Anthelmintic cycicooctadepsipeptides: complex in structure and mode of action

作者：Kruecken Juergen; Harder Achim; Jeschke Peter; Holden Dye Lindy; O' Connor Vincent; Welz Claudia; von Samson Himmelstjerna Georg^*

来源：Trends in Parasitology, 2012, 28(9): 385-394.

DOI：10.1016/j.pt.2012.06.005

• anthelmintic cycicooctadepsipeptides
• emodepside
• PF1022A
• SLO-1
• lathrophilin
• Rosellinia
• PF1022A synthesis

The broad-spectrum anthelmintic cyclooctadepsipeptide PF1022A is a fungal metabolite from Rosellinia sp. PF1022, which is a Mycelia sterilia found on the leaves of Camellia japonica. A broad range of structurally related cyclooctadepsipeptides has been characterized and tested for anthelmintic activities. These metabolites have been used as starting points to generate semisynthetic derivatives with varying nematocidal capacity. Predominant among these compounds is emodepside, which exhibits a broad nematocidal potential against gastrointestinal and extraintestinal parasites. Here we review the chemical biology and mode of action of cyclooctadepsides with particular attention to PF1022A and emodepside. We illustrate how they target nematode neuromuscular function, opening up new avenues for antiparasitic treatments with potential capability for important selective toxicity.

• 出版日期2012-9