来自昆虫病原 Xenorhabdus sp. PB61.4 的驱虫查亚菲米。

Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4.

机构信息

Merck Stiftungsprofessur für Molekulare Biotechnologie, Fachbereich Biowissenschaften, Goethe Universität Frankfurt , Max-von-Laue-Straße 9 60438 Frankfurt am Main, Germany.

出版信息

J Nat Prod. 2014 Apr 25;77(4):779-83. doi: 10.1021/np4007525. Epub 2014 Mar 27.

DOI:10.1021/np4007525

PMID:24673206

Abstract

A new class of four depsipentapeptides called chaiyaphumines A-D (1-4) was isolated from Xenorhabdus sp. PB61.4. Their structures were elucidated by detailed 1D and 2D NMR experiments and by a Marfey's analysis following flash hydrolysis of the peptide. Verification of the structure was achieved by three-dimensional modeling using NOE-derived distance constraints, molecular dynamics, and energy minimization. Chaiyaphumine A (1) showed good activity against Plasmodium falciparum (IC50 of 0.61 μM), the causative agent of malaria, and was active against other protozoal tropical disease causing agents.

摘要

从 Xenorhabdus sp. PB61.4 中分离得到了一类称为 chaiyaphumine A-D（1-4）的新型四 depsipentapeptides。通过详细的 1D 和 2D NMR 实验以及肽的快速水解后的 Marfey 分析确定了它们的结构。通过使用 NOE 衍生的距离约束、分子动力学和能量最小化的三维建模来验证结构。chaiyaphumine A（1）对引起疟疾的疟原虫（Plasmodium falciparum）表现出良好的活性（IC50 为 0.61 μM），并且对其他引起热带病的原生动物病原体也具有活性。