Planta Med 2003; 69(6): 527-531
DOI: 10.1055/s-2003-40640
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Antiparasitic Activity of Marine Pyridoacridone Alkaloids Related to the Ascididemins

Brent R. Copp1 , Oliver Kayser2 , Reto Brun3 , Albrecht F. Kiderlen4
  • 1Department of Chemistry, University of Auckland, Auckland, New Zealand
  • 2Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany
  • 3Schweizerisches Tropeninstitut, Basel, Switzerland
  • 4Department of Infectious Diseases, Robert Koch-Institut, Berlin, Germany
Further Information

Publication History

Received: October 2, 2002

Accepted: February 15, 2003

Publication Date:
16 July 2003 (online)

Abstract

A series of pyridoacridone alkaloids, including the marine alkaloid ascididemin were tested in vitro for antiparasitic activity against P. falciparum (K1, NF54), L. donovani, T. cruzi, T. b. rhodesiense and two mammalian cell lines (L6, RAW 264.7). Most compounds showed high antiplasmodial activity, moderate antileishmanial activity against both extra- and intracellular forms, and significant trypanocidal effects against T. cruzi and T. b. brucei. However, when tested against mammalian cell lines, most of the compounds were also toxic for macrophage-like RAW 264.7 cells and skeletal muscle myoblast L6 cells. Correlations between molecular structures and antiparasitic activity are discussed in detail. Specific compounds are illustrated with emphasis on their potential as new antiparasitic drug leads.

References

Dr. Oliver Kayser

Freie Universität Berlin

Institut für Pharmazie

Pharmazeutische Biotechnologie

Kelchstraße 31

12169 Berlin

Germany

Phone: +49-30-838 50689

Fax: +49-30-838 50605

Email: kayser@zedat.fu-berlin.de