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Synthesis, nano-scale assembly, and in vivo anti-thrombotic activity of novel short peptides containing L-Arg and L-Asp or L-Glu
Chen, Yu2; Cui, Guohui1; Zhao, Ming1; Wang, Chao2; Qian, Keduo3; Morris-Natschke, Susan3; Lee, Kuo-Hsiung3; Peng, Shiqi1,2
关键词Asp-arg-peptides Glu-arg-peptides Cu(Ii)-complex Synthesis Self-assembling Anti-thrombotic Activity
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2008-06-01
DOI10.1016/j.bmc.2008.04.064
16期:11页:5914-5925
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]PLATELET-AGGREGATION ; DISEASE ; FABRICATION ; INHIBITION ; MECHANISMS ; THROMBOSIS ; NANOTUBES ; PROTEINS ; FIBERS
英文摘要

Two tripeptides H-Asp(Arg)-Arg (3a) and H-Glu(Arg)-Arg (3b), four pentapeptides H-Asp(Arg-Asp)-Arg-Asp (6a), H-Glu(Arg-Asp)-Arg-Asp (6b), H-Asp(Asp-Arg)-Asp-Arg (10a), and H-Glu(Asp-Arg)-Asp-Arg (10b), and their Cu(II)-peptide complexes Cu(II)-Asp(Arg)-Arg [3a-Cu(II)], Cu(II)-Glu(Arg)-Arg [3b-Cu(II)], Cu(II)-Asp(Arg-Asp)-Arg-Asp [6a-Cu(II)], Cu(II)-Glu(Arg-Asp)-Arg-Asp [6b-Cu(II)], Cu(II)-Asp(Asp-Arg)-Asp-Arg [10a-Cu(II)], and Cu(II)-Glu(Asp-Arg)-Asp-Arg [10b Cu( II)] were designed and synthesized. Their self-assembling properties and in vivo anti-thrombotic activities were investigated. In normal saline (NS), the Cu(II)-peptide complexes assembled into stable nano-particles surrounded by negative charges (-4.102 to -9.825 mV), with diameters ranging from 212.1 +/- 4.0 to 632.4 +/- 36.7 nm. TEM analysis exhibited that the compounds remained as nano-globes in the solid state, with diameters ranging from 15 to 20 nm. In an in vivo anti-thrombotic assay, peptides (3,6,10) a, b at 5 mu mol/kg reduced the thrombus weights of a rat model by 15-40%. Aspirin, a widely used anti-thrombotic drug, achieved comparable activity in this model system at a dosage of ca. 110 mu mol/kg. The required dosage of Cu(II)-peptide complexes [(3,6,10) a, b]-Cu(II), which assemble into stable nano-particles, was significantly reduced to 0.05 mu mol/kg. Therefore, the antithrombotic activity of the nano-particles [(3,6,10) a, b] -Cu(II) increased dramatically by 100-fold over that of the corresponding peptides. (C) 2008 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000256378200009
引用统计
被引频次:8[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/55240
专题北京大学药学院
作者单位1.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
3.Univ N Carolina, Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA
推荐引用方式
GB/T 7714
Chen, Yu,Cui, Guohui,Zhao, Ming,et al. Synthesis, nano-scale assembly, and in vivo anti-thrombotic activity of novel short peptides containing L-Arg and L-Asp or L-Glu[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(11):5914-5925.
APA Chen, Yu.,Cui, Guohui.,Zhao, Ming.,Wang, Chao.,Qian, Keduo.,...&Peng, Shiqi.(2008).Synthesis, nano-scale assembly, and in vivo anti-thrombotic activity of novel short peptides containing L-Arg and L-Asp or L-Glu.BIOORGANIC & MEDICINAL CHEMISTRY,16(11),5914-5925.
MLA Chen, Yu,et al."Synthesis, nano-scale assembly, and in vivo anti-thrombotic activity of novel short peptides containing L-Arg and L-Asp or L-Glu".BIOORGANIC & MEDICINAL CHEMISTRY 16.11(2008):5914-5925.
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