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

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

  • Molecules. 2015 Jun 12;20(6):10873-83. doi: 10.3390/molecules200610873.
Jan Glaser 1,  Uta Schurigt 2,  Brian M Suzuki 3 4,  Conor R Caffrey 5 6,  Ulrike Holzgrabe 7
Affiliations

Affiliations

  • 1 Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany. [email protected].
  • 2 Institute for Molecular Infection Biology, University of Wuerzburg, Josef-Schneider-Str. 2/D15, D-97080 Wuerzburg, Germany. [email protected].
  • 3 Center for Discovery and Innovation in Parasitic Diseases, University of California, San Francisco, 1700 4th St., San Francisco, CA 94158, USA. [email protected].
  • 4 Department of Pathology, University of California, San Francisco, CA 94158, USA. [email protected].
  • 5 Center for Discovery and Innovation in Parasitic Diseases, University of California, San Francisco, 1700 4th St., San Francisco, CA 94158, USA. [email protected].
  • 6 Department of Pathology, University of California, San Francisco, CA 94158, USA. [email protected].
  • 7 Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany. [email protected].
PMID: 26076109 DOI: 10.3390/molecules200610873
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 1-30 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.

Keywords

Schistosoma; anti-schistosomal activity; autophagy; eugenyl cinnamate; parasite; schistosomula; thymyl cinnamate; vacuoles.

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