Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4.

Journal article

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.

Authors: Grundmann, F; Kaiser, M; Schiell, M; Batzer, A; Kurz, M

• Publication status: Published
• Publisher: American Chemical Society
• Journal: Journal of natural products
• Volume: 77
• Issue: 4
• Pages: 779-783
• Publication date: 2014-04-01
• DOI: 10.1021/np4007525
• EISSN: 1520-6025
• ISSN: 0163-3864
• Language: English
• Keywords: Plasmodium falciparum; Animals; Bacillus subtilis; Xenorhabdus; Parasitic Sensitivity Tests; Nematoda; Inhibitory Concentration 50; Trypanosoma cruzi; Nuclear Magnetic Resonance, Biomolecular; Saccharomyces cerevisiae; Micrococcus luteus; Molecular Structure; Thailand; Depsipeptides; Escherichia coli; Antiparasitic Agents; Humans; Trypanosoma brucei rhodesiense