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

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...

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Autores principales: Glaser, Jan, Schurigt, Uta, Suzuki, Brian M., Caffrey, Conor R., Holzgrabe, Ulrike
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272620/
https://www.ncbi.nlm.nih.gov/pubmed/26076109
http://dx.doi.org/10.3390/molecules200610873
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author Glaser, Jan
Schurigt, Uta
Suzuki, Brian M.
Caffrey, Conor R.
Holzgrabe, Ulrike
author_facet Glaser, Jan
Schurigt, Uta
Suzuki, Brian M.
Caffrey, Conor R.
Holzgrabe, Ulrike
author_sort Glaser, Jan
collection PubMed
description 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.
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spelling pubmed-62726202018-12-31 Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni Glaser, Jan Schurigt, Uta Suzuki, Brian M. Caffrey, Conor R. Holzgrabe, Ulrike Molecules Article 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. MDPI 2015-06-12 /pmc/articles/PMC6272620/ /pubmed/26076109 http://dx.doi.org/10.3390/molecules200610873 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Glaser, Jan
Schurigt, Uta
Suzuki, Brian M.
Caffrey, Conor R.
Holzgrabe, Ulrike
Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni
title Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni
title_full Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni
title_fullStr Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni
title_full_unstemmed Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni
title_short Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni
title_sort anti-schistosomal activity of cinnamic acid esters: eugenyl and thymyl cinnamate induce cytoplasmic vacuoles and death in schistosomula of schistosoma mansoni
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272620/
https://www.ncbi.nlm.nih.gov/pubmed/26076109
http://dx.doi.org/10.3390/molecules200610873
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