首页|新型塔斯品碱衍生物HMQ-T-B10诱导人结肠癌细胞LoVo凋亡作用及机制研究

新型塔斯品碱衍生物HMQ-T-B10诱导人结肠癌细胞LoVo凋亡作用及机制研究

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探讨塔斯品碱衍生物HMQ-T-B10对人结肠癌LoVo细胞生长的影响及其诱导细胞凋亡的可能作用机制。采用MTT法、细胞克隆形成实验、Hoechst染色法、流式细胞术法检测低(2 µmol/L)、中(4μmol/L)、高(8 μmol/L)3种浓度HMQ-T-B10对LoVo细胞株增殖及凋亡的影响;Western-Blot法检测3种浓度HMQ-T-B10对Bcl-2、Mcl-1、Bax、Cyto-C、Cleaved caspase-3、Cleaved caspase-7 蛋白表达水平的影响。MTT 法结果显示 HMQ-T-B10能明显抑制LoVo细胞的增殖,其半数抑制浓度(IC50)值为(7。9±1。1)μmol/L。细胞克隆形成实验表明3种浓度的HMQ-T-B10均可剂量依赖性抑制LoVo细胞增殖,Hoechst染色及流式细胞术显示HMQ-T-B10可剂量依赖性诱导LoVo细胞凋亡。Western-Blot结果显示4 μmol/L及8μmol/L HMQ-T-B10可显著下调Bcl-2蛋白表达并增加Cyto-C表达,3种浓度的HMQ-T-B10均可显著抑制Mcl-1蛋白表达并升高Bax及Cleaved caspase-7表达,8 μmol/L HMQ-T-B10可显著性增加Cleaved caspase-3表达。HMQ-T-B10可抑制LoVo细胞增殖,可能通过Bcl-2/Caspase通路诱导其凋亡。
Study of Apoptosis-inducing Effects and Underlying Mechanism of New Taspine Derivative HMQ-T-B10 in Human Colorectal Carcinoma LoVo Cells
To investigate the inhibitory effects of taspine derivatives HMQ-T-B10 and the possible mechanism of inducing apoptosis on human colorectal carcinoma LoVo cells,MTT assay and cell clone formation assay were used to detect the effects of low(2 μmol/L)concentration group,medium(4 μmol/L)concentration group and high(8 µmol/L)concentration group of HMQ-T-B10 on the pro-liferative of human colorectal carcinoma LoVo cell lines.Hoechst staining method and flow cytometry were used to detect the effects of low,medium and high concentrations group of HMQ-T-B10 on the apoptosis of human colorectal carcinoma LoVo cell lines.Western-Blot assay were used to detect the effects of three concentrations group of HMQ-T-B10 on the protein expression level of Bcl-2,Mcl-1,Bax,Cyto-C,Cleaved caspase-3 and Cleaved caspase-7.MTT assay showed that HMQ-T-B10 could significantly inhibit the proliferation of human colorectal carcinoma LoVo cells lines with half inhibitory concentration(IC50)value of(7.9±1.1)µmol/L,and the cell clone formation assay demonstrated that all the three concentrations group of HMQ-T-B10 could dose-dependently inhibit the proliferation of human colorectal carcinoma LoVo cells.Hoechst staining method and flow cytometry showed that all the three concentrations group of HMQ-T-B10 could dose-dependently induce apoptosis of human colorectal carcinoma LoVo cells.Western-Blot results showed that both 4 µmol/L and 8 μmol/L HMQ-T-B10 concentration group could significantly down-regulate the expression level of Bcl-2 protein and increase the expression level of Cyto-C protein,and that all the three concentrations of HMQ-T-B10 group could significantly inhibit the expression level of Mcl-1 protein and elevate the expression level of Bax protein and Cleaved caspase-7 protein,and 8 μmol/L HMQ-T-B10 concentration group could significantly increas the Cleaved caspase-3 protein expres-sion level.HMQ-T-B10 inhibited the proliferation of human colorectal carcinoma LoVo cells and probably induced apoptosis through the Bcl-2/Caspase pathway.

TaspineHMQ-T-B10Human colorectal carcinoma LoVo cellsProliferationApoptosisBcl-2Caspase

雍素云、张丹、周楠、张鹏、史先鹏

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陕西省人民医院药学部,陕西西安 710068

塔斯品碱 HMQ-T-B10 人结肠癌LoVo细胞 增殖 凋亡 Bcl-2 含半胱氨酸的天冬氨酸蛋白水解酶

陕西省中医药管理局中医药传承创新暨"秦药"重点科学研究项目陕西省人民医院院内人才支持计划项目陕西省自然科学基金青年项目陕西省自然科学基金

2021-02-zz-0152021JY-292023-JC-QN-09362022JM-605

2024

药物生物技术
中国药科大学,中国医药科技出版社,中国药学会

药物生物技术

CSTPCD
影响因子:0.463
ISSN:1005-8915
年,卷(期):2024.31(1)
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