Diatretol, an &#945;, &#945;'-dioxo-diketopiperazine, is a potent in vitro and in vivo antimalarial.

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

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

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

Afiliação

Ishiyama A; Omura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Hokari R; Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Nonaka K; Omura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Chiba T; Omura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Miura H; Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Otoguro K; Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.
Iwatsuki M; Omura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, 108-8641, Tokyo, Japan.

J Antibiot (Tokyo) ; 74(4): 266-268, 2021 04.

Article em En | MEDLINE | ID: mdl-33446930

ABSTRACT

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.).

Assuntos

Antimaláricos/farmacologia; Malária/tratamento farmacológico; Animais; Antimaláricos/química; Dicetopiperazinas/química; Modelos Animais de Doenças; Avaliação Pré-Clínica de Medicamentos; Eritrócitos/parasitologia; Humanos; Malária/parasitologia; Camundongos Endogâmicos ICR; Parasitemia/tratamento farmacológico; Parasitemia/parasitologia; Plasmodium berghei/parasitologia; Plasmodium falciparum/efeitos dos fármacos

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Malária / Antimaláricos Limite: Animals / Humans Idioma: En Revista: J Antibiot (Tokyo) Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Japão

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