Antimalarial activity of endoperoxide compound 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol

Akira Sato, Akiko Hiramoto, Masayuki Morita, Masahiro Matsumoto, Yuka Komich, Yukari Nakase, Natsuki Tanigawa, Osamu Hiraoka, Kazuyuki Hiramoto, Hikoya Hayatsu, Kazutaka Higaki, Satoru Kawai, Araki Masuyama, Masatomo Nojima, Yusuke Wataya, Hye Sook Kim

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

Plasmodium falciparum, the major causative parasite for the disease, has acquired resistance to most of the antimalarial drugs used today, presenting an immediate need for new antimalarial drugs. Here, we report the in vitro and in vivo antimalarial activities of 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251) against P. falciparum and Plasmodium berghei parasites. The N-251 showed high antimalarial potencies both in the in vitro and the in vivo tests (EC 50 2.3×10 -8 M; ED 50 15mg/kg (per oral)). The potencies were similar to that of artemisinin in vitro and greater than artemisinin's activity in vivo (p.o.). In addition, N-251 has little toxicity: a single oral administration at 2000mg/kg to a rat gave no health problems to it. Administration of N-251 to mice bearing 1% of parasitemia (per oral 68mg/kg, 3 times a day for 3 consecutive days) resulted in a dramatic decrease in the parasitemia: all the 5 mice given N-251 were cured without any recurrence, with no diarrhea or weight loss occurring in the 60days of experiment. N-251 deserves more extensive clinical evaluation, desirably including future trials in the human.

Original languageEnglish
Pages (from-to)270-273
Number of pages4
JournalParasitology International
Volume60
Issue number3
DOIs
Publication statusPublished - Sep 1 2011

Keywords

  • 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251)
  • Antimalarial activity
  • Endoperoxide compound
  • Plasmodium berghei
  • Plasmodium falciparum

ASJC Scopus subject areas

  • Parasitology
  • Infectious Diseases

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    Sato, A., Hiramoto, A., Morita, M., Matsumoto, M., Komich, Y., Nakase, Y., Tanigawa, N., Hiraoka, O., Hiramoto, K., Hayatsu, H., Higaki, K., Kawai, S., Masuyama, A., Nojima, M., Wataya, Y., & Kim, H. S. (2011). Antimalarial activity of endoperoxide compound 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol. Parasitology International, 60(3), 270-273. https://doi.org/10.1016/j.parint.2011.04.001