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学科主题: 药学
题名:
Identification, synthesis and bioassay for the metabolites of P6A
作者: Zhao, M; Wang, C; Yang, J; Liu, JY; Xu, YX; Wu, YF; Peng, SQ
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2003-11-17
DOI: 10.1016/j.bmc.2003.09.021
卷: 11, 期:23, 页:4913-4920
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]: ANGIOTENSIN CONVERTING ENZYME ; FIBRINOGEN ; PEPTIDE-6A
英文摘要:

The metabolites Ala-Arg-Pro-Ala-OH, Ala-Arg-Pro-OH, Arg-Pro-Ala-Lys-OH and Pro-Ala-Lys-OH were identified by HPLC/ESI/MS from the in vivo blood of Ala-Arg-Pro-Ala-Lys-OH (M) received mice. The in vitro incubation of P6A in the blood of mice the same metabolites were also found by use of the Prep LC System. The protective intermediates of these metabolites were prepared via the solution method using the stepwise synthesis in 77.4, 90, 88, and 80% yield, respectively. After deprotection with catalytic hydrogenation the intermediates were converted into the corresponding sequences Arg-Pro-Ala-Lys-OH Pro-Ala-Lys-OH, Ala-Arg-Pro-Ala-OH, and Ala-Arg-Pro-OH in 90, 95, 85% and 86% yield, respectively. In the thrombolysis in vivo assay the synthetic Ala-Arg-Pro-Ala-OH, and Ala-Arg-Pro-OH exhibited no activity. On the other hand the thrombolytic activity of Arg-Pro-Ala-Lys-OH was comparable to P6A, and an enhanced thrombolytic activity was observed for Pro-Ala-Lys-OH. In the in vitro fibrinolytic lysis tests the approximate results were obtained and an enhanced activity was also observed for Pro-Ala-Lys-OH. In the euglobulin clot lysis time tests P6A, Arg-Pro-Ala-Lys-OH and Pro-Ala-Lys-OH gave significantly shorter time than that given by UK, demonstrating their fast action. (C) 2003 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000186614400006
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/58554
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Zhao, M,Wang, C,Yang, J,et al. Identification, synthesis and bioassay for the metabolites of P6A[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2003,11(23):4913-4920.
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