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具有末端胺基的 Xenorhabdus innexi 衍生的 Rhabdopeptide/Xenortide 样肽具有很强的抗原生动物活性。

Rhabdopeptide/Xenortide-like Peptides from Xenorhabdus innexi with Terminal Amines Showing Potent Antiprotozoal Activity.

机构信息

Molekulare Biotechnologie, Fachbereich Biowissenschaften , Goethe Universität Frankfurt , 60438 Frankfurt am Main , Germany.

Institute of Botany, Jiangsu Province and Chinese Academy of Sciences , 210014 Nanjing , China.

出版信息

Org Lett. 2018 Sep 7;20(17):5116-5120. doi: 10.1021/acs.orglett.8b01975. Epub 2018 Aug 10.

Abstract

Seven new rhabdopeptide/xenortide-like peptides (RXPs) (1-7) with putrescine or ammonia as the C-terminal amines were isolated from Xenorhabdus innexi DSM 16336. Their chemical structures were elucidated by high-resoultion mass spectroscopy (HR-MS) and one-dimensional (1D) and two-dimensional (2D) NMR. They were evaluated for their activities against protozoan parasites and cytotoxicity against rat skeletal myoblasts (L6 cells). All tested compounds exhibited strong effects against Trypanosoma brucei rhodesiense and Plasmodium falciparum, with IC values of 0.07-6.25 and 0.091-3.16 μM, respectively, making them the most active RXP derivatives known to date.

摘要

从 Xenorhabdus innexi DSM 16336 中分离到了 7 种新的 Rhabdopeptide/xenortide 样肽 (RXPs) (1-7),它们的 C 末端胺是腐胺或氨。通过高分辨率质谱 (HR-MS) 和一维 (1D) 和二维 (2D) NMR 确定了它们的化学结构。评估了它们对原生动物寄生虫的活性和对大鼠成肌细胞 (L6 细胞) 的细胞毒性。所有测试的化合物对布氏锥虫和恶性疟原虫均表现出很强的活性,IC 值分别为 0.07-6.25 和 0.091-3.16 μM,是迄今为止已知的最活跃的 RXP 衍生物。

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