Stage specific activity of synthetic antimalarial endoperoxides, N-89 and N-251, against Plasmodium falciparum

Masayuki Morita; Takahiko Koyama; Hitomi Sanai; Akira Sato; Akiko Hiramoto; Araki Masuyama; Masatomo Nojima; Yusuke Wataya; Hye Sook Kim

doi:10.1016/j.parint.2014.10.007

Stage specific activity of synthetic antimalarial endoperoxides, N-89 and N-251, against Plasmodium falciparum

Masayuki Morita, Takahiko Koyama, Hitomi Sanai, Akira Sato, Akiko Hiramoto, Araki Masuyama, Masatomo Nojima, Yusuke Wataya, Hye Sook Kim

Research output: Contribution to journal › Article

5 Citations (Scopus)

Abstract

We have reported that two endoperoxides, N-89 and N-251, synthesized in 2001, possess potent antimalarial activities. Aiming at their eventual use for curing malaria in humans, we have been investigating various aspects of their antimalarial actions. Here we show that N-89 and N-251 inhibit the growth of Plasmodium falciparum within human erythrocytes in vitro at its lifecycle stage 'trophozoite' specifically. It is known that artemisinin compounds, which are currently used for curing malaria, have other stage-specificities. Therefore, it is likely that the antimalarial mechanism of N-89 and N-251 differs from those of artemisinin compounds. As malaria parasites resistant to artemisinin-based combination therapy are currently emerging in some tropical regions, N-89 and N-251 are candidates for overcoming these new problems.

Original language	English
Pages (from-to)	113-117
Number of pages	5
Journal	Parasitology International
Volume	64
Issue number	1
DOIs	https://doi.org/10.1016/j.parint.2014.10.007
Publication status	Published - Feb 1 2015

Keywords

Antimalarial candidates
N-251
N-89
Stage-specificity
Synthetic endoperoxides

ASJC Scopus subject areas

Parasitology
Infectious Diseases

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Morita, M., Koyama, T., Sanai, H., Sato, A., Hiramoto, A., Masuyama, A., Nojima, M., Wataya, Y., & Kim, H. S. (2015). Stage specific activity of synthetic antimalarial endoperoxides, N-89 and N-251, against Plasmodium falciparum. Parasitology International, 64(1), 113-117. https://doi.org/10.1016/j.parint.2014.10.007

Stage specific activity of synthetic antimalarial endoperoxides, N-89 and N-251, against Plasmodium falciparum. / Morita, Masayuki; Koyama, Takahiko; Sanai, Hitomi; Sato, Akira; Hiramoto, Akiko; Masuyama, Araki; Nojima, Masatomo; Wataya, Yusuke; Kim, Hye Sook.

In: Parasitology International, Vol. 64, No. 1, 01.02.2015, p. 113-117.

Research output: Contribution to journal › Article

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abstract = "We have reported that two endoperoxides, N-89 and N-251, synthesized in 2001, possess potent antimalarial activities. Aiming at their eventual use for curing malaria in humans, we have been investigating various aspects of their antimalarial actions. Here we show that N-89 and N-251 inhibit the growth of Plasmodium falciparum within human erythrocytes in vitro at its lifecycle stage 'trophozoite' specifically. It is known that artemisinin compounds, which are currently used for curing malaria, have other stage-specificities. Therefore, it is likely that the antimalarial mechanism of N-89 and N-251 differs from those of artemisinin compounds. As malaria parasites resistant to artemisinin-based combination therapy are currently emerging in some tropical regions, N-89 and N-251 are candidates for overcoming these new problems.",

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