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Ionophore and Anthelmintic Activity of PF 1022A, a Cyclooctadepsipeptide, Are Not Related

✍ Scribed by Geßner, Guido; Meder, Sabine; Rink, Thomas; Boheim, Günther; Harder, Achim; Jeschke, Peter; Scherkenbeck, Jürgen; Londershausen, Michael

Publisher
John Wiley and Sons
Year
1996
Tongue
English
Weight
841 KB
Volume
48
Category
Article
ISSN
1526-498X

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✦ Synopsis

PF 1022A, a 24-membered cyclooctadepsipeptide and a potent anthelmintic drug, is active against nematodes but not against arthropods. Muscle cells of Ascaris suum generate autorhythmic spikes in electrophysiological control experiments. Exposure of the worm to PF 1022A leads to flaccid paralysis and in parallel to the disappearance of these spike events. Results of such experiments in vitro were compared with those from experiments using planar lipid bilayer membranes incorporating PF 1022A, a related linear octadepsipeptide and other cyclodepsipeptides.

Whereas PF 1022A acts both as an ionophore in lipid bilayers, similar to other cyclodepsipeptides like valinomycin and enniatin A, and as a paralysing drug in worms, some of the series of depsipeptides examined have only an ion carrier function, while others exhibit only nematocidal activity. It is concluded that the ion carrier property of PF 1022A is not responsible for its paralyzing effect on nematodes and that there is a specific binding site for PF 1022A in nematodes. Binding may trigger the lethal reaction cascade, which is responsible for anthelmintic activity.

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A mono-proline analogue of the potent anthelmintic cyclooctadepsipeptide PF1022A has been synthesized. NMR studies in combination with molecular dynamics simulations demonstrate that the conürmation of this analogue is both rigidiüed and distorted compared with the asymmetric conformation of PF1022A