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Molecules 2015, 20(6), 10873-10883; doi:10.3390/molecules200610873

Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni

1
Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany
2
Institute for Molecular Infection Biology, University of Wuerzburg, Josef-Schneider-Str. 2/D15, D-97080 Wuerzburg, Germany
3
Center for Discovery and Innovation in Parasitic Diseases, University of California, San Francisco, 1700 4th St., San Francisco, CA 94158, USA
4
Department of Pathology, University of California, San Francisco, CA 94158, USA
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 5 May 2015 / Revised: 3 June 2015 / Accepted: 8 June 2015 / Published: 12 June 2015
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Abstract

Bornyl caffeate (1) was previously isolated by us from Valeriana (V.) wallichii rhizomes and identified as an anti-leishmanial substance. Here, we screened a small compound library of synthesized derivatives 130 for activity against schistosomula of Schistosoma (S.) mansoni. Compound 1 did not show any anti-schistosomal activity. However, strong phenotypic changes, including the formation of vacuoles, degeneration and death were observed after in vitro treatment with compounds 23 (thymyl cinnamate) and 27 (eugenyl cinnamate). Electron microscopy analysis of the induced vacuoles in the dying parasites suggests that 23 and 27 interfere with autophagy. View Full-Text
Keywords: Schistosoma; schistosomula; parasite; eugenyl cinnamate; thymyl cinnamate; vacuoles; autophagy; anti-schistosomal activity Schistosoma; schistosomula; parasite; eugenyl cinnamate; thymyl cinnamate; vacuoles; autophagy; anti-schistosomal activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Glaser, J.; Schurigt, U.; Suzuki, B.M.; Caffrey, C.R.; Holzgrabe, U. Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni. Molecules 2015, 20, 10873-10883.

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