Antimicrob Agents Chemother. 2003 Jun; 47(6): 1895-901.

Antileishmanial activity of a linalool-rich essential oil from Croton cajucara.

do Socorro S Rosa Mdo S, MendonÃ§a-Filho RR, Bizzo HR, de Almeida Rodrigues I, Soares RM, Souto-PadrÃ³n T, Alviano CS, Lopes AH.

Instituto de Microbiologia Prof. Paulo de GÃ³es, Centro de CiÃªncias da SaÃºde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, R.J., 219491-590, Brazil.

The in vitro leishmanicidal effects of a linalool-rich essential oil from the leaves of Croton cajucara against Leishmania amazonensis were investigated. Morphological changes in L. amazonensis promastigotes treated with 15 ng of essential oil per ml were observed by transmission electron microscopy; leishmanial nuclear and kinetoplast chromatin destruction, followed by cell lysis, was observed within 1 h. Pretreatment of mouse peritoneal macrophages with 15 ng of essential oil per ml reduced by 50% the interaction between these macrophages and L. amazonensis, with a concomitant increase by 220% in the level of nitric oxide production by the infected macrophages. Treatment of preinfected macrophages with 15 ng of essential oil per ml reduced by 50% the interaction between these cells and the parasites, which led to a 60% increase in the amount of nitric oxide produced by the preinfected macrophages. These results provide new perspectives on the development of drugs with activities against Leishmania, as linalool-rich essential oil is a strikingly potent leishmanicidal plant extract (50% lethal doses, 8.3 ng/ml for promastigotes and 8.7 ng/ml for amastigotes) which inhibited the growth of L. amazonensis promastigotes at very low concentrations (MIC, 85.0 pg/ml) and which presented no cytotoxic effects against mammalian cells.