論文

査読有り
2011年9月

Schistosomicidal and antifecuridity effects of oral treatment of synthetic endoperoxide N-89

PARASITOLOGY INTERNATIONAL
  • Toshie Taniguchi
  • Takashi Kumagai
  • Rieko Shimogawara
  • Shizuko Ichinose
  • Akiko Hiramoto
  • Akira Sato
  • Masayuki Morita
  • Masatomo Nojima
  • Hye-Sook Kim
  • Yusuke Wataya
  • Nobuo Ohta
  • 全て表示

60
3
開始ページ
231
終了ページ
236
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.parint.2011.02.007
出版者・発行元
ELSEVIER IRELAND LTD

1,2,6,7-Tetraoxaspiro[7.11]nonadecane (N-89) is a chemically synthesized compound with good efficacy against malaria parasites. We observed strong anti-schistosomal activities of N-89 both in vitro and in vivo. In a murine model with experimental infection of Schistosoma mansoni, orally administered N-89 at the dose of 300 mg/kg resulted in a significant reduction in worm burden (63%) when mice were treated at 2-weeks postinfection. Strong larvicidal effects of N-89 were confirmed in vitro; schistosomula of S. mansoni were killed by N-89 at an EC50 of 16 nM. In contrast, no significant reduction in worm burden was observed when N-89 was administered at 5 weeks postinfection in vivo. However, egg production was markedly suppressed by N-89 treatment at that time point. On microscopic observation, the intestine of N-89-treated female worms seemed to be empty compared with the control group, and the mean body length was significantly shorter than that of controls. Nutritional impairment in the parasite due to N-89 treatment was possible, and therefore quantification of hemozoin was compared between parasites with or without N-89 treatment. We found that the hemozoin content was significantly reduced in N-89 treated parasites compared with controls (P<0.001). The surface of adult worms was observed by scanning and transmission electron microscopy, but there were no apparent changes. Taken together, these observations suggested that N-89 has strong antischistosomal effects, probably through a unique mode of drug efficacy. As N-89 is less toxic to mammalian host animals, it is a possible drug candidate against schistosomiasis. (C) 2011 Elsevier Ireland Ltd. All rights reserved.

リンク情報
DOI
https://doi.org/10.1016/j.parint.2011.02.007
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/21397716
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000292673800001&DestApp=WOS_CPL
ID情報
  • DOI : 10.1016/j.parint.2011.02.007
  • ISSN : 1383-5769
  • PubMed ID : 21397716
  • Web of Science ID : WOS:000292673800001

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