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来自青蟹(Callinectes sapidus)的一种具有心脏活性的FMRF酰胺相关肽的鉴定及其构效关系

The identification and structure-activity relations of a cardioactive FMRFamide-related peptide from the blue crab Callinectes sapidus.

作者信息

Krajniak K G

机构信息

Whitney Laboratory, University of Florida, St. Augustine 32086-8632.

出版信息

Peptides. 1991 Nov-Dec;12(6):1295-302. doi: 10.1016/0196-9781(91)90210-g.

DOI:10.1016/0196-9781(91)90210-g
PMID:1815216
Abstract

The pericardial organs and thoracic ganglia of the blue crab Callinectes sapidus were resected and extracted. The extracts were fractionated by HPLC and the fractions analyzed by a radioimmunoassay (RIA) to FMRFamide. Multiple peaks of immunoreactivity were present and one of these, upon fast atom bombardment mass spectrometry (FAB-ms) and microsequencing, yielded the sequence GYNRSFLRFamide. The amount of this peptide in each crab is between 7 and 13 pmol. Several incomplete sequences were also characterized, suggesting a precursor with multiple copies of peptides related to GYNRSFLRFamide might occur. The peptide caused a dose-dependent increase in heart rate; threshold was 10 to 30 nM, and the EC50 was 323 +/- 62 nM. A structure-activity study of GYNRSFLRFamide on the crab heart suggests that, for full potency, a peptide should be at least a heptapeptide with the sequence XXZFLRFamide, where X is any amino acid and Z is either asparagine or serine.

摘要

切除并提取了青蟹(Callinectes sapidus)的心包器官和胸神经节。提取物通过高效液相色谱法(HPLC)进行分级分离,各分级部分通过放射免疫分析法(RIA)分析FMRF酰胺。存在多个免疫反应峰,其中一个经快速原子轰击质谱法(FAB-ms)和微量测序后,得到序列GYNRSFLRF酰胺。每只螃蟹中这种肽的含量在7至13皮摩尔之间。还鉴定了几个不完整的序列,表明可能存在与GYNRSFLRF酰胺相关的多拷贝肽的前体。该肽引起心率呈剂量依赖性增加;阈值为10至30纳摩尔,半数有效浓度(EC50)为323±62纳摩尔。对青蟹心脏进行的GYNRSFLRF酰胺结构活性研究表明,要达到完全效力,该肽应为至少含XXZFLRF酰胺序列的七肽,其中X为任意氨基酸,Z为天冬酰胺或丝氨酸。

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