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来自麻风树的环肽ribifolin及其潜在的抗疟活性。

Ribifolin, an orbitide from Jatropha ribifolia, and its potential antimalarial activity.

作者信息

Pinto Meri Emili F, Batista João M, Koehbach Johannes, Gaur Pratibha, Sharma Abhinay, Nakabashi Myna, Cilli Eduardo Maffud, Giesel Guilherme M, Verli Hugo, Gruber Christian W, Blanch Ewan W, Tavares Joseam F, da Silva Marcelo S, Garcia Celia R S, Bolzani Vanderlan S

机构信息

†Institute of Chemistry, São Paulo State University-UNESP, 14800-060, Araraquara, São Paulo, Brazil.

‡Manchester Institute of Biotechnology and Faculty of Life Sciences, The University of Manchester, M1 7DN, Manchester, United Kingdom.

出版信息

J Nat Prod. 2015 Mar 27;78(3):374-80. doi: 10.1021/np5007668. Epub 2015 Feb 20.

Abstract

A new orbitide named ribifolin was isolated and characterized from Jatropha ribifolia using mass spectrometry, NMR spectroscopy, quantitative amino acid analysis, molecular dynamics/simulated annealing, and Raman optical activity measurements and calculations. Ribifolin (1) and its linear form (1a) were synthesized by solid-phase peptide synthesis, followed by evaluation of its antiplasmodial and cytotoxicity activities. Compound 1 was moderately effective (IC50 = 42 μM) against the Plasmodium falciparum strain 3D7.

摘要

从麻风树中分离出一种名为ribifolin的新环肽,并通过质谱、核磁共振光谱、定量氨基酸分析、分子动力学/模拟退火以及拉曼光学活性测量和计算对其进行了表征。通过固相肽合成法合成了ribifolin(1)及其线性形式(1a),随后评估了其抗疟和细胞毒性活性。化合物1对恶性疟原虫3D7株具有中等效果(IC50 = 42 μM)。

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