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学科主题: 药学
题名:
Coordination of thrombolytic Pro-Ala-Lys peptides with Cu (II): Leading to nanoscale self-assembly, increase of thrombolytic activity and additional vasodilation
作者: Ren, Xue1; Cui, Guohui2; Zhao, Ming2; Wang, Chao1; Peng, Shiqi1,2
刊名: JOURNAL OF PHYSICAL CHEMISTRY B
发表日期: 2008-07-10
DOI: 10.1021/jp800645g
卷: 112, 期:27, 页:8174-8180
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Physical
研究领域[WOS]: Chemistry
关键词[WOS]: BLOOD-FLOW ; PENTAPEPTIDE ; FABRICATION ; COMPLEXES ; PROTEINS ; ANALOGS ; FIBRIN ; P6A
英文摘要:

Vasodilation is one of the biologically important properties for thrombolytic agents because of it may help thrombolysis via dilating blood vessels. Aimed at discovering agents with the dual-action of vasodilative and thrombolytic activities, H-Pro-Ala-Lys (PAK, 3a) and five novel analogs H-Pro-Ala-AA (2b-f, AA = Val, Phe, Ser, Glu, and His) were coordinated with Cu(II) to form Cu(II)-Pro-Ala-AA [(3a-f)-Cu(II)]. The coordination chemistry was confirmed by the d-d transition occurred in their UV and circular dichroism (CD) spectra and the molecular ion in their electrospray ionization mass spectrometry (ESI-MS) spectra. The particle size tests of their solution and powders revealed that the coordination generally resulted in nanoscale self-assembly. Zeta potential and half-peak width tests indicated that the formed nanoparticles were sufficiently stable during the monitored 8 days. The bioassays implied that comparing to the PAK peptides themselves and CuCl(2) the coordination led to a 3000-fold increase of the in vitro thrombolytic activity, a 10-fold increase of the in vivo thrombolytic activity, and especially an additional vasodilation. Thus Cu(II)-peptide coordination indeed is a way for thrombolytic peptide design.

语种: 英语
WOS记录号: WOS:000257335200029
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59627
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China

Recommended Citation:
Ren, Xue,Cui, Guohui,Zhao, Ming,et al. Coordination of thrombolytic Pro-Ala-Lys peptides with Cu (II): Leading to nanoscale self-assembly, increase of thrombolytic activity and additional vasodilation[J]. JOURNAL OF PHYSICAL CHEMISTRY B,2008,112(27):8174-8180.
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