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Holotransferrin Enhances Selective Anticancer Activity of Artemisinin against Human Hepatocellular Carcinoma Cells 被引量:5
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作者 邓小荣 刘朝霞 +6 位作者 刘峰 潘雷 余和平 姜进平 张建军 刘立 喻军 《Journal of Huazhong University of Science and Technology(Medical Sciences)》 SCIE CAS 2013年第6期862-865,共4页
Artemisinin, also termed qinghaosu, is extracted from the traditional Chinese medicine ar- temesia annua L. (the blue-green herb) in the early 1970s, which has been confirmed for effectively treating malaria, Additi... Artemisinin, also termed qinghaosu, is extracted from the traditional Chinese medicine ar- temesia annua L. (the blue-green herb) in the early 1970s, which has been confirmed for effectively treating malaria, Additionally, emerging data prove that artemisinin exhibits anti-cancer effects against many types of cancers such as leukemia, melanoma, etc. Artemisinin becomes cytotoxic in the presence of ferrous iron. Since iron influx is high in cancer cells, artemisinin and its analogs selectively kill can- cer cells with increased intracellular iron concentrations. This study is aimed to investigate the selective inhibitory effects of artemisinin on SMMC-7721 cells in vitro and determine the effect of holotransfer- fin, which increases the concentration of ferrous iron in cancer cells, combined with artemisinin on the anticancer activity. MTT assay was used for assessing the proliferation of SMMC-7721 cells treated with artemisinin. The induction of apoptosis and inhibition of colony formation in SMMC-7721 cells treated with artemisinin were determined by TdT-mediated dUTP nick end labeling (TUNEL) and col- ony formation assay, respectively. The results showed that artemisinin at various concentrations signifi- cantly inhibited growth, colony formation and cell viability of SMMC-7721 cells (P〈0.05), likely due to induction of apoptosis of SMMC-7721 cells. Of interest, it was found that incubation of artemisinin combined with holotransferrin sensitized the growth inhibitory effect of artemisinin on SMMC-7721 cells (P〈0.01). Our data suggest that treatment with artemisinin leads to inhibition of viability and pro- liferation, and apoptosis of SMMC-7721 ceils. Furthermore, we observed that holotransferrin signifi- cantly enhanced the anti-cancer activity of artemisinin. This study may provide a potential therapeutic choice for liver cancer. 展开更多
关键词 human hepatocellular carcinoma SMMC-7721 cells ARTEMISININ holotransferrin cell growth colony formation APOPTOSIS
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二氢青蒿素下调粒系白血病细胞转铁蛋白受体表达 被引量:8
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作者 王增 周慧君 《药学学报》 CAS CSCD 北大核心 2008年第6期576-583,共8页
通过建立常铁HL60和K562细胞以及富铁K562细胞体外模型,研究二氢青蒿素对粒系白血病细胞转铁蛋白受体(transferrin receptor,TfR)的调控作用。采用流式细胞术检测二氢青蒿素对粒系白血病细胞TfR密度的调控作用,Western blotting和RT-PC... 通过建立常铁HL60和K562细胞以及富铁K562细胞体外模型,研究二氢青蒿素对粒系白血病细胞转铁蛋白受体(transferrin receptor,TfR)的调控作用。采用流式细胞术检测二氢青蒿素对粒系白血病细胞TfR密度的调控作用,Western blotting和RT-PCR法检测二氢青蒿素对粒系白血病细胞TfR表达的调控作用,原子吸收分光光度法检测二氢青蒿素对常铁和富铁K562细胞铁含量的影响,以及MTT法和台盼蓝拒染法分析二氢青蒿素对粒系白血病细胞增殖的作用。结果显示,二氢青蒿素能显著降低常铁HL60和K562细胞TfR的密度和下调TfR蛋白的表达,且呈浓度和时间依赖性,并能有效地抑制细胞增殖,IC50值分别为1.74和11.33μmol.L-1。二氢青蒿素对富铁K562细胞的TfR蛋白和mRNA表达能进一步增强下调作用,与常铁培养组比较,10μmol.L-1二氢青蒿素对富铁K562细胞TfR蛋白和TfR mRNA表达量分别下调了28.1%(P<0.01)和26.2%(P<0.05),并能显著下降富铁K562细胞铁的含量(P<0.05),更有效地抑制富铁K562细胞增殖。由此可见,二氢青蒿素能下调粒系白血病细胞TfR密度以及TfR蛋白和mRNA的表达,有效抑制常铁HL60和K562细胞的增殖,对富铁K562细胞增殖的抑制作用能进一步增强。 展开更多
关键词 二氢青蒿素 转铁蛋白受体 K562细胞 HL60细胞 铁饱和转铁蛋白
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转铁蛋白偶联双氢青蒿素氧基苯甲酰肼的载药量分析 被引量:2
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作者 黄连喜 曾鑫 +1 位作者 蔡怀鸿 杨培慧 《分析化学》 SCIE EI CAS CSCD 北大核心 2008年第7期983-986,共4页
在含20%乙醇的B-R缓冲溶液(V/V,pH=7.2)中,利用电分析化学方法测得双氢青蒿素氧基苯甲酰肼(dihydroartemisininoxy benzoic acid hydrazide,DBAH)在银电极上于-0.66V(vs.SCE)处有一不可逆还原峰。DBAH与被高碘酸钠氧化后的转铁蛋白(holo... 在含20%乙醇的B-R缓冲溶液(V/V,pH=7.2)中,利用电分析化学方法测得双氢青蒿素氧基苯甲酰肼(dihydroartemisininoxy benzoic acid hydrazide,DBAH)在银电极上于-0.66V(vs.SCE)处有一不可逆还原峰。DBAH与被高碘酸钠氧化后的转铁蛋白(holotransferrin,Tf)结合形成电活性复合物,其还原峰峰电位由-0.16V负移至-0.84V,峰电流随DBAH和Tf浓度的增加而增加。该法测得一个Tf分子可以与3个DBAH分子连接,其结合常数为5.1×1010。紫外可见吸收光谱法测定结果与电化学测定结果相吻合。实验结果表明,Tf与DBAH共价结合形成电活性复合物。 展开更多
关键词 双氢青蒿素氧基苯甲酰肼 转铁蛋白 电分析化学 载药量
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