Diatretol, an α, α'-dioxo-diketopiperazine, is a potent in vitro and in vivo antimalarial

Aki Ishiyama; Rei Hokari; Kenichi Nonaka; Takuya Chiba; Hiromi Miura; Kazuhiko Otoguro; Masato Iwatsuki

doi:10.1038/s41429-020-00390-2

Diatretol, an α, α'-dioxo-diketopiperazine, is a potent in vitro and in vivo antimalarial

J Antibiot (Tokyo). 2021 Apr;74(4):266-268. doi: 10.1038/s41429-020-00390-2. Epub 2021 Jan 14.

Authors

Aki Ishiyama^#^{1

2}, Rei Hokari^#¹, Kenichi Nonaka^{1

2}, Takuya Chiba², Hiromi Miura^{1

2}, Kazuhiko Otoguro¹, Masato Iwatsuki^{3

4}

Affiliations

¹ Ōmura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
² Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
³ Ōmura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan. iwatuki@lisci.kitasato-u.ac.jp.
⁴ Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan. iwatuki@lisci.kitasato-u.ac.jp.

^# Contributed equally.

Abstract

A fungal metabolite, diatretol, has shown to be a promising antimalarial agent. Diatretol displayed potent in vitro antiparasitic activity against the Plasmodium falciparum K1 strain, with an IC₅₀ value of 378 ng ml^-1, as well as in vivo efficacy in a Plasmodium berghei-infected mice model, with ca. 50% inhibition at 30 mg/kg (p.o.).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antimalarials / chemistry
Antimalarials / pharmacology*
Diketopiperazines / chemistry
Disease Models, Animal
Drug Evaluation, Preclinical
Erythrocytes / parasitology
Humans
Malaria / drug therapy*
Malaria / parasitology
Mice
Mice, Inbred ICR
Parasitemia / drug therapy
Parasitemia / parasitology
Plasmodium berghei / parasitology
Plasmodium falciparum / drug effects

Substances

Antimalarials
Diketopiperazines