Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins

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Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins

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- Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins
- 阴离子卟啉对DNA转录和端粒酶抑制的研究
- Vol. 30, Issue 4, Pages: 354-358(2009)
- 作者机构：
  
  忻州师范学院化学系
- 作者简介：
- 基金信息：
- DOI：
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- Published：2009
- 稿件说明：
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翟保评. Study on DNA Transcription and Telomerase Inhibition of Anionic Porphyrins[J]. 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.

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references

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