Bioassay-guided isolation of dehydrocostus lactone from Echinops kebericho as a leishmanicidal drug

Abstract

Several strains of Leishmania parasite are involved in the occurrence of leishmaniasis infections, which makes its prevention and treatment very challenging. Currently, all forms of leishmaniasis are being treated with chemical drugs, which have limitations and adverse effects. Discovering antileishmanial agents from natural sources can lead to novel drugs against this dreadful disease. The essential oils and nonpolar solvent extracts of the roots of E. kebericho exhibit antileishmanial activity. Thus, the isolation of the leishmanicidal compounds from the roots of E. kebericho through a bioassay-guided technique was carried out in this study. The present finding showed that the essential oil and hexane fraction of crude extract from the roots of E. kebericho possessed significant leishmanicidal activity against L. major and L. tropica. Dehydrocostus lactone (1), one of the major constituents of the essential oil and hexane fraction, was more active than the standard drug miltefosine against L. major and L. tropica promastigotes. The presence of α-methylene, γ-lactone is the responsible moiety of dehydrocostus lactone towards the leishmanicidal activity against the tested Leishmania species. The MTT assay of dehydrocostus lactone showed inactive toxicity against the human cervical carcinoma HeLa cells. In addition, dehydrocostus lactone exhibits a broad spectrum of antibiotic activities. Based on this interesting finding, dehydrocostus lactone was identified as a potential lead for treating infections caused by Leishmania.