Anti-promastigote activity of dillapiole and isodillapiole against Leishmania chagasi

Leishmaniasis is still a worldwide health problem with 12 million people infected around the world and with 200 million people living at risk areas in 80 countries. Pentavalent antimonals are the main line treatment for leishmaniasis. Disadvantages such as costs, long-term treatment, side effects and low efficacy against and resistance to many strains have been reported. The search for newer substances obtained from natural products that can be used as prototypes potentially superior semi-synthetic analogues is currently an area of great interest. Dillapiole is the major component of the essential oil extracted from Piper aduncum. The aim of this work was to evaluate the leishmanicidal activity of dillapiole and the semi-synthetic analogues isodillapiole against promastigotes of L. chagasi. The anti-promastigote activity was evaluated as proposed by Delorenzi et al (2001). Promastigotes were incubated in the presence of different concentrations of Dillapiole and Isodillapiole, which were added only once to the cultures. After 3 days at 26°C, parasite survival was estimated by counting viable or motile forms. Both drugs exhibited a strong anti-promastigote activity, reducing parasite survival in 99 and 96%, respectively, when we used 50µg/ml of the drugs. Both drugs also showed a concentration dependent activity, however, isodillapiole was less active in lower concentrations. DMSO 1% was used as solvent control. No toxicity to the macrophages was observed after the treatment with the drugs, as measured by their spreading and adherence to glass surface.

Acknowledgements: Hebron Farmacêutica, MackPesquisa, PIBIC/Mackenzie.

References: 1. DELORENZI et al. DOI:10.1128/AAC.45.5.1349–1354.2001.