Anti-leishmanial and anti-trypanosomal potential of polygodial isolated from stem barks of Drimys brasiliensis Miers (Winteraceae)

Abstract

Parasitic protozoan diseases affect the poorest population in developing countries. Leishmaniasis and Chagas disease have been included among the most important threats for public health in Central and South American continent, with few therapeutic alternatives and highly toxic drugs. In the course of selection of novel drug candidates, we studied the anti-protozoal potential of Drimys brasiliensis. Thus, the crude hexane extract from stem bark as well as its main derivative, the sesquiterpene polygodial, were tested using in vitro assays. The crude hexane extract and polygodial showed activity against Leishmania spp. in the range between 22 and 62 μg/mL, but polygodial demonstrated high parasite selectivity towards Trypanosoma cruzi trypomastigotes (2 μg/mL), with a selectivity index of 19. Finally, polygodial showed a leishmanicidal effect, inducing intense ultrastructural damages in Leishmania in short-time incubation. The obtained results suggested that polygodial could be used as a tool for drug design studies against protozoan diseases and as a candidate molecule for further in vivo studies against T. cruzi.

Drimanes from Drimys brasiliensis with leishmanicidal and antimalarial activity

“…Previous studies have indicated that both a crude hexane extract of D. brasiliensis and polygodial show activity against Leishmania spp when applied in the range of 22-62 µg/mL and polygodial demonstrated high selectivity towards T. cruzi trypomastigotes (2 µg/mL) (Corrêa et al 2011). The drimanes 9-epideoxymuzigadial, 9-deoxymuzigadial, muzigadial and 3-β-acetoxypolygodial isolated from a hexane extract of the leaves of Canella winterana exhibited strong activity against the chloroquine-sensitive strain of P. falciparum, producing IC 50 values of 1.01, 2.19, 0.31 and 2.77 µg/mL, respectively (Grace et al 2010).…”

“…It has recently been demonstrated that a hexane extract of the stem bark of Drimys brasiliensis and polygodial, a drimane, exhibit activity against Leishmania spp and Trypanosoma cruzi (Corrêa et al 2011). This information contributes to the further study of this plant species, with the aim of obtaining new drugs to treat the neglected diseases.…”

Antiparasitic activity of natural and semi-synthetic tirucallane triterpenoids from Schinus terebinthifolius (Anacardiaceae) – Structure/activity relationships

“…NCTC (clone 929) cells were maintained in RPMI-1640 (without phenol red and supplemented with 10% FBS) at 37 °C in a humidified atmosphere containing 5% CO 2 [31].…”

Phytotoxic activity of differents plant parts of Drimys brasiliensis miers on germination and seedling development

“…In this species, sesquiterpene drimanes are predominant, including polygodial, 1-β-(p-methoxycinnamoyl)-polygodial and drimanial CECHINEL-FILHO et al, 1998;MALHEIROS et al, 2001;. These compounds exhibit antinociceptive (EL-SAYAH et al, 2000), antihyperalgesic (MEN-DES et al, 1998), antifungal (MALHEIROS et al, 2005, anti-inflammatory (LAGO et al, 2010), antibacterial (SILVEIRA et al, 2012), leishmanicidal and antimalarial activities (CORRÊA et al, 2011;CLAUDINO et al, 2013). However, few studies have examined the phytotoxicity of D. brasiliensis on other plants.…”