阴离子卟啉对DNA转录和端粒酶抑制的研究

翟保评

您当前的位置：

首页 >

文章列表页 >

阴离子卟啉对DNA转录和端粒酶抑制的研究

化工与环境工程 | 更新时间：2026-09-14

- 阴离子卟啉对DNA转录和端粒酶抑制的研究
- Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins
- 中北大学学报（自然科学版） 2009年30卷第4期页码：354-358
- 作者机构：
  
  忻州师范学院化学系
- 作者简介：
- 基金信息：
  
  山西省教育厅科技开发资助项目(200811046);忻州师范学院级院基金资助项目
- DOI：
  中图分类号：
- 纸质出版：2009
- 稿件说明：
移动端阅览
翟保评. 阴离子卟啉对DNA转录和端粒酶抑制的研究[J]. 中北大学学报（自然科学版）, 2009,30(4):354-358.

翟保评. Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins[J]. 2009, 30(4): 354-358.
翟保评. 阴离子卟啉对DNA转录和端粒酶抑制的研究[J]. 中北大学学报（自然科学版）, 2009,30(4):354-358. DOI：

翟保评. Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins[J]. 2009, 30(4): 354-358. DOI：

摘要

新型抗肿瘤药物的设计是当今化学生物学中发展迅速且具有挑战性的研究领域之一

阴离子卟啉有着比阳离子卟啉更好的膜通透性.利用合成的阴离子卟啉化合物1

2和3

通过凝胶电泳和端粒酶重复序列扩增法(TRAP)

研究了药物对DNA转录成为RNA和它们对端粒酶的抑制作用.实验结果表明:阴离子卟啉化合物1

2和3均可抑制DNA的转录和端粒酶的活性

其中化合物2的抑制作用尤为显著

其完全抑制的浓度分别为5μmol/L和3μmol/L

这与化合物2β-位所连8个强拉电子的溴原子所导致的整个分子的缺电子性有关.

Abstract

The design and synthesis of new antitumor drugs is one of the most challenging and rapid developing subjects in the field of chemical biology.The negatively charged porphyrins are more membrane permeable than cation porphyrins

so the transcription from DNA to RNA and telomerase inhibition of the anionic porphyrins compounds 1

and 3 are investigated with gel electrophoretic experiment and telomerase repeat amplification protocol assay(TRAP).It is found that all the compounds can exert effect on telomerase and inhibit the transcription

the inhibiting activity of the compound 2 is more prominent

and the inhibition concentration of the drugs is entirely 5 μmol/L and 3 μmol/L

respectively.The outstanding inhibiting ability of the compound 2 might be attributed to the electron-deficient property of the molecule resulted from the strong electron-withdrawing effect of the eight bromine atoms at β-positions.

关键词

Keywords

references

Fiel R J,Howard J C,Mark E H,et al.Interaction of DNA with a porphyrin ligand:Evidence for intercalation[J].Nucleic Acids Res.,1979,6:3093-3118.

He H P,Zhou Y,Liang F,et al.Combination of porphyrins and DNA-alkylation agents:Synthesis and tumor cellapoptosis induction[J].Bioorg.Med.Chem.,2006,14:1068-1077.

Hartman T,Carlsson J.Radiation dose heterogeneity in receptor and antigen mediated boron neutron capture therapy[J].Radiother.Oncol.,1994,31:61-75.

Hartman T,Lundqvist H,Westlin J E,et al.Radiation doses to the cell nucleus in single cells and cells inmicrometastases in targeted therapy with I-131 labeled ligands or antibodies[J].Int.J.Radiat.Oncol.,Biol.Phys.,2000,46:1025-1036.

Krishnamurthy P C,Du G,Fukvda Y,et al.Identification of a mammalian mitochondrial porphyrin transporter[J].Nature,2006,443:586-589.

Kessel D,Thompson P,Aatio S K,et al.Tumor localization and photosensitization by sulfonated derivatives oftetraphenylporphine[J].Photochem.Photobiol.,1987,45:787-790.

Berg K,Prydz K,Moan J.Photochemical treatment with the lysosomally localized dye tetra(4-sulfonatophenyl)porphine results in lysosomal release of the dye but not of a-N-acetyl-Dglucosamidase activity[J].Biochim.Biophys.Acta,1993,1158:300-306.

Kessel D,Oodburn W K.Biodistribution of photosensitizing agents[J].Int.J.Biochem.,1993,25:1377-1383.

Zhai B P,Shuai L,Yang L,et al.Octa-substituted anionic porphyrins:topoisomerase I inhibition and tumor cellapoptosis induction[J].Bioconj.Chem.,2008,19(8):1535-1542.

Patty F K L,Claudia T.Transcription inhibition by Rh(phi)2(phen)3[J].Chem.Commun.,2001:279-280.

萨姆布鲁克J,拉塞尔D W著.分子克隆实验指南[M].黄培堂译.北京:科学出版社,2002.

Chatterjee S R,Shetty S J,Devasagayam T P A,et al.Photocleavage of plasmid DNA by the porphyrin meso-tetrakis[4-(carboxymethyleneoxy)phenyl]porphyrin[J].Photochem.and Photobio.B:Biology,1997,41:128-135.

Kim N W,Piatyszek M A,Prowse K R,et al.Specific association of human telomerase activity with immortal cellsand cancer[J].Science,1994,266:2011-2015.

Royle N J.Telomerase and disease[J].J.Pathol.,1996,180:233-235.

Counter C M,Gupta J,Harley C B.Telomerase activity in normal leukocytes and in hematologic malignancices[J].Blood,1995,85:2315-2320.

Grinstaff M W,Hill M G,Labinger J A,et al.Mechanism of catalytic oxygenation of alkanes by halogenated ironporphyrins[J].Science,1994,264:1311-1313.

浏览量

214

下载量

CSCD

文章被引用时，请邮件提醒。

提交

工具集

关联资源

基于机器学习的复合材料结构设计与性能表征研究进展

基于低分子质量PEI的类PEG聚合物基因载体

面向高空爆炸试验的冲击波测试系统

基于Transformer⁃FPGA协同特征建模的光电坐标高精度定位技术

基于元学习与VAE⁃GAN的META⁃VAEGAN⁃DNN网络入侵检测方法