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Molecules 2014, 19(5), 6070-6079; doi:10.3390/molecules19056070
Article

In Vitro Leishmanicidal Activities of Sesquiterpene Lactones from Tithonia diversifolia against Leishmania braziliensis Promastigotes and Amastigotes

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Received: 20 March 2014; in revised form: 9 May 2014 / Accepted: 12 May 2014 / Published: 14 May 2014
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Abstract: Natural compounds represent a rich and promising source of novel, biologically active chemical entities for treating leishmaniasis. Sesquiterpene lactones are a recognized class of terpenoids with a wide spectrum of biological activities, including activity against Leishmania spp. In this work, a sesquiterpene lactone-rich preparation—a leaf rinse extract (LRE) from Tithonia diversifolia—was tested against promastigote forms of L. braziliensis. The results revealed that the LRE is a rich source of potent leishmanicidal compounds, with an LD50 value 1.5 ± 0.50 µg·mL−1. Therefore, eight sesquiterpene lactones from the LRE were initially investigated against promastigote forms of L. braziliensis. One of them did not present any significant leishmanicidal effect (LD50 > 50 µg·mL−1). Another had a cytotoxic effect against macrophages (4.5 µg·mL−1). The five leishmanicidal compounds with the highest level of selectivity were further evaluated against intracellular parasites (amastigotes) using peritoneal macrophages. Tirotundin 3-O-methyl ether, tagitinin F, and a guaianolide reduced the internalization of parasites after 48 h, in comparison with the negative control. This is the first report on sesquiterpene lactones that have potent leishmanicidal effects on both developmental stages of L. braziliensis.
Keywords: Tithonia diversifolia; Asteraceae; sesquiterpene lactones; antileishmanial activity; Leishmania braziliensis Tithonia diversifolia; Asteraceae; sesquiterpene lactones; antileishmanial activity; Leishmania braziliensis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

de Toledo, J.S.; Ambrósio, S.R.; Borges, C.H.G.; Manfrim, V.; Cerri, D.G.; Cruz, A.K.; Da Costa, F.B. In Vitro Leishmanicidal Activities of Sesquiterpene Lactones from Tithonia diversifolia against Leishmania braziliensis Promastigotes and Amastigotes. Molecules 2014, 19, 6070-6079.

AMA Style

de Toledo JS, Ambrósio SR, Borges CHG, Manfrim V, Cerri DG, Cruz AK, Da Costa FB. In Vitro Leishmanicidal Activities of Sesquiterpene Lactones from Tithonia diversifolia against Leishmania braziliensis Promastigotes and Amastigotes. Molecules. 2014; 19(5):6070-6079.

Chicago/Turabian Style

de Toledo, Juliano S.; Ambrósio, Sergio R.; Borges, Carly H.G.; Manfrim, Viviane; Cerri, Daniel G.; Cruz, Angela K.; Da Costa, Fernando B. 2014. "In Vitro Leishmanicidal Activities of Sesquiterpene Lactones from Tithonia diversifolia against Leishmania braziliensis Promastigotes and Amastigotes." Molecules 19, no. 5: 6070-6079.



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