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海洋细菌中环四肽的合成与生物筛选研究。

Toward the synthesis and biological screening of a cyclotetrapeptide from marine bacteria.

机构信息

Department of Pharmaceutical Chemistry, NRI Institute of Pharmacy, Bhopal 462 021, Madhya Pradesh, India.

出版信息

Mar Drugs. 2010 Dec 30;9(1):71-81. doi: 10.3390/md9010071.

DOI:10.3390/md9010071
PMID:21339947
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3039471/
Abstract

The first synthesis of a naturally occurring tetrapeptide cyclo-(isoleucyl-prolyl-leucyl-alanyl) has been achieved using a solution-phase technique via coupling of dipeptide segments Boc-L-Pro-L-Leu-OH and L-Ala-L-Ile-OMe. Deprotection of the linear tetrapeptide unit and its subsequent cyclization gave a cyclopeptide, identical in all aspects to the naturally occurring compound. Bioactivity results indicated the antifungal and antihelmintic potential of the synthesized peptide against pathogenic dermatophytes and earthworms.

摘要

首次采用溶液相技术，通过偶联二肽片段 Boc-L-Pro-L-Leu-OH 和 L-Ala-L-Ile-OMe，实现了天然存在的四肽环-(异亮氨酸-脯氨酸-亮氨酸-丙氨酸)的首次合成。线性四肽单元的脱保护及其随后的环化得到了一个环肽，在各个方面都与天然存在的化合物相同。生物活性结果表明，合成肽对致病皮肤真菌和蚯蚓具有抗真菌和抗寄生虫的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2b/3039471/82f00d4586e9/marinedrugs-09-00071f1a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2b/3039471/82f00d4586e9/marinedrugs-09-00071f1a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a2b/3039471/82f00d4586e9/marinedrugs-09-00071f1a.jpg

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