5-FU inhibition rate;The growth curve results showed that celastrol had the lowest cell concentration on the fourth day and the most obvious cell inhibition on the sixth day. HE staining suggested that celastrol induced cell morphology changes,reduced volume,deep stained nuclei and darker colors. Celastrol group significantly reduced LDH( P<0.01);Celastrol significantly reduced SDH activity and ATP content( P<0.05),but had no significant effect on HK and PK. Conclusion Celastrol can significantly reduce the activity of LDH and SDH in human lung cancer A549 cells,interfere with energy metabolism,inhibit energy ATP generation and inhibit the proliferation of A549 cells.

关 键 词：雷公藤红素 人肺癌A549 能量代谢 细胞增殖 

分 类 号：R285.5[医药卫生—中药学]