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

Molecules

Jan Glaser³  Uta Schurigt²  Brian M. Suzuki¹  Conor R. Caffrey¹  Ulrike Holzgrabe³ 

[1] Center for Discovery and Innovation in Parasitic Diseases, University of California, San Francisco, 1700 4th St., San Francisco, CA 94158, USA; E-Mails:;Institute for Molecular Infection Biology, University of Wuerzburg, Josef-Schneider-Str. 2/D15, D-97080 Wuerzburg, Germany;Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany; E-Mails:

关键词: Schistosoma;    schistosomula;    parasite;    eugenyl cinnamate;    thymyl cinnamate;    vacuoles;    autophagy;    anti-schistosomal activity;   

DOI  :  10.3390/molecules200610873

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.