Anti-Malarial Activity of Allyl Isothiocyanate and N-acetyl-S-(N-allylthiocarbamoyl)-l-Cysteine.

SCOPE: Malaria remains one of the most important infectious diseases in the world. Allyl isothiocyanate (AITC) is a main ingredient of traditional spice Wasabia japonica, which is reported to have anti-bacterial and antiparasitic activities. However, there is no information on effects of AITC against malaria. The present study investigates the anti-malarial activity of dietary AITC in vivo and that of AITC metabolites in vitro. METHODS AND RESULTS: The ad libitum administration of 35, 175, or 350 µM AITC-containing drinking water to ICR mice significantly inhibit the parasitemia induced after infection with Plasmodium berghei. On the other hand, after single oral administration of AITC (20 mg kg-1 body weight), N-acetyl-S-(N-allylthiocarbamoyl)-l-cysteine (NAC-AITC) as one of the AITC metabolites displays a serum Cmax of 11.4 µM at a Tmax of 0.5 h, but AITC is not detected at any time point. Moreover, NAC-AITC shows anti-malarial activity against Plasmodium falciparum in vitro, and its 50% inhibitory concentration (IC50 ) against parasitemia is 12.6 µM. CONCLUSIONS: These results indicate that orally administered AITC is metabolized to NAC-AITC and exerts anti-malarial activity against malaria parasites in blood, suggesting that the consumption of AITC-containing food stuffs such as cruciferous plants may prevent malaria.