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

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

Zhao L1,2, Kaiser M3,4, Bode HB1,5.

Author information

1
Molekulare Biotechnologie, Fachbereich Biowissenschaften , Goethe Universität Frankfurt , 60438 Frankfurt am Main , Germany.
2
Institute of Botany, Jiangsu Province and Chinese Academy of Sciences , 210014 Nanjing , China.
3
Parasite Chemotherapy , Swiss Tropical and Public Health Institute , 4051 Basel , Switzerland.
4
University of Basel , 4003 Basel , Switzerland.
5
Buchmann Institute for Molecular Life Sciences (BMLS) , Goethe Universität Frankfurt , 60438 Frankfurt am Main , Germany.

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 IC50 values of 0.07-6.25 and 0.091-3.16 μM, respectively, making them the most active RXP derivatives known to date.

PMID:
30095261
DOI:
10.1021/acs.orglett.8b01975
[Indexed for MEDLINE]

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